€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****ENDOCRINOLOGY***** Auf'mkolk M Ingbar JC Amir SM Winterhoff H Sourgens H Hesch RD Ingbar SH Inhibition by certain plant extracts of the binding and adenylate cyclase stimulatory effect of bovine thyrotropin in human thyroid membranes. In: Endocrinology (1984 Aug) 115(2):527-34 ISSN: 0013-7227 The present studies were undertaken to explore the mechanism by which, as previous studies have shown, freeze-dried aqueous extracts (FDE) of plants of the species Lycopus virginicus and Lycopus europaeus, Melissa officinalis (Laminaceae), and Lithospermum officinale (Boraginaceae) have the ability to inhibit at least many of the effects of exogenous and endogenous TSH on the thyroid gland. To this end, we have examined the in vitro effects of FDE from these plants on the ability of bovine TSH (bTSH) to both bind to human thyroid plasma membranes (TPM) and activate adenylate cyclase therein. FDE of these four species produced a dose-related, ultimately complete, inhibition of the binding of 125I-labeled bTSH when studied at 4 C in a 20 mM Tris-HCl-0.5% BSA buffer, pH 7.45. Half-maximum inhibition of bTSH binding was produced by approximately 50 mU/ml bTSH and only about 10-30 micrograms/ml of the four active FDE. When studied in Tris-BSA-50 mM NaCl buffer at 37 C, these FDE remained inhibitory to bTSH binding, but their potency was decreased to about one fifth of that seen in the absence of NaCl. The binding of [125I]hCG to rat testis membranes was also inhibited by all of these FDE, but no effect on the binding of [125I]insulin to crude rat liver membranes was observed. In concentrations as high as 1 mg/ml, FDE of Verbena officinalis (Verbenaceae), which belongs to the same order (Tubiflorae) as the other plants, but exhibits no antithyrotropic or antigonadotropic activity in vivo, had no effect on either the binding of bTSH to thyroid membranes or the binding of hCG to rat testis membranes. No inhibition of [125I]bTSH binding occurred when TPM were preincubated with the four active FDE, washed, and then incubated with [125I]bTSH in medium devoid of FDE. Hence, the inhibition of [125I]bTSH binding seen when labeled hormone and active FDE were added together was not due to irreversible binding of FDE to TPM or damage to the TSH receptor. When [125I]bTSH was incubated with the active FDE in Tris-BSA and the mixture was chromatographed on Sephadex G-100 using the same buffer, [125I]bTSH was shifted from an apparent mol wt of 30,000 and eluted at the void volume. Direct binding of [125I]bTSH in fractions from the new, large molecular peak was nil. Addition of a large excess of unlabeled bTSH during preincubation prevented the shift in the elution pattern of [125I] bTSH produced by these FDE.(ABSTRACT TRUNCATED AT 400 WORDS) Registry Numbers: EC 4.6.1.1 (Adenyl Cyclase) 9002-71-5 (Thyrotropin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CHUNG-KUO CHUNG HSI I CHIEH HO TSA CHIH***** Jin R Wan LL Mitsuishi T [Effects of shi-ka-ron and Chinese herbs in mice treated with anti- tumor agent mitomycin C] In: Chung Kuo Chung Hsi I Chieh Ho Tsa Chih (1995 Feb) 15(2):101-3 ISSN: 1003-5370 (Published in Chinese) The Shi-ka-Ron, and its constituent Chinese herbs Lithospermum erythrorhizon, Astragalus membranaceus and Ligusticum Wallichii were administered with antitumor agent, mitomycin C (MMC) to ICR mice, and their effects on murine macrophages and lymphocytes were studied. Peritoneal macrophages were significantly inhibited both in their number and chemotactic activity by MMC treatment. Splenic weight and blastogenic responsiveness to Concanavalin A of spleen lymphocytes also decreased significantly in MMC-treated mice. NK cell activity was also suppressed by MMC treatment. When these mice were orally treated with extracts of Shi-ka-ron or each Chinese herbs mentioned above, it showed protective effects to immunosuppressive mice on all 5 items studied. The number of macrophages, and the functions of macrophages and lymphocytes maintained the same or more than normal levels in MMC plus each group of these extracts treated mice. These results suggest that the Shi-Ka-Ron and Chinese herbs could resist immunosuppression induced by antitumor agent MMC, and its mechanisms might be correlated with stimulation of the RES (reticuloendothelial system), activation of T cell blastogenesis and NK cell