€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****AMERICAN JOURNAL OF CHINESE MEDICINE***** Lin CC Shieh DE The anti-inflammatory activity of Scutellaria rivularis extracts and its active components, baicalin, baicalein and wogonin. In: Am J Chin Med (1996) 24(1):31-6 ISSN: 0192-415X Five extracts (n-hexane, chloroform, ethyl acetate, n-butanol and water) of Scutellaria rivularis Benth. were evaluated for their anti- inflammatory activity against carrageenan-induced paw edema in rats and compared with indomethacin. The result indicated that chloroform extract proved to be the most effective in all of the extracts. Consequently, three major components (baicalin, baicalein and wogonin) of the chloroform extract were further tested for their anti- inflammatory activity using the same model. It was found that baicalin exhibits the greatest inhibition activity against carrageenan-induced rat paw edema. Registry Numbers: 21967-41-9 (baicalin) 491-67-8 (baicalein) 632-85-9 (wogonin) 9000-07-1 (Carrageenan) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Kang JJ Chen YC Kuo WC Chen T Cheng YW Kuo ML Ueng TH Modulation of microsomal cytochrome P450 by Scutellariae Radix and Gentianae scabrae Radix in rat liver. In: Am J Chin Med (1996) 24(1):19-29 ISSN: 0192-415X The present study has determined the effects of Scutellariae Radix (Huangqin) and Gentianae scabrae Radix (Longdan) on liver microsomal cytochrome P450 (P450)-dependent mono-oxygenases using rats pretreated with crude extracts of medicinal herbs. Scutellariae Radix resulted in a 53% decrease of pentoxyresorufin O-dealkylase activity in liver microsomes. In contrast, Gentianae scabrae Radix caused a 50% increase of benzo(a)pyrene hydroxylase activity. Immunoblotting analysis of liver microsomes revealed that Scutellariae Radix induced and suppressed the levels of P450 1A and 2B proteins, respectively. Scutellariae and Gentianae scabrae Radixes had no effects on microsomal aniline hydroxylase activity and P450 2E1 protein. Registry Numbers: 9035-51-2 (Cytochrome P-450) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Chiu HF Lin CC Yen MH Wu PS Yang CY Pharmacological and pathological studies on hepatic protective crude drugs from Taiwan (V): The effects of Bombax malabarica and Scutellaria rivularis. In: Am J Chin Med (1992) 20(3-4):257-64 ISSN: 0192-415X Bombax malabarica DC and Scutellaria rivularis B. were extracted in boiling water and concentrated into 1g/ml solution to investigate their hepatoprotective effect. Carbon tertrachloride (CCL4) was injected into rat subcutaneously with a dose of 3.0 ml/kg to induce experimental acute hepatotoxicity in the animal. The activities of serum glumtamic-oxaloacetic transaminase (SGOT) and serum glutamicpyruvic transaminase (SGPT) were measured after 72 hours of CCL4 administration. The hepatopathological changes of the liver tissue were observed simultaneously with liver enzyme activities determination. The pharmacological effect of B. malabarica and S. rivularis of Taiwan was compared with that of the Bupleurum chinense from mainland China. B malabarica (p < 0.001), S. rivularis (p < 0.001) and B. chinense (p < 0.05) all demonstrated a significant reduction in the CCL4-induced SGOT and SGPT. Pathological studies of these three drugs extracts demonstrated a marked hepato-protective effects on CCL4-induced liver fatty degeneration and cell necrosis. Registry Numbers: EC 2.6.1.1 (Aspartate Aminotransferase) EC 2.6.1.2 (Alanine Aminotransferase) 56-23-5 (Carbon Tetrachloride) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****ANNALS OF THE NEW YORK ACADEMY OF SCIENCES***** Nakamura T Kuriyama M Kosuge E Ishihara K Ito K Effects of saiboku-to (TJ-96) on the production of platelet- activating factor in human neutrophils. In: Ann N Y Acad Sci (1993 Jun 23) 685:572-9 ISSN: 0077-8923 Platelet-activating factor (PAF) has been recognized as an important chemical mediator in allergic and inflammatory reactions. Evidence suggests that PAF is deeply involved in the pathogenesis of bronchial asthma, in which PAF induces profound bronchospasms, increased vascular permeability, and eosinophil/neutrophil accumulation in the respiratory tract. The precise pharmacologic mechanisms of Kampo preparations are still obscure, but extensive experience has established their clinical effectiveness for the treatment of patients with allergic and inflammatory disorders. We tried to examine the effects of Saiboku-to (TJ-96), a Kampo prescription, on in vitro PAF production by human neutrophils because this preparation is widely used for the management of patients with bronchial asthma and bronchitis. Saibokuto inhibited in vitro PAF production in a dose- dependent manner. Among the major natural components of Saiboku-to, saiko (Bupleuri radix) and kanzo (Glycyrrhizae radix) showed inhibitory effects on PAF production, whereas ohgon (Scutellariae radix) had no inhibitory effect. Saikosaponin a and c, purified elements extracted from saiko, showed no inhibitory effects, but saikosaponin d and glycyrrhizin, extracted from kanzo, inhibited PAF production dose-dependently. Further studies are needed to evaluate the clinical significance of Kampo medicines in allergic diseases, but our present results suggest that the pharmacologic benefit of Saiboku-to is partially due to its inhibitory effect on PAF production. Registry Numbers: 1405-86-3 (glycyrrhizic acid) 20874-52-6 (saikosaponin) 471-53-4 (Glycyrrhetinic Acid) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****ANNALES PHARMACEUTIQUES FRANCAISES***** Yang D Michel D Bevalot F Chaumont JP Millet-Clerc J [Antifungal activity in vitro of Scutellaria baicalensis Georgi upon cutaneous and ungual pathogenic fungi] Activite antifongique in vitro de Scutellaria baicalensis Georgi vis- a-vis de champignons pathogenes cutanes et ungueaux. In: Ann Pharm Fr (1995) 53(3):138-41 ISSN: 0003-4509 (Published in French) The root of Scutellaria baicalensis Georgi (Lamiaceae) is one of the traditional drugs commonly used in the Far East. The extracts obtained by the successive exhaustion in chloroform and in ethyl acetat present clear fungistatic activities in vitro against to some cutaneous and ungual pathogenic fungi, and particularly upon strains of Candida albicans, Cryptococcus neoformans and Pityrosporum ovale. For each of these, its minimum inhibitory concentration is determined. The ethyl acetat extract appears the most interesting because of its efficiency and of its stability. An antifungal substance is found out as the baicalein. Registry Numbers: 491-67-8 (baicalein) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****ANTIVIRAL RESEARCH***** Nagai T Moriguchi R Suzuki Y Tomimori T Yamada H Mode of action of the anti-influenza virus activity of plant flavonoid, 5,7,4'-trihydroxy-8-methoxyflavone, from the roots of Scutellaria baicalensis. In: Antiviral Res (1995 Jan) 26(1):11-25 ISSN: 0166-3542 When mouse-adapted influenza virus A/PR/8/34 (A/PR8) (10 PFU/cell) was adsorbed to Madin-Darby canine kidney (MDCK) cells at 4 degrees C for 1 h and incubated at 37 degrees C, release of the virus from the cells was detected in the medium from 4 h after incubation and reached to plateau at 8 h. However, 5,7,4'-trihydroxy-8- methoxyflavone (F36) from the roots of Scutellaria baicalensis significantly reduced this single-cycle replication of A/PR8 from 4 h to 12 h after incubation by dose-dependent manner and the dose which decrease the virus titer one tenth was 11 microM. F36 (50 microM) did not inhibit the adsorption of A/PR8 to MDCK cells, but reduced release of the virus in the medium, when it was added at 0 or 2 h after the incubation. The cell-associated virus determined by sialidase activity was also reduced by F36 treatment at 0 or 2 h. F36 also inhibited the fusion of A/PR8 with liposomes containing bovine brain mixed gangliosides at pH 5.0. However, F36 little affected on the elongation activity of the viral RNA-dependent RNA polymerase in vitro. These results suggest that F36 reduces the replication of A/PR8 by inhibiting the fusion of the virus with endosome/lysosome membrane which occurs at early stage of virus infection cycle. Whereas, when F36 was added to the MDCK cells infected with A/PR8 at 3 or 4 h after incubation, release of the virus in the medium was reduced but the cell-associated virus was increased in comparison with control.(ABSTRACT TRUNCATED AT 250 WORDS) Registry Numbers: EC 3.2.1.18 (Neuraminidase) 57096-02-3 (5,7,4'-trihydroxy-8-methoxyflavone) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Nagai T Miyaichi Y Tomimori T Suzuki Y Yamada H In vivo anti-influenza virus activity of plant flavonoids possessing inhibitory activity for influenza virus sialidase. In: Antiviral Res (1992 Sep) 19(3):207-17 ISSN: 0166-3542 Isoscutellarein (5,7,8,4'-tetrahydroxyflavone) from the leaf of Scutellaria baicalensis non-competitively inhibited (IC50, 20 microM) the hydrolysis of sodium p-nitrophenyl-N-acetyl-alpha-D-neuraminate by influenza virus sialidase with an apparent Ki value of 41 microM. Negligible inhibitory activity was observed for mouse liver sialidase at a concentration of 79 microM. Isoscutellarein also inhibited the replication of influenza virus A/WSN/33 in Madin-Darby bovine kidney cells with 50% virus inhibitory dose at 16 nmol/well and influenza virus A/PR/8/34 in the allantoic sac of embryonated egg with little toxic effects. The flavone showed significant anti-influenza virus activity in vitro similar to isoscutellarein-8-methylether (F36) (Nagai, T., Miyaichi, Y., Tomimori, T., Suzuki, Y. and Yamada H., 1990, Chem. Pharm. Bull. 38, 1329-1332), and more potent virucidal activity in ovo than F36. However, F36 completely prevented proliferation of mouse-adapted influenza virus A/PR/8/34 in mouse lung by the intranasal (0.5 mg/kg) and intraperitoneal (4 mg/kg) administrations, and it was more potent than the known anti-influenza virus substance, amantadine. Intranasal administration of F36 (0.5 mg/kg) also protected mice against a lethal influenza virus A/PR/8/34 infection. Isoscutellarein significantly inhibited lung virus proliferation when administered intranasally or orally to mice. F36 and isoscutellarein showed negligible toxic effect against mice. These results suggested that flavones, which have potent influenza virus sialidase inhibitory activity, have anti-influenza virus activity in vivo. Registry Numbers: EC 3.2.1.18 (Neuraminidase) 82014-23-1 (isoscutellarein 6-galactoside) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS***** Chen S Hwang J Deng PS Inhibition of NAD(P)H:quinone acceptor oxidoreductase by flavones: a structure-activity study. In: Arch Biochem Biophys (1993 Apr) 302(1):72-7 ISSN: 0003-9861 A structure-activity study was carried out to determine the important regions of baicalein and oroxylin A, two flavones isolated from the Chinese herb Scutellariae radix, in inhibiting NAD(P)H:quinone acceptor oxidoreductase (EC 1.6.99.2; DT-diaphorase). This quinone reductase is a vitamin K reductase. It is a target for and has been used as a model enzyme to investigate the mode of action of oral anticoagulants. The two flavones were found to inhibit this quinone reductase in nanomolar ranges. The 5-hydroxyl, 7-hydroxyl, 8- hydroxyl, and 2-phenyl groups of these flavones were found to be important for their inhibition of the enzyme. The inhibition profiles of the flavones on the NADH-menadione reductase activity, the