€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CARCINOGENESIS***** Poginsky B Westendorf J Blomeke B Marquardt H Hewer A Grover PL Phillips DH Evaluation of DNA-binding activity of hydroxyanthraquinones occurring in Rubia tinctorum L. In: Carcinogenesis (1991 Jul) 12(7):1265-71 ISSN: 0143-3334 The naturally-occurring anthraquinones (AQs), alizarin (1,2- dihydroxyanthraquinone) and lucidin (1,3-dihydroxy-2- hydroxymethylanthraquinone), were incubated with DNA in the presence of S9 mix. The isolated DNA was analysed by 32P-postlabelling for the presence of aromatic adducts. Only lucidin formed up to five different DNA adducts in the range from 0.995 to 3.05 adducts/10(8) nucleotides. Lucidin was also incubated with polynucleotides poly[d(A- T)] and polydG*polydC in the presence of S9 mix. Analysis of polydG*polydC revealed a similar adduct pattern to that obtained with lucidin-modified DNA. Alizarin, lucidin, a glycoside mixture containing alizarinprimeveroside and lucidinprimeveroside, and Rubia Teep (a herbal drug made from Rubia tinctorum containing lucidin) were incubated with primary rat hepatocytes for 24 h and the isolated DNA was analysed by 32P-postlabelling. Lucidin, the glycoside mixture and Rubia Teep gave rise to DNA adducts, but alizarin did not. Male Parkes mice were treated orally for 4 days with alizarin (10 mg/d), lucidin (2 mg/d), the glycoside mixture (20 mg/d) or Rubia Teep (1/2 tablet/d) and DNA was isolated from liver, kidney, duodenum and colon. Analysis by 32P-postlabelling revealed that lucidin, the glycoside mixture and Rubia Teep, but not alizarin, formed DNA adducts in all the tissues examined but that the adduct patterns were organ-specific. Registry Numbers: 478-08-0 (lucidin) 72-48-0 (alizarin) 9007-49-2 (DNA) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CELL BIOLOGY AND TOXICOLOGY***** Westendorf J Poginsky B Marquardt H Groth G Marquardt H The genotoxicity of lucidin, a natural component of Rubia tinctorum L., and lucidinethylether, a component of ethanolic Rubia extracts. In: Cell Biol Toxicol (1988 Jun) 4(2):225-39 ISSN: 0742-2091 The genotoxic activity of lucidin (1,3-dihydroxy-2-hydroxymethyl-9,10- anthraquinone), a natural component of Rubia tinctorum L., was tested in a battery of short-term tests. The compound was mutagenic in five Salmonella typhimurium strains without metabolic activation, but the mutagenicity was increased after addition of rat liver S9 mix. In V79 cells, lucidin was mutagenic at the hypoxanthine-guanine phosphoribosyl transferase gene locus and active at inducing DNA single-strand breaks and DNA-protein cross-links as assayed by the alkaline elution method. Lucidin also induced DNA repair synthesis in primary rat hepatocytes and transformed C3H/M2-mouse fibroblasts in culture. We also investigated lucidinethylether, which is formed from lucidin by extraction of madder roots with boiling ethanol. This compound was also mutagenic in Salmonella, but only after addition of rat liver S9 mix. Lucidinethylether was weakly mutagenic to V79 cells which were cocultivated with rat hepatocytes. The compound did not induce DNA repair synthesis in hepatocytes from untreated rats, but positive results were obtained when hepatocytes from rats pretreated with phenobarbital were used. We conclude that lucidin and its derivatives are genotoxic. Registry Numbers: 17526-17-9 (lucidin ethyl ether) 478-08-0 (lucidin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CESKA A SLOVENSKA FARMACIE***** Nova D [Risk of adverse effects of drugs] Riziko nezadoucich ucink~u nekterych drog. In: Ceska Slov Farm (1996 Sep) 45(5):246-9 ISSN: 1210-7816 (Published