Phytochemistry and preliminary biological evaluation of Cyathostemma argenteum, a Malaysian plant used traditionally for the treatment of breast cancer

• Published in: Phytotherapy research 2004-07, Vol.18 (7), p.507-510
• Main Authors: Khamis, S, Bibby, M.C, Brown, J.E, Cooper, P.A, Scowen, I, Wright, C.W
• Format: Article
• Language: English
• Subjects: alkaloids; Animals; Annonaceae; Antineoplastic Agents, Phytogenic - administration & dosage; Antineoplastic Agents, Phytogenic - pharmacology; Antineoplastic Agents, Phytogenic - therapeutic use; Artemia - drug effects; Artemia salina; Biological and medical sciences; breast cancer; breast neoplasms; Breast Neoplasms - drug therapy; Breast Neoplasms - pathology; Cell Line, Tumor - drug effects; cell lines; Cyathostemma argenteum; Cyathostemma argentum; cytotoxicity; cytotoxicity tests; Female; flavanones; General pharmacology; Humans; Inhibitory Concentration 50; Malaysia; Medical sciences; medicinal plants; Medicine, Traditional; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; phytochemicals; Phytotherapy; Plant Extracts - administration & dosage; Plant Extracts - pharmacology; Plant Extracts - therapeutic use; Plant Oils - administration & dosage; Plant Oils - pharmacology; Plant Oils - therapeutic use; Plant Roots; roots; traditional medicine
• ISSN: 0951-418X; 1099-1573
• DOI: 10.1002/ptr.1318

Bioassay guided fractionation of the roots of Cyathostemma argenteum using the brine shrimp resulted in the isolation of two uncommon flavanones, 2,5‐dihydroxy‐7‐methoxyflavanone 1 and 2,5‐dihydroxy‐6,7‐dimethoxyflavanone 2 while the stem bark yielded the related compounds 5‐hydroxy‐7‐methoxyflavone 3 and 5‐hydroxy‐6,7‐dimethoxyflavone 4. The alkaloids liriodenine 5 and discretamine 6 as well as benzyl benzoate 7 were isolated from the roots and 6 was also isolated from the stembark. In cytotoxicity tests using four human breast cancer cell lines, 1 and 2 were weakly toxic to MCF‐7 cells (IC50 = 19.6 and 19.0 µm, respectively) but showed little activity against MCF‐7 cells resistant to doxorubicin or against two oestrogen receptor‐deficient cell lines. Compound 5, but not 6 and 7, was moderately cytotoxic against all four cell lines. These results are discussed in the context of the traditional use of C. argenteum in the treatment of breast cancer. Copyright © 2004 John Wiley & Sons, Ltd.