NADH- potassium ferricyanide reductase activity, and the NADH-methyl red reductase activity of this enzyme were different. Therefore, even though the flavones were found to be competitive inhibitors with respect to NADH, they probably did not inhibit the enzyme by binding to the nicotinamide nucleotide binding site. Inhibition kinetic studies which indicated that these compounds bound to different sites than those for dicoumarol and phenindone were performed. These results indicate that these flavones are a new type of inhibitor of NAD(P)H:quinone acceptor oxidoreductase and potentially useful as anticoagulant drugs. Registry Numbers: EC 1.6.99.2 (NAD(P)H Dehydrogenase (Quinone)) 12001-79-5 (Vitamin K) 13746-66-2 (potassium ferricyanide) 146-14-5 (FAD) 480-11-5 (oroxylin A) 491-67-8 (baicalein) 493-52-7 (methyl red) 53-59-8 (NADP) 53-84-9 (NAD) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS***** Nagai T Miyaichi Y Tomimori T Yamada H Inhibition of mouse liver sialidase by plant flavonoids. In: Biochem Biophys Res Commun (1989 Aug 30) 163(1):25-31 ISSN: 0006-291X Flavonoids (103 species) were tested for inhibitory activity against mouse liver sialidase using sodium p-nitrophenyl-N-acetyl-alpha-D- neuraminate (PNP-NeuAc) as substrate. Isoscutellarein-8-O-glucuronide from the leaf of Scutellaria baicalensis showed most potent activity (IC50, 40 microM), and this flavone appeared to be a non-competitive inhibitor of the enzyme. This flavone inhibited the lysosomal solubilized sialidase against PNP-NeuAc and sialyllactose effectively, but not microsomal enzyme against gangliosides and colominic acid, whereas, negligible or weak inhibitory activities were observed for influenza virus sialidase, beta-galactosidase, alpha-mannosidase, and alpha-glucosidase tested. These results indicate that this flavone may be useful to elucidate the function of the lysosomal solubilized sialidase. Registry Numbers: EC 3.2.1.18 (Neuraminidase) 487-26-3 (flavanone) 94-41-7 (Chalcone) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****BIOLOGICAL AND PHARMACEUTICAL BULLETIN***** Yamaoka Y Kawakita T Kaneko M Nomoto K A polysaccharide fraction of Zizyphi fructus in augmenting natural killer activity by oral administration. In: Biol Pharm Bull (1996 Jul) 19(7):936-9 ISSN: 0918-6158 Shosaiko-to (Xiao-chai-hu-tang, SHO), a Kampo medicine, was prepared by decocting a prescription of 7 kinds of crude drugs, namely Bupleuri Radix, Pinelliae Tuber, Scutellariae Radix, Zizyphi Fructus, Ginseng Radix, Glycyrrhizae Radix and Zingiberis Rhizoma. Previously, we reported that the effect of the orally administered SHO in augmenting natural killer (NK) activity in the peripheral blood was attributed to the acidic polysaccharide fraction. To characterize the active components in the crude materials in SHO, the effects of extracts and various fractions were investigated by oral administration. The extracts of Zizyphi Fructus, Zingiberis Rhizoma, Scutellariae Radix, Glycyrrhizae Radix and Pinelliae Tuber augmented NK activity by oral administration. The high weight molecular fraction of Zizyphi Fructus was the most effective in augmenting NK activity. Thus, we obtained an active polysaccharide fraction from the high weight molecular fraction of Zizyphi Fructus. This polysaccharide fraction with a high molecular weight of approximately 43,000 contained 54.7% carbohydrate, 61.8% uronic acid and 20.9% protein. The sugar moiety was composed of rhamnose, arabinose, xylose, fucose, mannose, galactose, glucose and galacturonic acid in molar ratios of 28:59:11:9:7:32:20:100. Registry Numbers: 63364-01-2 (saiko-keishi-to) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Nagai T Suzuki Y Tomimori T Yamada H Antiviral activity of plant flavonoid, 5,7,4'-trihydroxy-8- methoxyflavone, from the roots of Scutellaria baicalensis against influenza A (H3N2) and B viruses. In: Biol Pharm Bull (1995 Feb) 18(2):295-9 ISSN: 0918-6158 We investigated effects of isoscutellarein-8-methylether (5,7,4'- trihydroxy-8-methoxyflavone, F36) from the roots of Scutellaria baicalensis on the single-cycle replication of mouse-adapted influenza viruses A/Guizhou/54/89 (H3N2 subtype) and B/Ibaraki/2/85 in Madin-Darby canine kidney (MDCK) cells. The agent suppressed replication of these viruses from 6 to 12 h after incubation in a dose-dependent manner by 50% at 20 microM and 90% at 40 microM, respectively. F36 (50 microM) reduced the release of B/Ibaraki virus in the medium by 90-93% when it was added to the MDCK cells at 0 to 4 h after incubation. The cell-associated virus determined by sialidase activity was also reduced by the treatment at 0 to 4 h. F36 (120 microM) inhibited the low pH-dependent membrane fusion of both the viruses with the liposome containing mixed gangliosides from bovine brain. However, the agent little affected the hemagglutination and RNA-dependent RNA polymerase activities of these viruses in vitro. These results suggest that F36 inhibits the replication of A/Guizhou and B/Ibaraki viruses at least partly by inhibiting the fusion of viral envelopes with the endosome/lysosome membrane which occurs at the early stage of the virus infection cycle. F36 (0.5 mg/kg) showed no antiviral activity against A/Guizhou and B/Ibaraki viruses in mice when administered intranasally 5 min prior to virus inoculation, whereas it significantly inhibited their proliferation in the mouse lung when administered intranasally 7 times (total 3.5 mg/kg) from 18 h before to 54 h after virus infection. Registry Numbers: EC 2.7.7.48 (RNA Replicase) 57096-02-3 (5,7,4'-trihydroxy-8-methoxyflavone) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Ikegami F Matsunae K Hisamitsu M Kurihara T Yamamoto T Murakoshi I Purification and properties of a plant beta-D-glucuronidase form Scutellaria root. In: Biol Pharm Bull (1995 Nov) 18(11):1531-4 ISSN: 0918-6158 beta-D-Glucuronidase (baicalinase, GUS [EC 3.2.1.31]) activity in the crude drug, Scutellaria root, was assayed in line with the quality control standards of Kampo (Japanese Herbal) medicines. GUS was purified to homogeneity in the purification steps including DEAE- Sepharose Fast Flow and chromatofocusing used PBETM94 and Polybuffer 74. These results suggest that the Scutellaria GUS is composed of 55kDa active subunits and that the isoelectric point of this enzyme is pH 5.4. Optimal catalytic activity was found at pH 4.7 in the pH range 3.6--6.2 in 50 mM Na-citrate buffer. The purified enzyme hydrolyzed baicalin and wogonin glucuronide, but did not hydrolyze glycyrrhizin or some beta-glucosides found in other crude drugs. GUS activity in several crude drugs is also described. Registry Numbers: EC 3.2.1.31 (Glucuronidase) 21967-41-9 (baicalin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Saracoglu I Inoue M Calis I Ogihara Y Studies on constituents with cytotoxic and cytostatic activity of two Turkish medicinal plants Phlomis armeniaca and Scutellaria salviifolia. In: Biol Pharm Bull (1995 Oct) 18(10):1396-400 ISSN: 0918-6158 Ten known glycosidic compounds, betulalbuside A (1), 8- hydroxylinaloyl,3-O-beta-D-glucopyranoside (2) (monoterpen glycosides), ipolamide (3) (iridoid glycoside), acteoside (verbascoside) (4), leucosceptoside A (5), martynoside (6), forsythoside B (7), phlinoside B (8), phlinoside C (9), and teuerioside (10) (phenylpropanoid glycosides) were isolated from methanolic extracts of Phlomis armeniaca and Scutellaria salviifolia (Labiatae). Structure elucidations were carried out using 1H-, 13C- NMR and FAB-MS spectra, as well as chemical evidence. The cytotoxic and cytostatic activities of isolated compounds were investigated by the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) method. Among the glycosides obtained here, caffeic acid- containing phenylpropanoid (or phenethyl alcohol, or phenylethanoid) glycosides were found to show activity against several kinds of cancer cells. However, they didn't affect the growth and viability of primary-cultured rat hepatocytes. Study of the structure-activity relationship indicated that ortho-dihydroxy aromatic systems of phenylpropanoid glycosides are necessary for their cytotoxic and cytostatic activities. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****BIULLETEN EKSPERIMENTALNOI BIOLOGII I MEDITSINY***** Udintsev SN Krylova SG Konovalova ON [Correction by natural adaptogens of hormonal-metabolic status disorders in rats during the development of adaptation syndrome using functional tests with dexamethasone and ACTH] Korrektsiia adaptogenami prirodnogo proiskhozhdeniia narushenii gormonal'no-metabolicheskogo statusa organizma krys v protsesse razvitiia adaptatsionnogo sindroma pri provedenii funktsional'nykh prob s deksametazonom i AKTG. In: Biull Eksp Biol Med (1991 Dec) 112(12):599-601 ISSN: 0365-9615 (Published in Russian) Rats exposed to stress by fixation develop a complex of hormonal metabolic homeostasis disturbances (as evidenced by changed levels of ACTH, insulin, 11-HOCS, urea, glucose). One of the major mechanisms of these disorders in reduced hypothalamus sensitivity to regulatory signals and exhausted adrenocortical functional activity, developing at the stages of anxiety and exhaustion of the adaptation syndrome, respectively, and detectable by functional tests with dexamethasone and ACTH. Administration of natural adaptogens (Scutellaria baicalensis extract and its active principle, baikalin flavonoid) was conducive to normalization of the majority of the examined parameters whatever the direction of changes. Registry Numbers: 21967-41-9 (baicalin) 50-02-2 (Dexamethasone) 9002-60-2 (Corticotropin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CANCER LETTERS***** Wong BY Lau BH Teel RW Chinese medicinal herbs modulate mutagenesis, DNA binding and metabolism of benzo[a]pyrene 7,8-dihydrodiol and benzo[a]pyrene 7,8- dihydrodiol-9,10-epoxide. In: Cancer Lett (1992 Feb 29) 62(2):123-31 ISSN: 0304-3835 Oldenlandia diffusa(OD) and Scutellaria barbata (SB) have been used in traditional Chinese medicine for treating liver, lung and rectal tumors. In this study, the effects of aqueous extracts of these two herbs on benzo[a]pyrene 7,8-dihydrodiol. (BaP 7,8-DHD) and benzo[a]pyrene 7,8-dihydrodiol-9,10-epoxide (BPDE)-induced mutagenesis using Salmonella typhimurium TA100 as the bacterial tester strain and rat liver 9000 x g supernatant (S9) as the metabolic activation system were assessed. We also determined the effects of these two herbs on BaP 7,8-DHD and BPDE binding to calf thymus DNA. Organosoluble metabolites of BaP 7,8-DHD and water- soluble conjugates of BaP 7,8-DHD and BPDE were analyzed by high- performance liquid chromatography (HPLC) and alumina column liquid chromatography. Mutagenesis assays revealed that these two herbs produced a significant concentration-dependent inhibition of histidine-independent (His+) revertants induced by BaP 7,8-DHD and BPDE. OD and SB also inhibited BPDE-induced mutagenesis in a concentration-dependent manner in the absence of S9. SB had a greater inhibitory effect than OD. SB significantly inhibited BaP 7,8-DHD and BPDE binding to DNA while OD significantly enhanced DNA binding of both compounds. OD and SB inhibited the formation of organosoluble metabolites of BaP 7,8-DHD and decreased the formation of water- soluble conjugates of BaP 7,8-DHD and BPDE. However, the fraction of the total radioactivity in the water-soluble conjugates present as sulfate and glutathione was increased by OD and SB. Glucuronide