cytotoxicity. Registry Numbers: 50-07-7 (Mitomycin C) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CONTRACEPTION***** Zeller FJ Breneman WR The in-vivo effect of Lithospermum ruderale on LHRH activity in the chick. In: Contraception (1981 Jul) 24(1):77-81 ISSN: 0010-7824 Lithospermum (LSPM) plant extracts can inhibit gonadotropin action in mammals and birds. The experiments reported in this paper were performed to note the possible effect of LSPM on the ability of LHRH to stimulate 32P testis uptake in immature chicks. LHRH injected 2 h before autopsy significantly increased 32P uptake in these animals. Water extracts of Lithospermum ruderale roots were administered subcutaneously at various concentrations and times before LHRH. LSPM injections of 2.0, 4.0, or 8.0 mg equivalents of dried material given 10 h before LHRH significantly suppressed the releasing hormone effect. 4.0 mg LSPM was not inhibitory at 16, 22, 38 or 46 h before LHRH. Interestingly, LHRH had a greater effect, as measured by 32P testis uptake, when given to these latter 3 groups then when given to controls. This suggests that LSPM may have prevented the release but not the synthesis of anterior pituitary gonadotropins. Registry Numbers: 33515-09-2 (Gonadorelin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Findley WE The antigonadotropic activity of Lithospermum ruderale. II. The inhibition of LRF-induced gonadotropin release in vitro. In: Contraception (1981 Feb) 23(2):157-62 ISSN: 0010-7824 The antigonadotropic activity of lithosperm extracts was investigated at the pituitary level. When lithosperm extracts were added to primary pituitary cell cultures, LRF-stimulated LH release was inhibited. The cellular LH content was reduced but basal release was not significantly affected. These results suggest that lithosperm acts to directly inhibit the ability of LRF to stimulate LH release from the gonadotropes and the ability of the gonadotropes to produce LH. Registry Numbers: 33515-09-2 (Gonadorelin) 9002-67-9 (LH) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Findley WE Jacobs BR The antigonadotropic activity of Lithospermum ruderale I. The lack of steroid-like activity at the receptor level. In: Contraception (1980 Feb) 21(2):199-205 ISSN: 0010-7824 Previous work has demonstrated that extracts from the plant Lithospermum ruderale have antigonadotropic activity. The possibility of steroidal substances being responsible for this activity was examined at the receptor level. It was found that only at very high concentrations of crude lithosperm extract (LS) was progesterone, testosterone, or estradiol displaced from their respective uterine receptors. Because such high doses of LS may be toxic and because they are not required for in vivo or in vitro bioactivity, it is concluded that the antigonadotropic components of Lithospermum ruderale probably do not as a steroid. Registry Numbers: 50-28-2 (Estradiol) 57-85-2 (Testosterone) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****EKSPERIMENTALNA MEDITSINA I MORFOLOGIIA***** Ilarionov I [Androgenic and aphrodesiac action of the medicinal plant Lithospermum Arvense (bird millet)] Androgenno i androdiziachno deistvie na lechebnoto rastenie Lithospermum arvense (ptiche proso). In: Eksp Med Morfol (1989) 28(1):28-33 ISSN: 0367-0643 (Published in Bulgarian) Acute toxicity, androgenic, gonadotropic, estrogenic and aphrodisiac effect of the whole medical plant Lithospermum aver arvense and its seeds was investigated on white rats and white mice. It was established that Semen Lithispermi arvense were nontoxic--LD50 in white rats and white mice was over 3000 mg/kg of body weight. The water extract of plant seeds, administered orally, in a dose of 300 mg/kg of body weight, had manifested aphodisiac and androgenic action. The obtained results are discussed in view of the usage of tea from Lithospermum arvense as a aphrodisiac drug. Suggestion is made that various types of medical plants of a given family could contain active components with opposite effects on the male sexual system. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****HORMONE AND METABOLIC RESEARCH***** Winterhoff H Sourgens H Kemper FH Antihormonal effects of plant extracts. Pharmacodynamic effects of lithospermum officinale on the thyroid gland of rats; comparison with the effects of iodide. In: Horm Metab Res (1983 Oct) 15(10):503-7 ISSN: 0018-5043 The antithyrotropic activity of freeze-dried-extracts from Lithospermum officinale (Lith. off. FDE) was investigated in the rat. When administered together with TSH, Lith. off. FDE blocked the TSH- induced increase in endocytotic activity of the thyroid glands followed by a strong decline of thyroid hormone levels. Furthermore, when Lith. off. FDE was injected alone it caused a decline in endogenous TSH-levels as well as in thyroidal secretion and thyroid hormone levels. The efficacy of the extract in blocking thyroid secretion was compared to that of potassium iodide and it was found that the effect of Lith. off. FDE was of more rapid onset and of longer duration, suggesting that the FDE may have a different mode of action from that of KJ. A specific interaction between TSH and the active constituents of the plant extract is discussed. Experiments on thyroidectomized and T4 substituted rats have demonstrated as an additional pharmacodynamic effect of Lith. off. FDE an inhibition of peripheral T4-deiodination. Registry Numbers: 6893-02-3 (Triiodothyronine) 7488-70-2 (Thyroxine) 7681-11-0 (Potassium Iodide) 9002-71-5 (Thyrotropin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****INTERNATIONAL JOURNAL OF IMMUNOPHARMACOLOGY***** Yamada H Cyong JC Otsuka Y Purification and characterization of complement activating-acidic polysaccharide from the root of Lithospermum euchromum Royle [published erratum appears in Int J Immunopharmacol 1986;8(5):527] In: Int J Immunopharmacol (1986) 8(1):71-82 ISSN: 0192-0561 An extraordinary potent anti-complementary substance was isolated from the root of Lithospermum euchromum Royle (Japanese name: Nan- shikon) which activates the complement system in vitro, and the active principle was shown to be acidic polysaccharide (LR- polysaccharide IIa). LR-polysaccharide IIa was purified by chromatographies on DEAE-Sepharose, Sephadex G-100, concanavalin A- Sepharose, Ricinus communis agglutinin conjugated Sepharose, Sepharose CL-6B and Sepharose CL-2B. LR-polysaccharide IIa was found to be composed of rhamnose, fucose, arabinose, xylose, mannose, galactose and glucose in the molar ratios of 2.0:2.5:3.4:2.8:5.6:9.6:14.4. The polysaccharide also contained 15% of galacturonic acid and 3.8% of protein. The methylation analysis of the polysaccharide showed that rhamnose, arabinofuranose, xylose, glucose and galactose are present as a part of the nonreducing terminal residues. The main chain and side chains are composed of ---- 3Glc1----,----3Gal1----,----6Man1----,----4Gal1, [corrected] and the branching points consist of (formula; see erratum) These results indicated that LR-polysaccharide IIa has a highly complicated structure. A marked consumption of C4 was observed after the incubation of the serum with LR-polysaccharide IIa in the presence of the Ca++ ion. The anti-complementary activity of LR-polysaccharide IIa was reduced partially in the absence of the Ca++ ion. After the incubation of the serum with LR-polysaccharide IIa in the absence of Ca++ ion, a cleavage of C3 in the serum was found to have occurred through immunoelectrophoresis as well as from the consumption of the complement when rabbit erythrocytes were used in the assay system. These results indicate that the mode of complement activation by LR- polysaccharide IIa is via both the alternative and classical pathways. Complement titer also decreased in guinea pigs upon i.p. injection of LR-polysaccharide IIa. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****INTERNATIONAL UROLOGY AND NEPHROLOGY***** Grases F Melero G Costa-Bauza A Prieto R March JG Urolithiasis and phytotherapy. In: Int Urol Nephrol (1994) 26(5):507-11 ISSN: 0301-1623 The effects of seven plants with suspected application to prevent and treat stone kidney formation (Verbena officinalis, Lithospermum officinale, Taraxacum officinale, Equisetum arvense, Arctostaphylos uva-ursi, Arctium lappa and Silene saxifraga) have been studied using female Wistar rats. Variations of the main urolithiasis risk factors (citraturia, calciuria, phosphaturia, pH and diuresis) have been evaluated. It can be concluded that beneficial effects caused by these herb infusions on urolithiasis can be attributed to some disinfectant action, and tentatively to the presence of saponins. Specifically, some solvent action can be postulated with respect to uric stones or heterogeneous uric nucleus, due to the basifying capacity of some herb infusions. Nevertheless, for all the mentioned beneficial effects, more effective and equally innocuous substances are well known. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF MEDICINAL CHEMISTRY***** Ahn BZ Baik KU Kweon GR Lim K Hwang BD Acylshikonin analogues: synthesis and inhibition of DNA topoisomerase- I. In: J Med Chem (1995 Mar 17) 38(6):1044-7 ISSN: 0022-2623 Compounds bearing an acyl group of a various size at 1'-OH of shikonin were synthesized as acyl analogues of shikonin, which was isolated from the root of Lithospermum erythrorhizon, and evaluated for inhibitory effect on topoisomerase-I activity. A selective acylation at 1'-OH of shikonin in the presence of dicyclohexylcarbodiimide and 4-(dimethylamino)pyridine gave rise to a good yield of corresponding acylshikonin derivatives. In general, analogues with an acyl group of shorter chain lengths (C2-C6) exerted a stronger inhibitory action than those with longer chain lengths (C7- C20). While the halogen substitution at C-2 of the acetyl moiety failed to increase the inhibitory potency, the placement of double bonds in the acyl group (C5-C7) augmented the potency remarkably. Of the 32 derivatives evaluated, 15 compounds exhibited a higher inhibitory effect than shikonin. Noteworthy, the inhibitory potency of acetylshikonin, propanoylshikonin, and 4-pentenoylshikonin was approximately 4-fold greater than that of camptothecin. All these data suggest that the size of acyl moiety is important for the enhancement of potency, and the presence of olefinic double bonds is also beneficial. Registry Numbers: EC 5.99.1.2 (DNA Topoisomerase) 54952-43-1 (shikonin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****MUTATION RESEARCH***** Lee H Lin JY Antimutagenic activity of extracts from anticancer drugs in Chinese medicine. In: Mutat Res (1988 Feb) 204(2):229-34 ISSN: 0027-5107 The antimutagenic activities of extracts of 36 commonly used anticancer crude drugs from Chinese herbs were studied by using the Salmonella/microsomal system in the presence of picrolonic acid or benzo[a]pyrene to test whether they contain direct or indirect antimutagens. Each crude drug was extracted with boiling water for 2 h, the method which is commonly used by Chinese people to prepare the drug for oral intake. The extracts of Pteris multifida P. showed the highest antimutagenic activity against picrolonic acid-induced mutation. The extracts of 6 other different kinds of Chinese herbs were shown to have a moderate antimutagenic activity against picrolonic acid-induced mutation, and they are: Actinidia chinensis P., Artemisia lavendulaefolia DC. and Crotalaria sessiflora L., Prunella vulgaris L., Paris polyphylla S. and Ampelopsis brevipedunculata T. The extracts of Smilax china L., Prunella vulgaris L. and Actinidia chinensis P. were demonstrated to inhibit the mutagenicity of benzo[a]pyrene completely. The 12 other kinds of extracts of Chinese herbs which had a moderate antimutagenic activity against benzo[a]pyrene were: Pteris polyphylla S., Ampelopsis brevipedunculata T., Duchesnea indica F., Gossypium herbaceum L., Lithospermum erythrorrhizon SZ., Artemisia lavendulaefolia DC., Selaginella doederleinii H., Dianthus superbus L., Centipeda minima ABA., Curcuma zedoaria R., Marsdenia tenacissima WA. and Kalopanax septemlobus K. Among them, there were 5 kinds of crude drugs, Actinidia chinensis P., Artemisia lavendulaefolia DC., Prunella vulgaris L., Paris polyphylla S. and Ampelopsis brevipedunculata T., containing antimutagenic factors against both picrolonic acid- and benzo[a]pyrene-induced mutation. Registry Numbers: 50-32-8 (Benzo(a)pyrene) 550-74-3 (picrolonic acid) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PHYTOCHEMISTRY***** Zhao JF Kiyohara H Matsumoto T Yamada H Anti-complementary acidic polysaccharides from roots of Lithospermum euchromum. In: Phytochemistry (1993 Oct) 34(3):719-24 ISSN: 0031-9422 Extremely potent complement activating (anti-complementary) polysaccharides from roots of Lithospermum euchromum were fractionated in a novel way and also assayed for mitogenic and enhancing activity of immune complex binding to macrophages in vitro. Anti-complementary activity and enhancing activity of immune complex binding were observed in the different polysaccharide fractions, but no mitogenic activity was