in Czech) With regard to the demonstrated adverse effects of some vegetable drugs (Rubia tinctorum L., pyrrolizidine alkaloids), or serious suspicions of adverse effects (drugs containing hydroxyanthracene derivatives), the German Federal Health Authority (BGA) has taken the following measures: the drug Rubiae tinctorum radix and the preparations manufactured from it have been withdrawn from circulation, and in the drugs and preparations containing pyrrolizidine alkaloids and hydroxyanthracene derivatives the manner of use, dosing and information for the customer have been modified. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CHEMICAL AND PHARMACEUTICAL BULLETIN***** Itokawa H Morita H Takeya K Solution forms of an antitumor cyclic hexapeptide, RA-VII in dimethyl sulfoxide-d6 from nuclear magnetic resonance studies. In: Chem Pharm Bull (Tokyo) (1992 Apr) 40(4):1050-2 ISSN: 0009-2363 Using high-resolution proton nuclear magnetic resonance (1H-NMR) and carbon-13 nuclear magnetic resonance (13C-NMR) experiments, we have assigned three discernible configurational isomers observed in dimethyl sulfoxide-d6 (DMSO-d6) for an antitumor cyclic hexapeptide, RA-VII isolated from Rubia cordifolia. The largest isomer, amounting to 64%, has been assigned as conformer A with only a cis configuration between Tyr-5 and Tyr-6. The second configurational isomer, accounting for 32%, has adopted cis configurations between both Tyr-5 and Tyr-6 and between Ala-2 and Tyr-3. The third isomer, amounting to 4%, was determined to have cis configurations for all of the three N-methyl amide bonds. Registry Numbers: 67-68-5 (Dimethyl Sulfoxide) 7782-39-0 (Deuterium) 86229-97-2 (RA VII) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Itokawa H Ibraheim ZZ Qiao YF Takeya K Anthraquinones, naphthohydroquinones and naphthohydroquinone dimers from Rubia cordifolia and their cytotoxic activity. In: Chem Pharm Bull (Tokyo) (1993 Oct) 41(10):1869-72 ISSN: 0009-2363 Further investigation of the roots of Rubia cordifolia resulted in the isolation of four new naphthohydroquinones and two naphthohydroquinone dimers, and one known naphthohydroquinone, one naphthoquinone, two anthraquinones and one naphthohydroquinone dimer. The structures of these compounds were established by various chemical and spectroscopic methods including two dimensional NMR techniques. Also, the isolated compounds were submitted to a bio- assay for cytotoxic and antitumor activity. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Kawasaki Y Goda Y Yoshihira K The mutagenic constituents of Rubia tinctorum. In: Chem Pharm Bull (Tokyo) (1992 Jun) 40(6):1504-9 ISSN: 0009-2363 Twenty compounds were isolated from the roots of Rubia tinctorum which are used as a commercial source of madder color. Among these compounds, mollugin (1), 1-hydroxy-2-methylanthraquinone (2), 2- ethoxymethylanthraquinone(11), rubiadin (13), 1,3- dihydroxyanthraqunone (14), 7-hydroxy-2-methylanthraquinone (16), lucidin (17), 1-methoxymethylanthraquinone (18) and lucidin-3-O- primeveroside (19) showed mutagenicity with Salmonella typhimurium TA 100 and/or TA 98. Since the mutagenic compounds isolated are anthraquinone derivatives with the exception of compound 1, structure- mutagenicity relationships of the anthraquinones were also studied. The results suggested that the greatest activity is exhibited by 1,3- dihydroxyanthraquinones possessing methyl or hydroxylmethyl group on carbon 2. Registry Numbers: 117-02-2 (rubiadin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Morita H Yamamiya T Takeya K Itokawa H New antitumor bicyclic hexapeptides, RA-XI, -XII, -XIII and -XIV from Rubia cordifolia. In: Chem Pharm Bull (Tokyo) (1992 May) 40(5):1352-4 ISSN: 0009-2363 Four new bicyclic hexapeptides, named as RA-XI, -XII, XIII and -XIV were isolated from Rubia cordifolia and showed potent antitumor activities against P-388. The structures were elucidated from spectroscopic and chemical evidences. RA-XII, XIII and -XIV were proved to be unique bicyclic hexapeptidic glucosides. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CHEMOTHERAPY***** Adwankar MK Chitnis MP In vivo anti-cancer activity of RC-18: a plant isolate from Rubia cordifolia, Linn. against a spectrum of experimental tumour models. In: Chemotherapy (1982) 28(4):291-3 ISSN: 0009-3157 Anti-tumour activity of RC-18, a pure isolate from Rubia cordifolia was repeatedly tested in different sets of experiments on a spectrum of experimental murine tumours, viz. P388, L1210, L5178Y, B16 melanoma, Lewis lung carcinoma and sarcoma-180. RC-18 exhibited significant increase in life span of ascites leukaemia P388, L1210, L5178Y and a solid tumour B16 melanoma. However, it failed to show any inhibitory effect on solid tumours, Lewis lung carcinoma and sarcoma 180. Promising results against a spectrum of experimental tumours suggest that RC-18 may lead to the development of a potential anti-cancer agent. Registry Numbers: 82197-74-8 (RC-18) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Adwankar MK Chitnis MP IN VIVO ANTI-CANCER ACTIVITY OF RC-18. A PLANT ISOLATE FROM RUBIA CORDIFOLIA LINN. AGAINST A SPECTRUM OF EXPERIMENTAL TUMOUR MODELS In: Chemotherapy (1982) 28(4):291-293 ISSN: 0009-3157 Anti-tumor activity of RC-18, a pure isolate from Rubia cordifolia, was repeatedly tested in different sets of experiments on a spectrum of experimental murine tumors, viz P388, L1210, L5178Y, B16 melanoma, Lewis lung carcinoma and sarcoma-180. RC-18 exhibited significant increase in life span of ascites leukemia P388, L1210, L5178Y and a solid tumor B16 melanoma. However, it failed to show any inhibitory effect on solid tumors, Lewis lung carcinoma and sarcoma 180. Promising results against a spectrum of experimental tumors suggest that RC-18 may lead to the development of a potential anti-cancer agent. (Author abstract) (8 Refs) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ **CHUNG-KUO CHUNG YAO TSA CHIH CHINA JOURNAL OF CHINESE MATERIA MEDICA* Lin XY Li XL Yang Y [Determination of trace elements in several hemostatic medicinal plants and their boiling water extracts] In: Chung Kuo Chung Yao Tsa Chih (1993 Apr) 18(4):223-4, 254-5 ISSN: 1001-5302 (Published in Chinese) The experimental results indicate that the amounts of Cu, Zn, Fe and Mn in Rubia cordifolia and Agrimonia pilosa var. japonica are very small in boiling water extracts (only 6%). But after digestion they may rise to 30%. It was found that the amounts of four trace elements decreased with the increase of extracting time, but the ratios of Mn/Zn and Zn/Cu were almost the same. Registry Numbers: 7439-89-6 (Iron) 7439-96-5 (Manganese) 7440-50-8 (Copper) 7440-66-6 (Zinc) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****INDIAN JOURNAL OF EXPERIMENTAL BIOLOGY***** Adwankar MK Chitnis MP Khandalekar DD Bhadsavale CG ANTI-CANCER ACTIVITY OF THE EXTRACTS OF RUBIA CORDIFOLIA LINN In: Indian J Exp Biol (1980) 18(1):102 ISSN: 0019-5189 The anti-cancer activity of extracts of Rubia cordifolia, tested against the P388 tumor system in BDF1 mice, compared well with that of the positive control, 5-fluorouracil. (1 Ref) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Pandey S Sharma M Chaturvedi P Tripathi YB Protective effect of Rubia cordifolia on lipid peroxide