fraction was decreased. The results of this study affirm our previous work suggesting that these two Chinese medicinal herbs possess antimutagenic properties and further suggest that they act as blocking agents through a scavenging mechanism. Registry Numbers: 13345-25-0 (benzo(a)pyrene 7,8-dihydrodiol) 55097-80-8 (7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10- oxide) 9007-49-2 (DNA) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Wong BY Lau BH Yamasaki T Teel RW Modulation of cytochrome P-450IA1-mediated mutagenicity, DNA binding and metabolism of benzo[a]pyrene by Chinese medicinal herbs. In: Cancer Lett (1993 Jan 15) 68(1):75-82 ISSN: 0304-3835 Oldenlandia diffusa (OD) and Scutellaria barbata (SB) have been used in traditional Chinese medicine for treating liver, lung and rectal tumors. We previously showed that they inhibited mutagenesis, DNA binding and metabolism of benzo[a]pyrene (BaP) and aflatoxin B1 (AFB1) bioactivated by Aroclor 1254-induced rat hepatic S9. The purpose of this study was to investigate the effects of OD and SB on the cytochrome P-450IA1-mediated mutagenicity of BaP in Salmonella typhimurium TA100 using beta-naphthoflavone (beta NF)-induced rat hepatic S9. We also determined the effects of OD and SB on cytochrome P-450IA1-linked ethoxyresorufin O-deethylase (EROD) activity in beta NF-induced hepatic microsomes. In addition, we studied the effects of these two herbs on BaP metabolite binding to calf thymus DNA and using high performance liquid chromatography (HPLC) we investigated the effects of OD and SB on the metabolism of BaP by beta NF-induced S9. Our experimental results showed that OD and SB inhibited the mutagenicity of BaP in the presence of either non-induced or beta NF- induced S9. SB significantly inhibited BaP binding to DNA. These effects correlated with the inhibition of cytochrome P-450IA1-linked EROD activity in beta NF-induced microsomes and with an inhibition of beta NF-induced S9 mediated metabolism of [3H]BaP as determined by HPLC. These results suggest that OD and SB may possess antimutagenic activity by inhibiting P-450IA-mediated metabolism of BaP. Registry Numbers: EC 1. (Oxidoreductases) EC 1.- (Cytochrome P-450 CYP1A1) 50-32-8 (Benzo(a)pyrene) 9007-49-2 (DNA) 9035-51-2 (Cytochrome P-450) EC 1.- (ethoxyresorufin O-deethylase) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CELLULAR AND MOLECULAR BIOLOGY RESEARCH***** Li BQ Fu T Yan YD Baylor NW Ruscetti FW Kung HF Inhibition of HIV infection by baicalin--a flavonoid compound purified from Chinese herbal medicine. In: Cell Mol Biol Res (1993) 39(2):119-24 ISSN: 0968-8773 Baicalin (BA), (formulated as 7-D-glucuronic acid-5,6-dihydroxy- flavone), was purified from the plant Scutellaria Baicalensis Georgi. It has been used as a traditional Chinese herbal medicine. The inhibitory effect of BA against human immunodeficiency virus (HIV-1) infection and replication has been studied in vitro. The compound inhibits HIV-1 infection and replication as measured by: (1) a quantitative focal syncytium formation on CEM-ss monolayer cells; and (2) HIV-1 specific core antigen p24 expression and retroviral reverse transcriptase (RT) activity in the HIV-1-infected H9 cells. We have further demonstrated that the enzymatic activity of purified recombinant HIV-1/RT was inhibited by BA. In addition to lymphoid cell lines, the anti-HIV-1 activity of BA was also observed in cultures of primary human peripheral blood mononuclear cells infected with HIV-1 in vitro. Neither cytotoxic nor cytostatic effects on the indicator cells were found under the assay condition. This data suggests that BA may serve as a useful drug for the treatment and prevention of HIV infections. Registry Numbers: EC 2.7.7.- (HIV-1 Reverse Transcriptase) EC 2.7.7.49 (RNA-Directed DNA Polymerase) 21967-41-9 (baicalin) EC 2.7.7.- (HIV-1 reverse transcriptase) EC 2.7.7.49 (Reverse Transcriptase) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CESKOSLOVENSKA FARMACIE***** Hubik J Spilkova J [Herbal drugs in Kampo preparations] Rostlinne drogy v Kampo pripravcich. In: Cesk Farm (1993 Apr) 42(2):65-7 ISSN: 0009-0530 (Published in Czech) Medicaments of the Kampo medicine are composed from vegetable drugs. This article describes drugs unknown in European medicine and used in Kampo preparations--Radix bupleuri, Tuber pinelliae, Hoelen, Radix scutellariae, Cortex magnoliae, Fructus zizyphi, Herba perillae, Radix paeoniae, Rhizoma atractylodis, Rhizoma alismatis, Radix alismae, Rhizoma cnidii, Radix angelicae, Rhizoma coptidis, Fructus gardeniae, Cortex phellodendri, Polyporus, Radix ginseng. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CHEMICAL AND PHARMACEUTICAL BULLETIN***** Konoshima T Kokumai M Kozuka M Iinuma M Mizuno M Tanaka T Tokuda H Nishino H Iwashima A Studies on inhibitors of skin tumor promotion. XI. Inhibitory effects of flavonoids from Scutellaria baicalensis on Epstein-Barr virus activation and their anti-tumor-promoting activities. In: Chem Pharm Bull (Tokyo) (1992 Feb) 40(2):531-3 ISSN: 0009-2363 To search for possible anti-tumor-promoters, fourteen flavones obtained from the root of Scutellaria baicalensis were examined for their inhibitory effects on the Epstein-Barr virus early antigen (EBV- EA) activation by a short-term in vitro assay. Among these flavones, 5,7,2'-trihydroxy- and 5,7,2',3'-tetrahydroxyflavone showed remarkable inhibitory effects on the EBV-EA activation, and the effect of the latter on Raji cell cycle was also examined by flow cytometer. These two flavones exhibited remarkable inhibitory effects on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. Registry Numbers: 73046-40-9 (5,7,2'-trihydroxyflavone) 74805-70-2 (5,7,2',3'-tetrahydroxyflavone) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Nagai T Miyaichi Y Tomimori T Suzuki Y Yamada H Inhibition of influenza virus sialidase and anti-influenza virus activity by plant flavonoids. In: Chem Pharm Bull (Tokyo) (1990 May) 38(5):1329-32 ISSN: 0009-2363 Flavonoids (103 species) were tested for inhibitory activity against influenza virus sialidase using sodium p-nitrophenyl-N-acetyl-alpha-D- neuraminate as substrate. 5,7,4'-Trihydroxy-8-methoxyflavone from the root of Scutellaria baicalensis showed the most potent activity (IC50, 55 microM), and this flavone appeared to be a non-competitive inhibitor of the enzyme. Whereas, negligible or weak inhibitory activities were observed for mouse liver sialidase, beta- galactosidase and alpha-mannosidase as tested. This flavone also inhibited the infection by influenza virus A/PR/8/34 of Madin-Darby canine kidney cells, and replication of the virus in the allantoic sack of embryonated egg. These results suggest that flavone, which has potent influenza virus sialidase inhibitory activity, may have anti-influenza virus activity Registry Numbers: EC 3.2.1.18 (Neuraminidase) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Abe K Inoue O Yumioka E Biliary excretion of metabolites of baicalin and baicalein in rats. In: Chem Pharm Bull (Tokyo) (1990 Jan) 38(1):209-11 ISSN: 0009-2363 Biliary excretion of metabolites of baicalin, present in Scutellariae Radix, was investigated using rats. The bile of rats administered baicalin orally was shown to contain five major metabolites, which were identified as baicalein 6-O-beta-glucopyranuronoside (M1), 6-O- methyl-baicalein 7-O-beta-glucopyranuronoside (oroxylin A 7-O-beta- glucuronide (M2], baicalein 7-O-beta-glucopyranuronoside (M3), 6-O- beta-glucopyranuronosyl- baicalein 7-O-sulfate (M4), and baicalein 6,7-di-O-beta-glucopyranuronoside (M5) on the basis of chemical and spectroscopic evidence. The bile of rats treated with baicalein also contained the above metabolites. Slower biliary excretion of the metabolites after baicalin administration suggested that it was absorbed as baicalein after hydrolysis in the gastrointestinal tract. The total cumulative amounts of the five metabolites excreted in the bile during 30 h after oral administration of baicalin and that of baicalein were approximately 54% and 40% of the doses, respectively. In addition the bilary metabolites of both drugs were shown to be mainly composed of M5 and M4, which have high polarity and large molecular weight. Registry Numbers: 21967-41-9 (baicalin) 491-67-8 (baicalein) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Nikaido T Ohmoto T Kinoshita T Sankawa U Delle Monache F Botta B Tomimori T Miyaichi Y Shirataki Y Yokoe I et al Inhibition of adenosine 3',5'-cyclic monophosphate phosphodiesterase by flavonoids. III. In: Chem Pharm Bull (Tokyo) (1989 May) 37(5):1392-5 ISSN: 0009-2363 Sixty-one flavanones, twenty-six isoflavones and eight other flavonoids, obtained from Sophora tomentosa, S. flavescens, Scutellaria baicalensis and other medicinal plants or synthesized, were tested for their inhibitory activity against adenosine 3',5'- cyclic monophosphate (cAMP) phosphodiesterase from beef heart. The structure-activity relationships were investigated. Registry Numbers: EC 3.1.4.17 (3',5'-Cyclic-Nucleotide Phosphodiesterase) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Iinuma M Tanaka T Mizuno M Katsuzaki T Ogawa H Structure-activity correlation of flavonoids for inhibition of bovine lens aldose reductase. In: Chem Pharm Bull (Tokyo) (1989 Jul) 37(7):1813-5 ISSN: 0009-2363 To clarify the structure-activity correlation of flavonoids for inhibition of aldose reductase, about fifty flavonoid compounds were screened. The presence of hydrophobic substituents on the A ring and hydrophilic substituents on the B ring of the flavonoid skeleton was suggested to improve the potency of inhibitory activity. The activities of extracts of Scutellaria baicalensis, Andrographis paniculata and Gutierrezia microcephala are also described. Registry Numbers: EC 1.1. (Sugar Alcohol Dehydrogenases) EC 1.1.1.21 (Aldehyde Reductase) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ ***CHUNG HSI I CHIEH HO TSA CHIH CHINESE JOURNAL OF MODERN DEVELOPMENTS*** Zhang H Huang J [Preliminary study of traditional Chinese medicine treatment of minimal brain dysfunction: analysis of 100 cases] In: Chung Hsi I Chieh Ho Tsa Chih (1990 May) 10(5):278-9, 260 ISSN: 0254-9034 (Published in Chinese) This paper reports the clinical treatment of 100 patients with minimal brain dysfunction (MBD), their age ranged from 7-14.2 years, and the average age was 10.5. Patients were divided into TCM and WM group randomly. The TCM group (80 cases) were treated with the therapy of subdueing hyperactivity of the Liver and invigorating the function of the Spleen by using: Bupleurum chinense, Scutellaria baicalensis, Astragalus membranaceus, Codonopsis pilosula, Ligustrum lucidum, Lophatherum gracile and thread of ivory. The WM group (20 cases) were treated with retalin 5-15 mg twice daily. One course of treatment lasted one month, and effects were evaluated after 1-3 courses of treatment. The results were as follows: In the TCM group, 23 cases were cured (clinical symptom and sign disappeared, 10 IQ units were raised in their intelligence, abnormal electroencephalogram was recovered and there was no recurrence during the first six months after recovery). 