found. The acidic polysaccharide fraction (LR-2) which had the most potent anti-complementary activity was highly heterogeneous, and on further fractionation gave active polysaccharides. Extremely potent anti-complementary polysaccharides, LR-2IId-1a, LR-2IId-1b, LR-2IId-3a and LR-2IId-5a were characterized chemically. These consisted mainly of mannose, galactose, glucose and glucuronic acid, in addition to rhamnose, fucose and arabinose as minor components. Methylation analysis showed that the four polysaccharides contained mainly (1-->3)-linked galactose, (1-->3)- linked fucose and (1-->4)-linked glucose. (1-->3)-Linked mannose was also detected in LR-2IId-1a, 1b and 5a, and (1-->4)-linked glucuronic acid in LR-2IId-1a and 1b as the major glycosidic linkages. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Fullas F Wani MC Wall ME Tucker JC Beecher CW Kinghorn AD Triterpenes from the combined leaf and stem of Lithospermum caroliniense. In: Phytochemistry (1996 Dec) 43(6):1303-5 ISSN: 0031-9422 An investigation of the combined leaf and stem of Lithospermum caroliniense afforded two new pentacyclic triterpenoids based on the olean-12-ene and taraxast-12-ene skeletal types. The structures of these compounds were elucidated on the basis of spectral analysis as 1 alpha,3 beta,23-trihydroxyolean-12-ene-28-oic acid and 3 alpha,19 beta,21 alpha,23-tetrahydroxytaraxast-12-ene-28-oic acid. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PLANTA MEDICA***** Nahrstedt A Albrecht M Wray V Gumbinger HG John M Winterhoff H Kemper FH Structures of compounds with antigonadotropic activity obtained by in vitro oxidation of caffeic acid. In: Planta Med (1990 Aug) 56(4):395-8 ISSN: 0032-0943 Two new cyclolignan derivatives were isolated by HPLC from the mixture of substances obtained after oxidation of caffeic acid with KMnO4. Their structures were elucidated by spectroscopic methods as 2,3-dicarboxy-6,7-dihydroxy-1-(3', 4'-dihydroxy)-phenyl-1, 2- dihydronaphthalene (1) and 3-carboxy-6,7-dihydroxy-1-(3', 4'- dihydroxy)-phenylnaphthalene (2). Compounds 1 and 2 exhibit antigonadotropic activity as do the extracts of crude drugs of Lycopus europaeus and Lithospermum officinale after oxidation by plant enzymes. Registry Numbers: 121242-02-2 (KS IV) 130752-21-5 (KS I) 331-39-5 (caffeic acid) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PROCEEDINGS / ANNUAL MEETING OF THE AMERICAN ASSOCIATION FOR***** Ahn BZ Baik KU Hwang BD Lim K Kweon KR Inhibitory effect of 2-(1-acyloxyalkyl)-5,8-di-hydroxynaphthoquinones on DNA topoisomerase I (Meeting abstract). In: Proc Annu Meet Am Assoc Cancer Res (1994) 35:A2709 ISSN: 0197-016X 2-(1-Hydroxy-4-methylpent-3-enyl)-5,8-dihydroxynaphthoquinone (shikonin) and 2-(1-acetoxy-4-methylpent-3-enyl)-5,8- dihydroxynaphthoquinone (acetylshikonin), isolated from the root of Lithospermum erythrorhizon, showed IC50 (inhibition concentration) values of 60 ug/ml and 15 ug/ml, respectively. The finding that acetylshikonin has a more potent inhibitory effect than shikonin prompted us to synthesize various kinds of 2-(1-acyloxyalkyl)-5,8-di- hyroxynaphthoquinones and to test the inhibitory effect. Relating the chain length of the acyl groups to the inhibitory effect reveals that the short chain length acylshikonins showed stronger inhibition than the longer chain ones. The 2-(1-acyloxyalkyl)-5,8- dihydroxynaphthoquinones with acyl chains of C2 to C5 (carbon number) have the IC50 value range of 15-50 ug/ml and turned out to show stronger inhibitory effect than that of camptothecin (IC50=50 ug/ml) in this test. Registry Numbers: 54952-43-1 (shikonin) 54984-93-9 (acetylshikonin) EC 5.99.1.2 (DNA Topoisomerase) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Kweon KR Baik KU Lim K Hwang BD Ahn BZ Inhibitory effects of Lithosperma root and its constituents on DNA topoisomerases I and II (Meeting abstract). In: Proc Annu Meet Am Assoc Cancer Res (1993) 34:A1954 ISSN: 0197-016X Petroleum ether extract of the root of Lithospermum erythrorhizon showed cytotoxic activity against L1210 cell (ED50 = 11.0 ug/ml). Acetylshikonin was eventually isolated as the active principle. This compound exhibits potent cytotoxicity against L1210 cell (ED50=0.10 ug/ml) and strong antitumor activity against S-180 cell (T/C=182%) in ICR mice. The above extract also showed inhibitory effects on DNA Topoisomerases I and II (ID50=50 ug/ml on Topo