formation in isolated rat liver homogenate. In: Indian J Exp Biol (1994 Mar) 32(3):180-3 ISSN: 0019-5189 Rubia cordifolia Linn. (Rubiaceae) is an important component of the ayurvedic system of medicine. It has a variety of uses such as blood purifier, immunomodulant, antiinflammatory and anti-PAF. In this report the anti-peroxidative property of the solvent free alcoholic extract of R. cordifolia has been studied in rat liver homogenate. It prevents the cumene hydroperoxide induced malondialdehyde formation in the dose and time dependent manner. This effect is accompanied by the maintained reduced glutathione level even in the presence of above toxin. Registry Numbers: 542-78-9 (Malondialdehyde) 70-18-8 (Glutathione) 80-15-9 (cumene hydroperoxide) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Tripathi YB Pandey S Shukla SD Anti-platelet activating factor property of Rubia cordifolia Linn. In: Indian J Exp Biol (1993 Jun) 31(6):533-5 ISSN: 0019-5189 Rubia cordifolia is clinically used for the purification of blood by the physicians of the Indian System of Medicine. For the first time, the effect of the partially purified fraction of this whole plant has been studied on rabbit platelets. It inhibits the platelet aggregation induced by PAF (platelet activating factor) but not thrombin. It also inhibits the binding of 3H-PAF to the platelets in the dose-dependent manner. Thus it appears that R. cordifolia inhibits action of PAF at its receptor level either by it's blocking or by desensitization. Registry Numbers: 64-17-5 (Alcohol, Ethyl) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF NATURAL PRODUCTS***** Ho LK Don MJ Chen HC Yeh SF Chen JM Inhibition of hepatitis B surface antigen secretion on human hepatoma cells. Components from Rubia cordifolia. In: J Nat Prod (1996 Mar) 59(3):330-3 ISSN: 0163-3864 The antiviral activity in the roots of Rubia cordifolia was examined, and three naphthohydroquinones, furomollugin (1), mollugin (2), and rubilactone (3), were isolated from it. Compounds 1 and 2 strongly suppressed the secretion of hepatitis B surface antigen (HBsAg), both with IC50 = 2.0 micrograms/mL, in human hepatoma Hep3B cells while having little effect on the viability of the cells. Evaluation of structurally related derivatives of 1 and 2 revealed that a 6-hydroxy group and a pyran or furan ring contribute to this suppressive effect. Registry Numbers: 142182-54-5 (rubilactone) 55481-88-4 (rubimaillin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Chung MI Jou SJ Cheng TH Lin CN Ko FN Teng CM Antiplatelet constituents of formosan Rubia akane. In: J Nat Prod (1994 Feb) 57(2):313-6 ISSN: 0163-3864 A known steroid, in addition to triterpenoids, anthraquinones, naphthalenes and a new anthraquinone glycoside, xanthopurpurin 3-O- beta-D-glucoside, were isolated from the roots of Rubia akane grown in Taiwan. Mollugin, a naphthohydroquinone, showed strong inhibition of arachidonic acid (AA)-induced and collagen-induced platelet aggregation. In contrast, 2-methyl-1,3,6-trihydroxyl-9,10- anthraquinone, xanthopurpurin 3-O-beta-D-glucoside, and xanthopurpurin showed mainly strong inhibition of collagen-induced platelet aggregation. Registry Numbers: EC 3.4.21.5 (Thrombin) 506-32-1 (Arachidonic Acid) 9007-34-5 (Collagen) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JPMA. JOURNAL OF THE PAKISTAN MEDICAL ASSOCIATION***** Gilani AH Janbaz KH Zaman M Lateef A Suria A Ahmed HR Possible presence of calcium channel blocker(s) in Rubia cordifolia: an indigenous medicinal plant. In: JPMA J Pak Med Assoc (1994 Apr) 44(4):82-5 ISSN: 0030-9982 Crude extract of Rubia cordifolia (RC) was tested in