46 cases were improved (clinical symptom and sign markedly improved, 4 IQ units raised in intelligence and electroencephalogram improved), and 11 cases ineffective. The effective rate was 86.25%. In the WM group, 6 cases were cured, 12 cases improved and 2 cases ineffective, the clinical effective rate being 90.0%. There was no significant difference between the two groups in this study, but, the side-effects of the TCM group was less than the WM group, and the TCM group had more beneficial effects to improve intelligence, enuresis and the black of orbits. The study showed that the Verbal Scale in Wechsler Intelligence Scale for children is one of the indications of diagnosis and evaluating of the curative effect of MBD. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CHUNG-KUO CHUNG HSI I CHIEH HO TSA CHIH***** Huang WM Yan J Xu J [Clinical and experimental study on inhibitory effect of sanhuang mixture on platelet aggregation] In: Chung Kuo Chung Hsi I Chieh Ho Tsa Chih (1995 Aug) 15(8):465-7 ISSN: 1003-5370 (Published in Chinese) Sanhuang mixture (Xinmai capsule) is composed of Astragalus membranaceus, Coptis chinensis and Scutellaria baicalensis. It could inhibit platelet aggregation (PAG) induced by ADP in rats or by ADP and ADR in vivo. Patients with high PAG took Xinmai capsule for 4 weeks, the effective rate was 88.7%, which was same as the efficacy of aspirin 50 mg/day. In Syndrome Differentiation of TCM, the effective rate was the highest (92.3%) in the Syndrome of Qi Deficiency-Blood Stasis, and the lowest (72.7%) in the Syndrome of Stasis Phlegm and combined together. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *CHUNG-KUO CHUNG YAO TSA CHIH CHINA JOURNAL OF CHINESE MATERIA MEDICA* Su W [Application of cluster analysis to the classification of Radix scutellariae] In: Chung Kuo Chung Yao Tsa Chih (1991 Oct) 16(10):579-81, 638 ISSN: 1001-5302 (Published in Chinese) Ten samples of Radix Scutellariae from different habitats were analyzed by thin layer chromatography. From the analysis numerical characteristic features were obtained that represent the quality difference of samples. All of the multivariate data were treated with mathematic method of cluster analysis. Scutellaria bai alensis included in Chinese Pharmacopoeia was clearly differentiated from the other four varieties of herbs (S. rehderiana, S. viscidula, S. amoena, S. likiangensis). €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Huang L Liu J Li D Wang Z Ye W Cai B Liu M Li M [A study on components and compound prescription of huangqin decoction] In: Chung Kuo Chung Yao Tsa Chih (1991 Mar) 16(3):177-81, back cover ISSN: 1001-5302 (Published in Chinese) The results obtained from the pharmacological experiments have preliminarily demonstrated that the compound prescription is better than its individual component drug in the range and potency of pharmacological activities. In the prescription Radix Scutellariae plays a principal role in pharmacological effects. Radix Scutellariae and Radix Paeoniae Alba can potentiate each other. Radix Glycyrrhizae and Fructus Jujubae in the compound prescription also exhibit biological activities to some extent. The relieving effect of the prescription for spasm and pain may result from the synergistic interaction between Radix Paeoniae Alba and Radix Glycyrrhiza, and the heat clearing and diarrhea stopping action is due to the biological activity of Radix Scutellariae. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Huang L Ye W Cai B Li D Liu J Liu M [A preliminary study on the pharmacology of the compound prescription huangqin tang and its component drugs] In: Chung Kuo Chung Yao Tsa Chih (1990 Feb) 15(2):115-7, 128 ISSN: 1001-5302 (Published in Chinese) Results obtained from the pharmacological experiments demonstrated that the compound prescription Huangqin Tang and its component drugs, roots of Paeonia lactiflora, Scutellaria baicalensis and Glycyrrhiza uralensis, and the fruit of Ziziphus jujuba showed marked anti- inflammatory effect. The compound prescription and its component drugs, except the peony root, possessed significant antispastic effect. Antipyretic effect of Radix Scutellariae, Radix Glycyrrhizae and Huangqin Tang was suggested. Huangqin Tang, Radix Paeoniae alba, and Radix Glycyrrhizae showed marked analgesic effect. In addition, the experiments confirmed that both Huangqin Tang and single Radix Scutellariae have sedative effect. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Chen F Guo Y Meng X Zhang S [Identification of chaihu guizhi ganjiang decoction by three dimensional HPLC] In: Chung Kuo Chung Yao Tsa Chih (1995 Apr) 20(4):223-4, 253 ISSN: 1001-5302 (Published in Chinese) The Chaihu Guizhi Ganjiang Decoction was identified by three dimensional HPLC. The result showed that the constituents in this decoction, namely Radix Bupleuri; Ramulus Cinnamomi; Radix Glycyrrhizae and Radix Scutellariae could all be identified clearly. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Guo XW Zhang FC Lin SY [Effect of ultrasonic extracting on the extraction rate of baicalin] In: Chung Kuo Chung Yao Tsa Chih (1994 Jun) 19(6):348-9, 383 ISSN: 1001-5302 (Published in Chinese) The method of extracting baicalin from Scutellaria baicalensis by ultrasound is studied. Compared with that of the decocting process which is usually used in medical industry, the method does not need to heat the medicine and can reduce the extraction time and raise the extraction rate. Registry Numbers: 21967-41-9 (baicalin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Wang JZ Chen DY Su YY [Analytical study on processing of Scutellaria baicalensis Georyl by HPLC] In: Chung Kuo Chung Yao Tsa Chih (1994 Jun) 19(6):340-1, 383 ISSN: 1001-5302 (Published in Chinese) This paper deal with the effect of processing on Scutellaria baicalensis. A HPLC method for the determination of baicalin in the drug processed in four different ways has been established. The method is simple, specific and accurate. The recovery is 99.5% and relative standard deviation 0.99%. Registry Numbers: 21967-41-9 (baicalin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Li S Su SX Huang RL [A report of fertilizer-spreading experiment of Scutellaria baicalensis Georgi] In: Chung Kuo Chung Yao Tsa Chih (1993 Mar) 18(3):142-5, 190 ISSN: 1001-5302 (Published in Chinese) The result shows that all the three kinds of fertilizers nitrogen, phosphorus and potassium can markedly raise the production of Scutellaria baicalensis. Both single spreading and mixed spreading help to enhance the yield, but mixed spreading gives higher yield--an increase of 26% over the non-spreading. Registry Numbers: 7440-09-7 (Potassium) 7723-14-0 (Phosphorus) 7727-37-9 (Nitrogen) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Han GR Wang YD Feng L Liu ZQ Zhang HB [Quality standards for qingwei huanglian pills] In: Chung Kuo Chung Yao Tsa Chih (1993 Feb) 18(2):93-5, 126 ISSN: 1001-5302 (Published in Chinese) In the paper systematic studies on quality standards for Qingwei Huanglian Pills are reported, along with the TLC identification of Gardenia jasminoides, Scutellaria baicalensis and Anemarrhena asphodeloides and the quantitative determination of berberine in Coptis chinensis and Phellodendron chinese by TLC densitometric method. To simplify the operation, the same solvent was used for both the identification and determination. The quantitative method is simple, sensitive, reproducible and accurate. The recovery of berberine is 99.48%. The coefficient of variation is 1.42%. Registry Numbers: 2086-83-1 (Berberine) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****DEVELOPMENTAL PHARMACOLOGY AND THERAPEUTICS***** Yin J Wennberg RP Miller M Induction of hepatic bilirubin and drug metabolizing enzymes by individual herbs present in the traditional Chinese medicine, yin zhi huang. In: Dev Pharmacol Ther (1993) 20(3-4):186-94 ISSN: 0379-8305 Yin Zhi Huang (YZH) is a decoction of four plants which is widely used in Asia to treat neonatal jaundice. This study compares the ability of phenobarbital and the individual herbs comprising YZH, Artemisia, Gardenia, Rheum, and Scutellaria baicalensis, to induce hepatic drug and bilirubin metabolizing enzymes in rats. Herbal decoctions (30 ml/kg/day) or phenobarbital (60 mg/kg/day) were administered for 5 days. Only phenobarbital increased cytochrome P- 450 levels whereas Gardenia slightly decreased levels. Artemisia, Rheum and phenobarbital increased bilirubin glucuronyl transferase activity. Glucuronidation of alpha-naphthol was increased by Gardenia and phenobarbital, whereas Artemisia and Rheum were ineffective inducers. Phenobarbital was the most effective inducer of glutathione- S-transferase (GSHT) activity. Phenobarbital and Gardenia both induced delta 5-3-ketosteroid isomerase activity, a marker for the Ya subunit of GSHT responsible for intracellular bilirubin transport in liver. The selective patterns of enzyme induction suggest potential value for using specific plant decoctions to modify drug and bilirubin metabolic pathways. Registry Numbers: EC 1.11.1.9 (Glutathione Peroxidase) EC 1.13.12. (Mixed Function Oxidases) EC 2.4.1.17 (Glucuronosyltransferase) EC 2.5.1.18 (Glutathione Transferases) EC 5.3.3.- (Steroid Isomerases) EC 5.3.3.1 (steroid delta-isomerase) 50-06-6 (Phenobarbital) 635-65-4 (Bilirubin) 9035-51-2 (Cytochrome P-450) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****DISS ABSTR INT [B]***** Wong BY Modulation of rat hepatic S9-dependent mutagenesis, DNA binding, and metabolism of aflatoxin B(1) and benzo(a)pyrene by four Chinese medicinal herbs. In: Diss Abstr Int [B] (1992) 53(6):2676 ISSN: 0419-4217 Extracts of the herbs Oldenlandia diffusa (OD) and Scutellaria barbata (SB) have been used in traditional Chinese medicine for treating liver, lung and rectal tumors while extracts of Astragalus membranaceus and Ligustrum lucidum (LL) are often used as adjuncts in cancer therapy. In this study, we determined the effects of aqueous extracts of these four herbs on aflatoxin B1 (AFB1), benzo(a)pyrene (BaP), benzo(a)pyrene 7,8-dihydrodiol (BaP 7,8-DHD) and benzo(a)pyrene 7,8-dihydrodiol-9,10-epoxide (BPDE)-induced mutagenesis, mediated by enzymes in rat hepatic 9000 x g supernatant (S9), in Salmonella typhimurium TA100. We also studied the effects of these four herbs on AFB1 and BaP binding to calf thymus DNA and the effects of OD and SB on BaP 7,8-DHD and BPDE binding to calf thymus DNA. After incubation with rat hepatic S9, organosoluble metabolites of AFB1, BaP, and BaP 7,8-DHD were analyzed by reverse-phase high- performance liquid chromatography (HPLC), and water-soluble conjugates of BaP, BaP 7,8-DHD and BPDE were analyzed by alumina column liquid chromatography. Water-soluble conjugates of AFB were determined by passing through C18-Sep-pak cartridge and analyzed by HPLC. Mutagenesis assays showed that aqueous extracts of the herbs that we tested produced a concentration-dependent inhibition of histidine-independent revertant colonies induced by AFB1, BaP, BaP 7,8-DHD, and BPDE. LL, OD, and SB inhibited AFB1 metabolite binding to calf thymus DNA, formation of AFB1-DNA adducts and metabolism of AFB1. These three herbs also inhibited the binding of BaP metabolites to calf thymus DNA. LL and SB decreased BaP-DNA adduct formation, and SB inhibited the metabolism of BaP. OD and SB significantly inhibited the metabolism of BaP 7,8-DHD and the formation of water-soluble conjugates of BaP 7,8-DHD and BPDE. Both OD and SB modified the distribution of conjugates within the water-soluble fraction. SB inhibited BaP 7,8-DHD and BPDE binding to DNA and decreased the formation of adducts. Our results therefore suggest that the Chinese medicinal herbs LL, OD