I, ID50=200 ug/ml on Topo II). Three active fractions were separated from the extract by using silica gel column. Acetylshikonin isolated from the 3rd fraction had ID50 value of 50 ug/ml against both enzymes. This activity evidently indicates that this substance is one of major active components. Its inhibitory effect on Topo I and II should be responsible for the cytotoxic activities mentioned above. Structural elucidation and enzymatic study of the active compounds from the other fractions are also in progress. Registry Numbers: EC 5.99.1.2 (DNA Topoisomerase) EC 5.99.1.3 (DNA Topoisomerase (ATP-Hydrolysing)) 54984-93-9 (acetylshikonin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****YAKUGAKU ZASSHI. JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN***** Ozaki Y Suga C Yoshioka T Morimoto T Harada M [Evaluation on equivalence of pharmacological properties between natural crude drugs and their cultured cells based on their components. Accelerative effect of lithospermi radix and inhibitory effect of coptidis rhizoma on proliferation of granulation tissue] In: Yakugaku Zasshi (1990 Apr) 110(4):268-72 ISSN: 0031-6903 (Published in Japanese) The present study was carried out to evaluate an equivalence of pharmacological properties between natural crude drugs and their cultured cells. The effects of ether extract of Lithospermi Radix and cultured cells of Lithospermum erythrorhizon Sieb. et Zucc. and aqueous extract of Coptidis Rizoma and cultured cells of Coptis japonica Makino var. dissecta Nakai on proliferation of granulation tissue in rats were compared. The ether extracts of Lithospermi Radix and the cultured cells enhanced proliferation of granulation tissue by the cotton pellet method. The potency of both extract was about the same, if results were compared with the corresponding doses which contained the same quantity of shikonin derivatives. On the other hand, the aqueous extracts of Coptidis Rhizoma and the cultured cells inhibited it. The potency of both extract was about the same, if results were compared with the corresponding doses which contained the same quantity of berberine-type alkaloids. From these results, to evaluate an equivalence of pharmacological properties between natural crude drugs and their cultured cells, it is concluded that their qualities and quantities are not so different each other and the almost same pharmacological effect expected on the basis of their uses is required. Registry Numbers: 54952-43-1 (shikonin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Yamasaki K Otake T Mori H Morimoto M Ueba N Kurokawa Y Shiota K Yuge T [Screening test of crude drug extract on anti-HIV activity] In: Yakugaku Zasshi (1993 Nov) 113(11):818-24 ISSN: 0031-6903 (Published in Japanese) The anti-HIV-1 effects of 204 crude drugs of common use in Japan were evaluated in vitro. As a result, 45 samples inhibited HIV-1-induced cytopathogenicity in MT-4 cells. In particular, the hot water extracts of Lithospermum erythrorhizon (root) and Prunella vulgaris (spike) showed the strongest anti-HIV-1 activities. Their IC100 values were both 16 micrograms/ml. In general, the hot water extracts of the crude drug suppressed the replication of HIV-1 growth more strongly than the cold water extracts. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Konoshima T Kozuka M Tokuda H Tanabe M [Anti-tumor promoting activities and inhibitory effects on Epstein- Barr virus activation of Shi-un-kou and its constituents] In: Yakugaku Zasshi (1989 Nov) 109(11):843-6 ISSN: 0031-6903 (Published in Japanese) The Kampo-prescription, Shi-un-kou, and its constituent crude drugs [Lithospermum erythrorhizon (1), Macrotomia euchroma (2) and Angelica acutiloba (3)] were assayed for their inhibitory effects on Epstein- Barr virus activation induced by the tumor promoter, 12-O- tetradecanoylphorbol-13-acetate (TPA). The crude drugs exhibited inhibitory activity singly and in combinations. In particular, the combination of 2 and 3 yielded enhanced inhibition and lower cytotoxicity. The anti-tumor promoter activity suggested by these results was further investigated in an in vivo study, which demonstrated that Shi-un-kou markedly inhibited TPA-induced skin tumor formation in mice. Registry Numbers: 16561-29-8 (Tetradecanoylphorbol Acetate) 57-97-6 (9,10-Dimethyl-1,2-benzanthracene) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€