isolated tissue preparations for its possible calcium channel antagonistic activity. RC suppressed the spontaneous contractions of guinea-pig atria, rabbit jejunum and rat uterus in a concentration dependent manner (0.1-3 mg/ml). In rabbit aorta, it inhibited norepinephrine (10 microM) and KCl (80 mM) induced contractions. Replacement of physiological salt solution with calcium free solution abolished the spontaneous movements of rabbit jejunum. However, addition of calcium (25 micrograms/ml) in the tissue bath restored the spontaneous movements. When the tissues were pretreated with plant extract (1 mg/ml) or verapamil (0.5 microgram/ml), addition of calcium failed to restore spontaneous contractions. These results indicate that the plant extract exhibits spasmolytic activity similar to that of verapamil suggestive of presence of calcium channel blocker like constituent(s) in this plant. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****MUTATION RESEARCH***** Blomeke B Poginsky B Schmutte C Marquardt H Westendorf J Formation of genotoxic metabolites from anthraquinone glycosides, present in Rubia tinctorum L. In: Mutat Res (1992 Feb) 265(2):263-72 ISSN: 0027-5107 Rubia tinctorum L., a medicinal plant used for the treatment of kidney and bladder stones, contains a characteristic spectrum of 9,10- anthraquinone derivatives, which are substituted in only one of the aromatic benzo rings. The majority of the anthraquinones present in the plant itself or in plant extracts are glycosides. We investigated the metabolism of two such glycosides, alizarinprimeveroside (AlP) and lucidinprimeveroside (LuP). AlP given orally to rats was metabolized to alizarin (Al) and 1-hydroxyanthraquinone (1-HA). The reductive cleavage of AlP was also observed after treatment of this compound with rat liver enzymes (S9) and NADPH. 1-HA has been reported to induce unscheduled DNA synthesis (UDS) in primary rat hepatocytes (PRH) and intestinal and liver tumors in rats after chronic treatment. The in vitro genotoxicity of 1-HA was confirmed by our present investigations. We also observed that the glycoside AlP was active at inducing UDS in PRH, but the compound was inactive in the Salmonella/microsome assay. Oral administration of LuP to rats resulted in the excretion of lucidin and rubiadin. When LuP was treated with rat liver extract and NADPH, the compound was reduced to rubiadinprimeveroside (RuP), which was hydrolyzed to rubiadin. We have recently shown that lucidin is highly genotoxic in a battery of short-term tests. We now report that rubiadin is also highly genotoxic in Salmonella typhimurium. However, in contrast to lucidin, it requires metabolic activation. In the UDS assay in PRH, rubiadin was even more potent than lucidin and equal to the positive control DMBA. In addition, the glycoside LuP is active in the Salmonella/microsome assay as well as in the UDS assay. The present work demonstrates that the uptake of the anthraquinone glycosides AlP and LuP leads to the rodent carcinogen 1-HA, and to the highly genotoxic compounds lucidin and rubiadin. This extends our previous studies and supports our suggestion that the therapeutic use of Rubia tinctorum may involve a carcinogenic risk. Registry Numbers: 117-02-2 (rubiadin) 129-43-1 (1-hydroxyanthraquinone) 152-84-1 (ruberythric acid) 29706-59-0 (lucidin 3-O-beta-primveroside) 478-08-0 (lucidin) 72-48-0 (alizarin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Yasui Y Takeda N Identification of a mutagenic substance, in Rubia tinctorum L. (madder) root, as lucidin. In: Mutat Res (1983 Sep) 121(3-4):185-90 ISSN: 0027-5107 Mutagenicity of the extract from