and SB possess antimutagenic and anticarcinogenic properties. OD and SB may possess these properties because they are able to scavenge the reactive metabolites and thus prevent their interaction with DNA. (Full text available from University Microfilms International, Ann Arbor, MI, as Order No. AAD92-33338.) Registry Numbers: 1162-65-8 (Aflatoxin B1) 50-32-8 (Benzo(a)pyrene) 9007-49-2 (DNA) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****EUROPEAN JOURNAL OF CANCER PREVENTION***** Wong BY Lau BH Yamasaki T Teel RW Inhibition of dexamethasone-induced cytochrome P450-mediated mutagenicity and metabolism of aflatoxin B1 by Chinese medicinal herbs. In: Eur J Cancer Prev (1993 Jul) 2(4):351-6 ISSN: 0959-8278 Oldenlandia diffusa (OD) and Scutellaria barbata (SB) have been used in traditional Chinese medicine for treating liver, lung and rectal tumours. We previously showed that they inhibited mutagenesis, DNA binding and metabolism of aflatoxin B1 (AFB1) and benzo(a)pyrene (BaP) bioactivated by Aroclor 1254-induced rat S9. The purpose of this study was to investigate the effects of OD and SB on the mutagenicity of AFB1 in Salmonella typhimurium TA100 using dexamethasone (DXM)-induced rat hepatic S9, on cytochrome P450-linked aminopyrine N-demethylase (APND) activity in DXM-induced hepatic microsomes and on the metabolism of AFB1 by DXM-induced S9 using high- performance liquid chromatography (HPLC). The experimental results showed that OD and SB consistently inhibited the mutagenicity of AFB1 bioactivated by either non-induced or DXM-induced S9. These effects correlated with the inhibition of cytochrome P450-linked APND activity in DXM-induced microsomes and with an inhibition of DXM- induced S9 mediated metabolism of [3H]AFB1 as determined by HPLC. Since DXM treatment has been associated with an induction of the CYP3 enzyme family, these results suggest that OD and SB may possess antimutagenic and antitumorigenic activity towards AFB1 through an inhibition of CYP3-mediated metabolism of AFB1. Registry Numbers: EC 1.5.3.- (Aminopyrine N-Demethylase) 1162-65-8 (Aflatoxin B1) 32215-02-4 (aflatoxin P1) 50-02-2 (Dexamethasone) 52819-96-2 (aflatoxin Q1) 6795-23-9 (Aflatoxin M1) 9035-51-2 (Cytochrome P-450) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****EUROPEAN JOURNAL OF PHARMACOLOGY***** Huang HC Wang HR Hsieh LM Antiproliferative effect of baicalein, a flavonoid from a Chinese herb, on vascular smooth muscle cell. In: Eur J Pharmacol (1994 Jan 4) 251(1):91-3 ISSN: 0014-2999 The effects of baicalein, baicalin and wogonin, the flavonoids from Scutellaria baicalensis, on the proliferative responses of cultured rabbit vascular smooth muscle cells were studied. The proliferative response was determined from the uptake of tritiated thymidine. In rabbit vascular smooth muscle cells, all three flavonoids dose dependently inhibited the proliferative response induced by 5% fetal calf serum at the dose range of 10(-6) to 10(-4) M. Baicalin and wogonin were less effective than baicalein as inhibitors of the serum- induced smooth muscle cell proliferation, indicating that the three hydroxyl groups on positions 5, 6 and 7 seem to be necessary and sufficient for full inhibitory activity against the proliferative response of smooth muscle cells. Baicalein had a greater inhibitory effect on the proliferative reponse stimulated by platelet-derived growth factor than on serum-stimulated proliferation. Baicalein, a flavonoid with antiproliferative and lipoxygenase-inhibitory activities, may be useful as another template for the development of better drugs to prevent the pathological changes of atherosclerosis and restenosis. Registry Numbers: 21967-41-9 (baicalin) 491-67-8 (baicalein) 50-89-5 (Thymidine) 632-85-9 (wogonin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****INTERNATIONAL JOURNAL OF IMMUNOPHARMACOLOGY***** Matsuura K Kawakita T Nakai S Saito Y Suzuki A Nomoto K Role of B-lymphocytes in the immunopharmacological effects of a traditional Chinese medicine, xiao-chai-hu-tang (shosaiko-to). In: Int J Immunopharmacol (1993 Feb) 15(2):237-43 ISSN: 0192-0561 We previously reported that a traditional Chinese medicine, Xiao-chai- hu-tang (Japanese name: Shosaiko-to), induced interferon (IFN) activity in the serum of mice after intraperitoneal (i.p.) administration. In the present study in which murine spleen cells were cultured in vitro with Shosaiko-to, B-cells isolated by anti- immunoglobulin-coated plates were confirmed to generate IFN in response to Shosaiko-to stimulation. IFN activity was induced in the serum after i.p. administration of Glycyrrhizae radix, Scutellariae radix, Bupleuri radix and Pinelliae tuber which are included in Shosaiko-to as its constituent. Such an IFN-inducing activity was confirmed to exist in methanol-insoluble fractions of these extracts derived from Shosaiko-to and these constituents but not in methanol- soluble fractions. These four extracts as well as Shosaiko-to, induced interleukin 6 (IL-6) in the serum after the administration. In in vitro stimulation of spleen cells, Shosaiko-to and extracts of Glycyrrhizae radix, Bupleuri radix and Pinelliae tuber showed mitogenic activity, but an extract of Scutellariae radix with in vivo IFN-inducing activity did not. B-cells appear to participate in the immunopharmacological effects of Shosaiko-to through mitogenic activity, IFN induction and the effect of IL-6. Registry Numbers: 63364-01-2 (saiko-keishi-to) 9008-11-1 (Interferons) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF CHROMATOGRAPHY***** Wakui Y Yanagisawa E Ishibashi E Matsuzaki Y Takeda S Sasaki H Aburada M Oyama T Determination of baicalin and baicalein in rat plasma by high- performance liquid chromatography with electrochemical detection. In: J Chromatogr (1992 Mar 13) 575(1):131-6 ISSN: 0021-9673 A rapid and sensitive method, using electrochemical detection, has been developed for the determination of baicalin and baicalein, the flavonoid of Scutellariae radix, in rat plasma. Following separation by high-performance liquid chromatography, baicalin and baicalein were oxidized at a glassy carbon electrode to permit selective electrochemical detection. Absolute detection limits were found to be 5 ng/ml from 50 microliters of plasma for baicalin and 2 ng/ml from 100 microliters of plasma for baicalein. The resulting assays were suitable for pharmacokinetic studies of baicalin and baicalein in rats. Registry Numbers: 21967-41-9 (baicalin) 491-67-8 (baicalein) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF ETHNOPHARMACOLOGY***** Umeda M Amagaya S Ogihara Y Effects of certain herbal medicines on the biotransformation of arachidonic acid: a new pharmacological testing method using serum. In: J Ethnopharmacol (1988 May-Jun) 23(1):91-8 ISSN: 0378-8741 Two in vitro experimental systems were compared to evaluate the pharmacological effects of some herbal medicines on the biotransformation of arachidonic acid (AA) using the microsomal fraction of sheep vesicular glands as an enzyme source. The first system involved the addition of serum obtained from rats treated orally with the herbal medicines, while the second system involved the direct addition of herbal medicine extracts to the enzyme medium. Both systems were performed in parallel. Indomethacin, used as a reference drug, inhibited AA biotransformation in a dose-dependent manner in both experimental systems. The serum of rats orally pretreated for 1 h with Coptis japonica rhizome and Paeonia lactiflora root also inhibited AA biotransformation. Direct addition of hot water extracts of Rheum officinale rhizome, Scutellaria baicalensis root, Paeonia moutan bark and Zingiber officinale rhizome also inhibited AA biotransformation, while the extracts of Coptis japonica rhizome and Paeonia lactiflora root showed no effects. Registry Numbers: 506-32-1 (Arachidonic Acid) 53-86-1 (Indomethacin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF INFECTIOUS DISEASES***** Baylor NW Fu T Yan YD Ruscetti FW Inhibition of human T cell leukemia virus by the plant flavonoid baicalin (7-glucuronic acid, 5,6-dihydroxyflavone). In: J Infect Dis (1992 Mar) 165(3):433-7 ISSN: 0022-1899 The ability of baicalin (7-glucuronic acid, 5,6-dihydroxyflavone), a flavonoid compound purified from the Chinese medicinal herb, Scutellaria baicalensis georgi, to inhibit human T cell leukemia virus type I (HTLV-I) was examined. Baicalin produced concentration- dependent inhibition of HTLV-I replication in productively infected T and B cells. Moreover, baicalin treatment selectively reduced the detectable levels of HTLV-I p19 gag protein in infected cells by greater than 70% at concentrations that produced insignificant effects on total cellular protein and DNA synthesis with no loss in cell viability. Resistance to HTLV-I infection and virus-mediated transformation was noted in uninfected peripheral blood lymphocytes pretreated with baicalin before cocultivation with lethally irradiated chronically infected cells. Baicalin inhibited reverse transcriptase activity in HTLV-I-infected cells as well as the activity of purified reverse transcriptase from Moloney murine leukemia virus and Rous-associated virus type 2. These results suggest that baicalin may be a potential therapeutic agent against HTLV-I-associated T cell diseases. Registry Numbers: EC 2.7.7.49 (RNA-Directed DNA Polymerase) 21967-41-9 (baicalin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF PHARMACY AND PHARMACOLOGY***** Homma M Oka K Niitsuma T Itoh H A novel 11 beta-hydroxysteroid dehydrogenase inhibitor contained in saiboku-to, a herbal remedy for steroid-dependent bronchial asthma. In: J Pharm Pharmacol (1994 Apr) 46(4):305-9 ISSN: 0022-3573 To identify the inhibitor of prednisolone metabolism contained in Saiboku-To, we conducted in-vitro experiments of 11 beta- hydroxysteroid dehydrogenase (11 beta-HSD), using rat liver homogenate and cortisol as a typical substrate. We studied the effects of ten herbal constituents on 11 beta-HSD. Five herbal extracts showed inhibitory activity with Glycyrrhiza glabra > Perillae frutescens > Zizyphus vulgaris > Magnolia officinalis > Scutellaria baicalensis. This suggests that unknown 11 beta-HSD inhibitors are contained in four herbs other than G. glabra which contains a known inhibitor, glycyrrhizin (and glycyrrhetinic acid). Seven chemical constituents which have been identified as the major urinary products of Saiboku-To in healthy and asthmatic subjects were studied; magnolol derived from M. officinalis showed the most potent inhibition of the enzyme (IC50, 1.8 x 10(-4) M). Although this activity was less than that of glycyrrhizin, the inhibition mechanism (non-competitive) was different from a known competitive mechanism. These results suggest that magnolol might contribute to the inhibitory effects of Saiboku-To on prednisolone metabolism through inhibition of 11 beta-HSD. Registry Numbers: EC 1.1.