Rubia tinctorum L. (madder) root was demonstrated on Salmonella typhimurium TA100 and TA98. The active substance wa purified and characterized by TLC, UV spectrum, IR spectrum, mass spectrum and [1H]NMR spectrum. All the mutagenic activity of the extract from the root of Rubia tinctorum L. was due to lucidin (1,3-dihydroxy,2-hydroxymethyl-9, 10-anthraquinone). Registry Numbers: 478-08-0 (lucidin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PHARMAZIE***** Berg W Hesse A Kraft R Herrmann M [Elucidation of the structure of new anthraquinone derivatives from Rubia tinctorum L. 1. 1,4-dihydroxy-2-ethoxymethylanthraquinone (Christofin)] Zur Strukturaufklarung von neuen Anthrachinon-derviaten aus Rubia tinctorum L. Teil 1: 1,4-Dihydroxy-2-athoxymethylanthrachinon (Christofin) In: Pharmazie (1974 Jul) 29(7):478-82 ISSN: 0031-7144 (Published in German) [No Abstract Available] €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PHYTOCHEMISTRY***** Takeya K Yamamiya T Morita H Itokawa H Two antitumour bicyclic hexapeptides from Rubia cordifolia. In: Phytochemistry (1993 Jun) 33(3):613-5 ISSN: 0031-9422 Two novel antitumour bicyclic hexapeptides, named RA-XV and -XVI, were isolated from Rubia cordifolia and their structures were characterized by spectroscopic and chemical means. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PROCEEDINGS / ANNUAL MEETING OF THE AMERICAN ASSOCIATION FOR***** Poginsky B Phillips D Westendorf J Blomeke B Marquardt H FORMATION OF DNA ADDUCTS BY THE HYDROXYANTHRAQUINONE LUCIDIN (MEETING ABSTRACT) In: Proc Annu Meet Am Assoc Cancer Res (1991) 32:A575 ISSN: 0197-016X Lucidin (1,3-dihydroxy-2-hydroxymethylanthraquinone) is the genotoxic principle of madder roots (Rubia tinctorum L). To investigate whether lucidin, indeed, interacts covalently with DNA, we incubated the compound (200 ug/ml) for 3 hr with DNA or polydG.polydC and S9 mix and examined the reisolated nucleic acids by 32P-postlabeling. Similar adduct patterns, containing up to 5 spots, were obtained on PEI-cellulose tlc with DNA or polydG.polydC. Formation of DNA adducts was also observed after treatment with lucidin (40 ug/ml) of primary rat hepatocytes in culture. Finally, DNA adducts were detected in liver, kidney, duodenum and colon of male Parkes mice that had been treated po for 4 days with lucidin (2 mg/day), its glycoside lucidinprimeveroside (10 mg/day) or Rubia Teep (1/2 tablet/day), a pharmaceutical preparation containing the two compounds. These results suggest that the therapeutic use of lucidin may constitute a carcinogenic risk. Registry Numbers: 25512-84-9 (poly(dG).poly(dC)) 9007-49-2 (DNA) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****TOXICOLOGY AND INDUSTRIAL HEALTH***** Ino N Tanaka T Okumura A Morishita Y Makita H Kato Y Nakamura M Mori H Acute and subacute toxicity tests of madder root, natural colorant extracted from madder (Rubia tinctorum), in (C57BL/6 X C3H)F1 mice. In: Toxicol Ind Health (1995 Jul-Aug) 11(4):449-58 ISSN: 0748-2337 As part of the safety assessment of madder root (MR), a food colorant extracted from madder (Rubia tinctorum), toxicity tests were undertaken using (C57BL/6 x C3H)F1 mice of both sexes. An acute toxicity test was performed by 14-day administration of MR dissolved in distilled water by gavage at doses of 0, 500, 2000, 3500, and 5000 mg/kg body weight to groups of each sex. One male mouse dosed at 5000 mg/kg body weight was dead before the end of the study, indicating that the maximum tolerated dose of MR was between 3500 and 5000 mg/kg body weight. A subacute toxicity test of MR was performed using 62 mice of each sex, mixing their diets with MR at concentrations of 0, 0.3, 0.6, 1.25, 2.5, and 5% for 90 days. All mice tolerated these doses of MR well. The body weight gains of either sex were not affected by the treatment. None of the mice treated with MR showed clinical signs of toxicity. Histopathological examinations showed retention cysts of the kidneys and epidermal vaginal cysts in a few of the treated or control mice. No hyperplastic, preneoplastic, and neoplastic lesions and no pathological findings of toxicity were found. These results suggest that dietary exposure of MR at these doses has no acute or subacute toxic effects on mice. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****YAO HSUEH HSUEH PAO [ACTA PHARMACEUTICA SINICA]***** Qiao YF Wang SX Wu LJ Li X Zhu TR [Studies on antibacterial constituents from the roots of Rubia cordifolia L.] In: Yao Hsueh Hsueh Pao (1990) 25(11):834-9 ISSN: 0513-4870 (Published in Chinese) Twelve compounds were isolated from the roots of Rubia cordifolia L.. Nine of them were established by chemical and spectroscopic methods to be alizarin (I),1-hydroxy-2-methyl-9,10-anthraquinone(II),1,3,6- trihydroxy-2-methyl- 9,10-anthra-quinone-3-O-(6'-O-acetyl)-alpha-L- rhamnosyl(1--- -2)-beta-D- glucoside(III),1,3,6-trihydroxy-2-methyl- 9,10-anthraqueinone-3-O-a lpha- L-rhamnosyl(1----2)-beta-D- glucoside(IV),1,3,6-trihydrozy-2- methyl-9,10- anthraquinone-3-O-(6'- O-acetyl)-beta-D-glucoside(V),2-carbomethyoxy++ +-3-prenyl- 1,4- naphthohydroquinone di-beta-D-glucoside(VI),rubimallin(VII),beta- sitosterol(VIII) and daucosterol(IX), among them, V is a nwe compound and IX was obtained from this genus for the first time, III, VI and VII showed certain antibacterial activities. Registry Numbers: 132367-98-7 (1,3,6-trihydroxy-2-methyl-9,10-anthraquinone-3-O-(6'-acetylglucoside)) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Wang SX Hua HM Wu LJ Li X Zhu TR [Studies on anthraquinones from the roots of rubia cordifolia l] In: Yao Hsueh Hsueh Pao (1992) 27(10):743-7 ISSN: 0513-4870 (Published in Chinese) Seven anthraquinones were isolated from the ethyl alcohol extracts of the roots of Rubia Cordifolia L. By means of spectrometric data combined with physico-chemical properties, six of them were identified as 2-methyl-1,3,6-trihydroxy-9,10-anthraquinone (I), 1- hydroxy-9,10-anthraquinone(II), 1,2,4-trihydroxy-9,10- anthrequinone(III), 2-methyl-1,3,6-trihydroxy-9,10-anthraquinone-3-O- beta-D-glucoside(IV), 1,2-dijhydroxy-9,10-anthraquinone-2-O-beta-D- xylosyl(1-->6)-beta-D -glucoside(V) and 1,3-dihydroxy-2- hydroxymethyl1-9,10-anthraquinone-3-O-beta-D- xylosyl(1-->6)-beta-D- glucoside(VI). VII is a new compound. Its structure was elucidated to be 2-methyl-1,3,6-trihydroxy-9,10-anthraquinone-3-O-beta-D-xylosyl(1-- >2)-b eta-D- (6'-O-acetyl)glucoside. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Hua HM Wang SX Wu LJ Li X Zhu TR [Studies on naphthoic acid esters from the roots of Rubia cordifolia L] In: Yao Hsueh Hsueh Pao (1992) 27(4):279-82 ISSN: 0513-4870 (Published in Chinese) Four naphthoic acid esters including a new compound were isolated from the roots of Rubia cordifolia L. The new one was named as rubilactone and its structure was elucidated as 3'-carbomethoxy-4'- hydroxy-naphtho[1',2'-2,3] pyran-6-one (I) based on the physicochemical properties and spectrometric analyses (UV, IR, MS, 1HNMR and 13CNMR). The other three were 3'-carbomethoxy-4'-hydroxy- naphtho [1',2'-2,3] furan (II), dihydromollugin (III) and 3- carbomethoxy-2-(3'-hydroxy)isopentyl-1,4-naphthohydroquinone-1-O - beta-D-glucoside (IV). Registry Numbers: 142182-54-5 (rubilactone) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€