- (Hydroxysteroid Dehydrogenases) EC 1.1.1.146 (11 beta-hydroxysteroid dehydrogenase) 1405-86-3 (glycyrrhizic acid) 35354-74-6 (honokiol) 471-53-4 (Glycyrrhetinic Acid) 50-23-7 (Hydrocortisone) 528-43-8 (magnolol) 53-06-5 (Cortisone) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JAPANESE JOURNAL OF PHARMACOLOGY***** Takase H Inoue O Saito Y Yumioka E Suzuki A Roles of sulfhydryl compounds in the gastric mucosal protection of the herb drugs composing oren-gedoku-to (a traditional herbal medicine). In: Jpn J Pharmacol (1991 Aug) 56(4):433-9 ISSN: 0021-5198 We investigated the involvement of sulfhydryl compounds in the cytoprotective effect of each component herb drug composing Oren- gedoku-to (OGT) against ethanol-induced gastric lesions and potential difference (PD) reduction in comparison with that of OGT in rats. Pretreatment with N-ethylmaleimide (NEM) significantly blocked the cytoprotective effects of OGT, Coptidis rhizoma and Phellodendri cortex, but did not block the cytoprotective effects of Gardeniae fructus and Scutellariae radix. The inhibitory effects of OGT, Coptidis rhizoma and Phellodendri cortex against the PD reduction disappeared in the presence of NEM or diethyldithiocarbamate (DDC), whereas NEM or DDC had little or no effect with Gardeniae fructus and Scutellariae radix. These results suggest that the gastric mucosal protection of Coptidis rhizoma and Phellodendri cortex may be ascribed to the reinforcement of mucosal barrier resistance through endogenous sulfhydryl compounds and DDC-sensitive compounds, but those of Gardeniae fructus and Scutellariae radix may be independent of NEM- or DDC-sensitive compounds. Registry Numbers: 128-53-0 (Ethylmaleimide) 147-84-2 (Ditiocarb) 64-17-5 (Alcohol, Ethyl) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Takase H Imanishi K Miura O Yumioka E Watanabe H Features of the anti-ulcer effects of Oren-gedoku-to (a traditional Chinese medicine) and its component herb drugs. In: Jpn J Pharmacol (1989 Mar) 49(3):301-8 ISSN: 0021-5198 This report describes the features of the anti-ulcer effect of Oren- gedoku-to (OGT, a traditional Chinese medicine) and its component herb drugs. Coptidis rhizoma and Phellodendri cortex given orally dose-dependently inhibited the appearance of ethanol-induced gastric hemorrhagic lesions in a dose range of 25-100 mg/kg, but the formation of the lesions was not prevented by Scutellariae radix or Gardeniae fructus at the same doses. Coptidis rhizoma, Phellodendri cortex and Gardeniae fructus inhibited the gastric potential difference (PD) reduction induced by ethanol, whereas Scutellariae radix did not prevent the decrease in the PD reduction caused by ethanol. Phellodendri cortex, Scutellariae radix and Gardeniae fructus had no significant influence on the basal PD, while Coptidis rhizoma increased the basal PD. The four herb drugs prevented gastric acid secretion induced by 2-deoxy-D-glucose, but the three drugs except for Phellodendri cortex showed little effect on pentagastrin- stimulation. These results suggest that the gastric mucosal protection by OGT is ascribed to Coptidis rhizoma and Phellodendri cortex, and its antisecretory effect is due to the four drugs. Registry Numbers: 5534-95-2 (Pentagastrin) 64-17-5 (Alcohol, Ethyl) 7683-59-2 (Isoproterenol) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****MOLECULAR PHARMACOLOGY***** Liu XF Liu ML Iyanagi T Legesse K Lee TD Chen SA Inhibition of rat liver NAD(P)H:quinone acceptor oxidoreductase (DT- diaphorase) by flavonoids isolated from the Chinese herb scutellariae radix (Huang Qin). In: Mol Pharmacol (1990 Jun) 37(6):911-5 ISSN: 0026-895X The glucuronide conjugates of oroxylin A and two other flavones, baicalein, and wogonin, were isolated from the methanol extract of the herb scutellariae radix (Huang Qin) and were found to be inhibitors of rat liver NAD(P)H:quinone acceptor oxidoreductase (EC 1.6.99.2). Baicalin (baicalein 7-O-glucuronide) and oroxylin-A 7-O- glucuronide are approximately 50-fold more potent than wogonin 7-O- glucuronide. The enzyme kinetic analysis revealed that oroxylin-A 7-O- glucuronide is a competitive inhibitor with respect to NADH (the electron donor), with a Ki value of 63 nM. Considering the similarities of their structures and inhibition kinetics to those of dicoumarol, it is thought that oroxylin-A 7-O-glucuronide and the other two flavonoids bind to an identical site and inhibit this quinone reductase in the same fashion as dicoumarol. The results also suggest that the inhibition of NAD(P)H:quinone acceptor oxidoreductase or another vitamin K reductase by oroxylin-A 7-O- glucuronide and the related flavonoids may be one of the steps associated with the anticoagulation action of the herb. These compounds are potentially useful anticoagulant drugs. Registry Numbers: EC 1.6.99. (Quinone Reductases) EC 1.6.99.2 (NAD(P)H Dehydrogenase (Quinone)) 66-76-2 (Dicumarol) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****MUTATION RESEARCH***** Wong BY Lau BH Tadi PP Teel RW Chinese medicinal herbs modulate mutagenesis, DNA binding and metabolism of aflatoxin B1. In: Mutat Res (1992 Jun 1) 279(3):209-16 ISSN: 0027-5107 Oldenlandia diffusa (OD) and Scutellaria barbata (SB) have been used in traditional Chinese medicine for treating liver, lung and rectal tumors while Astragalus membranaceus (AM) and Ligustrum lucidum (LL) are often used as an adjunct in cancer therapy. In this study, we determined the effects of aqueous extracts of these four herbs on aflatoxin B1 (AFB1)-induced mutagenesis using Salmonella typhimurium TA100 as the bacterial tester strain and rat liver 9000 x g supernatant as the activation system. The effects of these herbs on [3H]AFB1 binding to calf-thymus DNA were assessed. Organosoluble and water-soluble metabolites of AFB1 were extracted and analyzed by high- performance liquid chromatography (HPLC). Mutagenesis assays revealed that all of these herbs produced a concentration-dependent inhibition of histidine-independent revertant (His+) colonies induced by AFB1. At a concentration of 1.5 mg/plate, SB and OD in combination exhibited an additive effect. The trend of inhibition of these four herbs on AFB1-induced mutagenesis was: SB greater than LL greater than AM. LL, OD and SB significantly inhibited AFB1 binding to DNA, reduced AFB1-DNA adduct formation, and also significantly decreased the formation of organosoluble metabolites of AFB1. Our data suggest that these Chinese medicinal herbs possess cancer chemopreventive properties. Registry Numbers: 1162-65-8 (Aflatoxin B1) 9007-49-2 (DNA) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Sakai Y Nagase H Ose Y Sato T Kawai M Mizuno M Effects of medicinal plant extracts from Chinese herbal medicines on the mutagenic activity of benzo[a]pyrene. In: Mutat Res (1988 Nov) 206(3):327-34 ISSN: 0027-5107 The effects of medicinal plants on the mutagenicity of benzo[a]pyrene were studied with Salmonella typhimurium tester strains. The chosen medicinal plants are very frequently used as Chinese herbal medicines. Each medicinal plant was extracted with hot water, which is similar to the method used in Chinese medicinal treatment. Cinnamomi cortex, Rhei rhizoma, Scutellariae radix and Rehmanniae radix were found to decrease the mutagenic activity of benzo[a]pyrene. Atractylodis rhizoma also reduced the mutagenicity of benzo[a]pyrene, but this was not certain, because it showed a killing effect on the cell survival test. Bupleuri radix and Aurantii nobilis pericarpium had an enhancing effect, but then neither of these extracts is itself mutagenic. Each medicinal plant extract showed a different effect on the mutagenicity of benzo[a]pyrene. These effects were classified into 5 types: (I) decreasing effect, (II) killing effect, (III) enhancing effect, (IV) enhancing and decreasing effect and (V) inactive. Registry Numbers: 50-32-8 (Benzo(a)pyrene) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****NIPPON YAKURIGAKU ZASSHI. FOLIA PHARMACOLOGICA JAPONICA***** Minematsu S Taki M Watanabe M Takahashi M Wakui Y Ishihara K Takeda S Fujii Y [Effects of Shosaiko-to-go-keishikashakuyaku-to (TJ-960) on the valproic acid induced anomalies of rat fetuses] In: Nippon Yakurigaku Zasshi (1990 Nov) 96(5):265-73 ISSN: 0015-5691 (Published in Japanese) Shosaiko-to-go-keishikashakuyaku-to (TJ-960) is an extract of nine herbal drugs (Paeoniae radix, Cinna momi cortex, Bupleuri radix, Zingiberis rhizoma, Glycyrrhizae radix, Ginseng radix, Scutellariae radix, Pinelliae tuber and Zizyphi fructus) that has a potent anticonvulsant action. The rat fetuses treated orally with TJ-960 during the organogenesis period (days 7-17 of gestation) revealed no anomalies (up to 3000 mg/kg/day). When TJ-960 was co-administered with sodium valproate (VPA, 400 mg/kg) during the organogenesis period, embryonic resorption, fetal body weight, ossification and skeletal variation or anomalies induced by VPA were markedly reduced. The maternal plasma and embryonic concentration of VPA with TJ-960, however, were not significantly different from VPA alone. These results suggest that TJ-960 has protective effects against the teratogenicity of VPA. Registry Numbers: 63364-01-2 (saiko-keishi-to) 99-66-1 (Valproic Acid) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PHYTOCHEMISTRY***** Calis I Saracoglu I Basaran AA Sticher O Two phenethyl alcohol glycosides from Scutellaria orientalis subsp. pinnatifida. In: Phytochemistry (1993 Apr) 32(6):1621-3 ISSN: 0031-9422 Two new phenethyl alcohol glycosides, darendoside A and B (= deacyl martynoside) were isolated from the methanolic extract of the aerial parts of Scutellaria orientalis subsp. pinnatifida, along with four known glycosides, syringin, martynoside, leucosceptoside A and verbascoside. On the basis of chemical and spectral evidence the structures of darendoside A and B were determined as beta-(4- hydroxyphenyl)ethyl O-beta-D-apiofuranosyl-(1-->2)-O-beta-D- glucopyranoside and beta-(3-hydroxy-4-methoxyphenyl)ethyl O-alpha-L- rhamnopyranosyl-(1-->3)-O-beta-D-glucopyranoside (= deacyl martynoside), respectively. Registry Numbers: 118-34-3 (syringin) 149596-95-2 (darendoside A) 60-12-8 (Phenylethyl Alcohol) 94410-28-3 (darendoside B) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Ishimaru K Nishikawa K Omoto T Asai I Yoshihira K Shimomura K Two flavone 2'-glucosides from Scutellaria baicalensis. In: Phytochemistry (1995 Sep) 40(1):279-81 ISSN: 0031-9422 Two new flavone glucosides, 5,2',6'-trihydroxy-6,7,8- trimethoxyflavone 2'-O-glucoside and 5,2',6'-trihydroxy-6,7- dimethoxyflavone 2'-O-glucoside were isolated from the aqueous methanol extract of the roots of Scutellaria baicalensis. From the extract, seven phenolics, 5,7,2',6'-terahydroxyflavone, 5,7,2',5'- tetrahydroxy-8,6'-dimethoxyflavone, skullcapflavone II, baicalin, baicalin methyl ester, wogonin 7-glucuronide and 3,5,7,2',6'- pentahydroxyflavanone were also isolated. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PLANTA MEDICA***** Nagai T Yamada H Otsuka Y Inhibition of mouse liver sialidase by the root of Scutellaria baicalensis. In: Planta Med (1989 Feb) 55(1):27-9 ISSN: 0032-0943 Of 266 Chinese crude drugs, the hot water extract from the root of Scutellaria baicalensis showed potent mouse liver sialidase inhibitory activity; in addition, wogonin, wogonin glucuronide, baicalein, and baicalin were identified as the inhibitors. These flavonoids showed almost the same inhibitory activity when 50-125 micrograms/ml doses of the samples were used for the assay, while wogonin and baicalein showed a more potent activity than wogonin glucuronide and baicalin at the lower concentration (10 micrograms/ml). However, these flavonoids, except wogonin, showed negligible inhibitory activity against Arthrobacter ureafaciens sialidase. These results indicated that S. baicalensis extract contains the sialidase inhibitors which are specific to mouse liver sialidase. Registry Numbers: EC 3.2.1.18 (Neuraminidase) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Chung CP Park JB Bae KH Pharmacological effects of methanolic extract from the root of Scutellaria baicalensis and its flavonoids on human gingival fibroblast. In: Planta Med (1995 Apr) 61(2):150-3 ISSN: 0032-0943 The methanolic extract from the root of Scutellaria baicalensis Georgi and its flavonoids, wogonin, baicalein, and baicalin were evaluated for anti-inflammatory action and the activatory effect on gingival fibroblasts. In LPS-induced production of IL-1 beta, three flavonoids at 1 microgram/ml expressed a significant (> 50%) inhibitory effect, similar to that of prednisolone. Moreover, the flavonoids inhibited IL-1 beta-induced synthesis of PGE2 and LTB4 considerably, although the effect of wogonin on LTB4 synthesis was marginal. In addition, three flavonoids exerted a moderate inhibition (33-36%) of collagenolytic activity, comparable to 40% inhibition by tetracycline. Meanwhile, the cellular activity of fibroblasts was augmented remarkably (40%) by baicalein (2) and slightly by baicalin (3) or wogonin (1). Consistent with the cellular activation, flavonoids enhanced the synthesis of both collagen and total protein in fibroblasts, in contrast to growth factors which increased only the synthesis of total protein. Although the effects of the methanolic extract resembled those of the flavonoids, the extract expressed a preferential effect on the synthesis of collagen and total protein. Registry Numbers: EC 3.4.24.- (Collagenases) 67-56-1 (Alcohol, Methyl) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PROCEEDINGS / ANNUAL MEETING OF THE AMERICAN ASSOCIATION FOR***** Wong BY Jia TY Wan CP Lau BH Chinese medicinal herbs inhibit tumor growth and augment macrophage oxidative burst (Meeting abstract). In: Proc Annu Meet Am Assoc Cancer Res (1994) 35:A2856 ISSN: 0197-016X Oldenlandia diffusa (OD) and Scutellaria barbata (SB) are two medicinal herbs frequently found in various herbal formulas used for treating cancers in China. In this study, we determined the effects of these herbs on the growth of a murine renal cell carcinoma (RENCA) and their effects on oxidative burst of a murine macrophage cell line, J774. Balb/c mice were transplanted subcutaneously with 1 x 10(5) RENCA cells. They were divided into groups to receive oral feeding of OD (4 mg/day), SB (4 mg/day), or saline as control. Oral feeding with OD or SB resulted in 79% and 78% reduction of tumor volumes, respectively. Oxidative burst of J774 cells was monitored with a microfluorometric assay using 2',7-'dichlorofluorescin diacetate. Both OD and SB exhibited a dose-dependent enhancement of the oxidative burst of J774 cells. Macrophages can infiltrate into the tumor site to cause inflammatory reactions leading to tumor destruction. Our data suggest that these phytochemicals may exert their antitumor effects, in part, via augmentation of phagocyte functions. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Wong BY Lau BH Teel RW EFFECTS OF CHINESE MEDICINAL HERBS ON MUTAGENESIS, DNA BINDING AND METABOLISM OF AFLATOXIN B1 (MEETING ABSTRACT) In: Proc Annu Meet Am Assoc Cancer Res (1992) 33:A977 ISSN: 0197-016X Oldenlandia diffusa (OD) and Scutellaria barbata (SB) have been used in traditional Chinese medicine for treating liver, lung and rectal tumors while Astragalus membranaceous and Ligustrum lucidum are often used as an adjunct in cancer therapy. This study determined the effects of aqueous extracts of these 4 herbs on aflatoxin B1 (AFB1)- induced mutagenesis using Salmonella typhimurium TA100, on [3H]AFB1 binding to calf thymus DNA, and on the formation of organosoluble and water-soluble metabolites of AFB1. Mutagenesis assays revealed that all of these herbs produced a concentration-dependent inhibition of histidine-independent revertant (His+) colonies induced by AFB1. OD and SB significantly inhibited AFB1 binding to DNA, reduced AFB1-DNA adduct formation, and also significantly decreased the formation of organosoluble metabolites of AFB1. Our data suggest that these Chinese medicinal herbs possess cancer chemopreventive properties. Registry Numbers: 10028-17-8 (Tritium) 1162-65-8 (Aflatoxin B1) 9007-49-2 (DNA) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PROCEEDINGS, ANNUAL MEETING OF THE AMERICAN SOCIETY OF CLINICAL***** Sakata Y Suzuki H Kamataki T Preventive effect of TJ-14, a Kampo medicine, on diarrhea induced by irinotecan (Meeting abstract). In: Proc Annu Meet Am Soc Clin Oncol (1994) 13:A1578 ISSN: 0736-7589 Diarrhea is one of the dose-limiting factors of irinotecan (CPT-11) and its incidence is over 60% in patients receiving this drug. CPT-11 causes both early and late diarrhea. The early diarrhea (ED) is observed from immediately after CPT-11 infusion and it is due to cholinergic effect of CPT-11. The late diarrhea (LD) usually occurs 3- 7 days after CPT-11 infusion and tends to be more severe than ED. Effective supportive therapy for LD has not yet been established. Our non clinical findings have suggested that the mechanism of LD is strongly related to the metabolism of CPT-11. CPT-11 is transformed to an active metabolite SN-38, by carboxylesterase, and then is converted to SN-38-glucuronide by glucuronyltransferase in the liver. This glucuronide is excreted in the bile and is transformed back to SN-38 again by the beta-glucuronidase (beta-G) of intestinal microflora. The SN-38 is supposed to injure intestinal mucosa and cause LD. Thus, LD could possibly be reduced by inhibiting beta-G. We found that baicalin, one of the ingredients of Scutellaria baicalensis (SB), was a strong beta-G inhibitor. However, baicalin is not available for clinical use. Therefore, we used Hange-shashin-to (TJ-14), an ethical Kampo medicine with a high SB content, to prevent LD. Twenty-three patients (pts) were studied, including 9 lung cancer, 4 pancreatic cancer, 2 colorectal cancer, 4 malignant lymphoma, and 4 other types of cancer. All pts were treated with CPT- 11 in combination with oral TJ-14 (7.5 g tid) prior to CPT-11 infusion. The dose of CPT-11 was 60 mg/m2/w in 8 pts, 80 mg/m2/w in 3 pts, greater than 100 mg/m2/1-2 w in 7 pts, 40 mg/m2/d x 3 days/w in 2 pts, and some other dose in 3 pts. Four pts could not tolerate TJ- 14 due to its odor. Nine pts showed an excellent response (no diarrhea or only 1 day of ECOG grade 1 diarrhea) and 9 pts showed a good response (grade 1 diarrhea that disappears within 3 days). Thus, the response rate of TJ-14 on diarrhea induced by CPT-11 was 95% (18/19). The response rate of CPT-11 was 39% (9/23), including 3 CRs and 6 PRs. We conclude that TJ-14 has a preventive effect on diarrhea induced by CPT-11 without reducing the antitumor activity. Registry Numbers: 100286-90-6 (CPT 11) 7689-03-4 (Camptothecin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PROCEEDINGS OF THE NATIONAL SCIENCE COUNCIL, REPUBLIC OF CHINA. Liao JF Jan YM Huang SY Wang HH Yu LL Chen CF Evaluation with receptor binding assay on the water extracts of ten CNS-active Chinese herbal drugs. In: Proc Natl Sci Counc Repub China B (1995 Jul) 19(3):151-8 ISSN: 0255-6596 In the present study, we established receptor binding assays to evaluate the water extracts of ten central nervous system (CNS)- active Chinese herbal drugs. These ten herbal drugs are Chaihu (Radix Bupleuri), Chuanxiong (Rhizoma Chuanxiong), Danggui (Radix Angelicae sinensis), Danshen (Radix Salviae miltiorrhizae), Duhuo (Radix Angelicae pubescentis), Hangqin (Radix Scutellariae), Qinjiao (Radix Gentianae macrophyllae), Shengma (Rhizoma Cimicifugae), Suanzaoren (Semen Zizphi spinose), and Yangjihua (Flos Daturae). The results indicated that these water extracts contained the principles acting on the dopamine (D1 & D2), muscarinice acetylcholine (M1), or 5-HT (5- HT1A & 5-HT2) receptors, or the benzodiazepine and the gamma-amino-n- butyric acid (GABA) binding sites of GABAA receptors as determined by receptor binding assays. The receptors or binding sites which predominantly acted by each water extract are listed as follows: Chaihu: D2, 5-HT1A, GABA; Chuanxiong: GABA, 5-HT1A; Danggui: GABA, 5- HT1A; Danshen: BDZ; Duhuo: GABA, 5-HT1A, D2, D1; Hangqin: BDZ, D1, 5- HT1A; Qinjiao: GABA, BDZ, 5-HT1A, D2; Shengma: 5-HT1A; Suanzaoren: 5- HT1A, 5-HT2, GABA; Yangjihua: M1, 5-HT1A, 5-HT2. These results provided evidence to explain the CNS effects of these herbal drugs at the receptor level. Furthermore, these results provided information to direct the isolation and purification of receptor-interactive compounds from these herbal drugs. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****REPRODUCTIVE TOXICOLOGY***** Kim SH Kim YH Han SS Roh JK Teratogenicity study of Scutellariae Radix in rats. In: Reprod Toxicol (1993) 7(1):73-9 ISSN: 0890-6238 This teratogenicity study was carried out in pregnant S.P.F. Sprague- Dawley female rats. These animals received for a period of 11 days, from day 7 to 17 of gestation, by daily oral administration, the water extract concentrates of the medicinal herb, Scutellariae Radix, at dose levels of 0.25 g/kg (group I), 12.49 g/kg (group II), and 24.98 g/kg (group III). Two-thirds of pregnant females in each group were sacrificed on day 20 of gestation and their fetuses were examined. The remaining dams were allowed to litter naturally, and postnatal development of the offspring was observed. There was a significant (P < 0.05) dose-dependent increase in the incidence of skeletal variations (presence of lumbar rib). There was also a dose- dependent increase in the incidence of abnormal urinary system (mainly dilatation of ureter) although the abnormality incidence of group III was comparable to group II. There were no significant differences between the control and treated groups in maternal body weight, intake of diet and water, efficiency of diet, hematologic values, resorbed and dead fetuses, corpora lutea, separation of eyelids, emergence of abdominal hair and incisors, traction test values, sex organ function in fetuses, and growth of fetuses. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ **RESEARCH COMMUNICATIONS IN MOLECULAR PATHOLOGY AND PHARMACOLOGY** Gao D Sakurai K Chen J Ogiso T Protection by baicalein against ascorbic acid-induced lipid peroxidation of rat liver microsomes. In: Res Commun Mol Pathol Pharmacol (1995 Oct) 90(1):103-14 ISSN: 1078-0297 The effect of baicalein (5,6,7-trihydroxy-2-phenyl-4H-1-benzopyran-4- one), a flavonoid isolated from Scutellaria baicalensis Georgi, on lipid peroxidation in rat liver microsomes was studied. Ascorbic acid- induced lipid peroxidation in microsomes obtained from baicalein- treated rats was inhibited by treatment on different days and at different doses. Iron release induced by ascorbic acid from microsomes of baicalein-treated rats was markedly lower than from microsomes of control rats. However, no statistical differences in total, nonheme and nonprotein-bound (free iron) iron contents could be detected in the two microsomes. The degradation of calf thymus DNA, an indicator of free iron existence, was observed in the reactions of microsomes obtained from control and baicalein-treated rats with ascorbic acid in the presence of bleomycin. These results suggest that baicalein can inhibit lipid peroxidation in microsomes induced by ascorbic acid by forming an inert complex of iron. Registry Numbers: 11056-06-7 (Bleomycin) 117-39-5 (Quercetin) 153-18-4 (Rutin) 491-67-8 (baicalein) 50-81-7 (Ascorbic Acid) 7439-89-6 (Iron) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****VESTNIK ROSSIISKOI AKADEMII MEDITSINSKIKH NAUK***** Daugel'-Dauge NO Durnev AD Kulakova AV Seredenin SB Velichkovskii BT [Corpuscular mutagenesis and its prevention] Korpuskuliarnyi mutagenez i ego profilaktika. In: Vestn Ross Akad Med Nauk (1995)(1):29-38 ISSN: 0869-6047 (Published in Russian) The carcinogenic and mutagenic activity of dust containing chrysotile- asbestos and zeolites, as well as the role of active oxygen species in their cytotoxic and mutagenic actions are discussed. Superoxide dismutase (50 mg/ml) was demonstrated to prevent the mutagenic effects of chrysotile-asbestos and latex, catalase (20 mg/ml) to prevent the same of zeolites in experiments on cultured human whole blood. The intraperitoneal administration of dusts of chrysotile- asbestos and zeolites in a dose of 50 mg/kg to C57B1/6 mice was found to elevate the count of cells with chromosomal aberrations in the peritoneal liquid and bone marrow cells of mice, which was dependent on dust exposure time. It was revealed that ascorbic acid, rutin, chemically modified flavonoid of Scutellaria Baicalensis Georgy, drugs such as bemitil and thomersol in the broad range of concentrations (10(-7)-10(-3) M) decreased or completely reduced the clustogenic action of zeolites and chrysotile-asbestos on cultured human whole blood. The ability of bemitil (1.8-19 mg/kg) rather than the others to prevent the mutagenic effect of chrysotile-asbestos was confirmed by the method of recording chromosomal aberrations in the cells of peritoneal liquid and bone marrow in mice. The findings suggest that the mutagenic effects of the corpuscular xenobiotics under study are mediated by active oxygen species and that the use of the models in vitro and in vivo is adequate for investigations into corpuscular mutagenesis. Based on their own data and literature data, the authors have defined possible lines of further research of corpuscular mutagenesis. Registry Numbers: 1318-02-1 (Zeolites) 1332-21-4 (Asbestos) 63513-71-3 (bemethyl) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****VOPROSY ONKOLOGII***** Razina TG Udintsev SN Tiutrin II Borovskaia TG Iaremenko KV [The role of thrombocyte aggregation function in the mechanism of the antimetastatic action of an extract of Baikal skullcap] Izuchenie roli agregatsionnoi funktsii trombotsitov v mekhanizme protivometastaticheskogo deistviia ekstrakta shlemnika baikal'skogo. In: Vopr Onkol (1989) 35(3):331-5 ISSN: 0507-3758 (Published in Russian) The advancement of Pliss' lymphosarcoma in rats was shown to be associated with disorders of platelet-mediated hemostasis presenting with either lowered or increased aggregation activity of platelets. In the latter case, a direct correlation was observed between functional activity of thrombocytes, on the one hand, and degree of tumor advancement and its metastatic activity, on the other. Extract of Scutellaria baicalensis Georgi was shown to produce a normalizing effect on platelet-mediated hemostasis whatever the pattern of alteration which points to the adaptogenic activity of the drug. This activity is thought to be responsible for the drug's antitumor and, particularly, metastasis-preventing effect. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****YAKUGAKU ZASSHI. JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN***** Suzuki M Nikaido T Ohmoto T [The study of Chinese herbal medicinal prescription with enzyme inhibitory activity. V. The study of hange-shashin-to, kanzo-shashin- to, shokyo-shashin-to with adenosine 3',5'-cyclic monophosphate phosphodiesterase] In: Yakugaku Zasshi (1991 Nov) 111(11):695-701 ISSN: 0031-6903 (Published in Japanese) Fifty-nine species of extracts of Chinese herbal medicinal prescription were tested for inhibitory activity of adenosine 3',5'- cyclic monophosphate (cAMP) phosphodiesterase (PDE). Kanzo-shashin-to showed the highest activity in these prescriptions. Kanzo-shashin-to, Hange-shashin-to and Shokyo-shashin-to, whose contracting crude drugs were very similar, were especially studied among these prescriptions. Pinellia tuber acted as an ascent component for Scutellaria root and a mitigatory component for Giycyrrhiza. Jujube acted as a mitigatory component for Glycyrrhiza. Ginger acted as an additional component for Scutellaria root in cAMP PDE test. This additional effect of 6- gingerol, 6-shogaol from Ginger and baicalin from Scutellaria root were investigated. Registry Numbers: 555-66-8 (shogaol) 60-92-4 (Cyclic AMP) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Kumazawa N Ohta S Ishizuka O Sakurai N Kamogawa A Shinoda M [Protective effects of various methanol extracts of crude drugs on experimental hepatic injury induced by carbon tetrachloride in rats] In: Yakugaku Zasshi (1990 Dec) 110(12):950-7 ISSN: 0031-6903 (Published in Japanese) The protective effects of 67 methanol extracts of crude drugs on rat hepatic injury by carbon tetrachloride (CC14) were examined. In terms of the release of intrahepatic enzymes and bilirubin into the blood, 11 methanol extracts decreased these factors significantly. Among them methanol extracts of Caryophylli Flos, Angelicae Dahuricae Radix, Polygoni Avicularis Herba, Myricae Cortex and Forsythiae Fructus were newly found to have protective effects against acute hepatic injury induced by CCl4. And then these 11 extracts which protected hepatic injury by CCl4 were investigated for their membrane stabilizing and inhibitory effects of lipid peroxidation. The extract of Bupleuri Radix only decreased the hemolysis induced by hypotonic pressure. Nine kinds of extracts without those of Desmodii Herba and Bupleuri Radix suppressed the lipid peroxidation induced by CCl4 in rat hepatic microsomes. In addition, Scutellariae Radix, Caryophylli Flos and Myricae Cortex were shown to have inhibitory effects of non- enzymatic lipid peroxidation in rat hepatic mitochondria. This study reports that the methanol extracts of Caryophylli Flos, Angelicae Dahuricae Radix, Polygoni Avicularis Herba, Myricae Cortex and Forsythiae Fructus protect the hepatic injury by CC14 and these protective effects are connected with the inhibitory effects of the lipid peroxidation in hepatic microsomes. Registry Numbers: 67-56-1 (Alcohol, Methyl) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Matsuura Y Miyaichi Y Tomimori T [Studies on the Nepalese crude drugs. XIX. On the flavonoid and phenylethanoid constituents of the root of Scutellaria repens Buch.- Ham. ex D. Don] In: Yakugaku Zasshi (1994 Oct) 114(10):775-88 ISSN: 0031-6903 (Published in Japanese) From the root of Scutellaria repens Buch.-Ham ex D. Don, two new flavonoids (10, 11) and three new phenylethanoids (12-14) were isolated, together with nine known compounds. The structures of 10-14 were shown to be 5,7,2'-trihydroxy-6,8-dimethoxyflavone, O-5-hydroxy- 6,8-dimethoxyflavone-7-yl beta-D-glucuronopyranoside, O-2-(3-hydroxy- 4-methoxyphenyl)ethyl O-2,3-di-O-acethyl-alpha-L-rhamnopyranosyl- (1-- >3)-(4-O-trans-feruloyl)-beta-D-glucopyranoside, O-2-(3-hydroxy-4- methoxyphenyl)ethyl O-alpha-L-rhamnopyranosyl-(1-->3)-(4-O-cis- feruloyl)-beta-D-glu cop yranoside and O-2-(3-hydroxy-4- methoxyphenyl)-ethyl O-2,3-di-O-acethyl-alpha-L-rhamnopyranosyl- (1-- >3)-(4-O-cis-feruloyl)-beta-D- glucopyranoside, respectively, on the basis of the chemical and spectral data. Registry Numbers: 60-12-8 (Phenylethyl Alcohol) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Miyaichi Y Kizu H Yamaguchi Y Tomimori T [Studies on the constituents of Scutellaria species. XV. On the diterpenoid constituents of the leaves of Scutellaria alpina L.] In: Yakugaku Zasshi (1994 Apr) 114(4):264-71 ISSN: 0031-6903 (Published in Japanese) From the leaves of Scutellaria alpina L., four new neo-clerodane diterpenes (1-4) were isolated. The structures of 1-4 were shown to be (4S)-19-acetoxy-8 beta-hydroxy-6 alpha-benzoyloxy-4,18-epoxy-neo- cleroda-11,13- dien-15,16-olide, (4S)-19-acetoxy-8 beta-hydroxy-6 alpha-tigloyloxy-4,18-epoxy-neo-cleroda-11,13- dien-15,16-olide, (4S, 11S)-11-acetoxy-8 beta,19-dihydroxy-6 alpha-tigloyloxy-4,18-epoxy-neo- clerod-13-en-15,16-olide, and (4S)-19-acetoxy-8 beta-hydroxy-6 alpha, 7 beta-dibenzoyloxy-4,18-epoxy-neo- cleroda-11,13-dien-15,16- olide, respectively, by the chemical and spectral data. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****YAO HSUEH HSUEH PAO [ACTA PHARMACEUTICA SINICA]***** Wang YQ Matsuzaki K Takahashi K Okuyama T Shibata S Studies on the constituents of Scutellaria species. IV. High performance liquid chromatography of glucuronylflavonoids in Scutellaria ikonnikovii juz. In: Yao Hsueh Hsueh Pao (1991) 26(5):358-61 ISSN: 0513-4870 Recently several procedures have been reported for the simultaneous separation of flavonoid glycosides by high performance liquid chromatography (HPLC), and reversed phase column is more suitable than normal phase column. Even so, the simultaneous separation of flavonoids with closely related structures is not easy. We investigated a successful procedure for the simultaneous separation of glucuronyl flavonoids with 5-hydroxyl group by using a reversed phase column combined with gradient elution in the constituent studies of Scutellaria ikonnikovii Juz.. We have also studied the relationship between the retention time and the position of hydroxyls and glucuronyls in the chemical structure. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Hu BH Liu YL Zhang T Song WZ [Studies on the structure of scuteamoenin from the root of Scutellaria amoena] In: Yao Hsueh Hsueh Pao (1990) 25(4):302-6 ISSN: 0513-4870 (Published in Chinese) In containing our studies on the flavonoids from Scutellaria amoena C.H. Wright, a new flavanone (I) and six known compounds (II-VII) were isolated from the roots of this plant. On the basis of spectroscopic analysis (UV, 1H NMR, 13C NMR, MS and CD) and chemical evidence, the structure of the new compound was elucidated as (2S) - 2',5,6'-trihydroxy-7-methoxyflavanone (I) and named scuteamoenin, the other six known compounds were identified as (2R,3R) -3,5,7- trihydroxyflavanone (II), 2',3,5,6,7-pentahydroxyflavone (III), 2',5,7-trihydroxy-6-methoxyflavone (IV), skullcaflavone II (V), chrysin (VI) and beta-sitosterol (VII) respectively. Compounds II-VII were obtained from this plant for the first time. Registry Numbers: 129138-49-4 (scuteamoenin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Hu BH Liu YL [Studies on the structures of new flavonoids from the root of Scutellaria amoena] In: Yao Hsueh Hsueh Pao (1989) 24(3):200-6 ISSN: 0513-4870 (Published in Chinese) From the root of Scutellaria amoena C.H. Wright, two new flavonoids (I, II) and six known flavonoids (III-VIII) were isolated. On the basis of spectroscopic analysis (UV, 1HNMR, 13CNMR, MS and CD) and chemical evidences, the structures of I and II were elucidated as (2S)-2',5,6'-trihydroxy-7-methoxyflavanone-2'-O-beta-D-glucopyrano side (I) and (2R, 3R)-2',3,5,7-tetrahydroxyflavanone (II) respectively. The other six known compounds were identified as (2S)- 5,7,8-trihydroxyflavanone (III), (2S)-2',5,6',7-tetrahydroxyflavanone (IV), (2R, 3R)-2',3,5,6',7-pentahydroxyflavanone (V), 2',5,6',7- tetrahydroxyflavone (VI) norwogonin (VII) and oroxylin-A (VIII) respectively. Compounds III-VIII were obtained from this plant for the first time. Registry Numbers: 123914-35-2 (scuteamoenoside) 31477-95-9 (2',3,5,7-tetrahydroxyflavanone) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€