Hu Ke, Yao Xinsheng
Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, State University of New York at Buffalo, 539 Hochstetter Hall, Buffalo, NY 14260, USA.
Cancer Invest. 2003 Jun;21(3):389-93. doi: 10.1081/cnv-120018230.
Methyl protodioscin (NSC-698790) was a furostanol saponin isolated from the rhizome of Dioscorea collettii var. hypoglauca (Dioscoreaceae), a Chinese herbal remedy for the treatment of cervical carcinoma, carcinoma of the urinary bladder, and renal tumors for centuries. To systematically evaluate its potential anticancer activity, methyl protodioscin was tested cytotoxicity in vitro against human cancer cell lines by the NCI's (National Cancer Institute) anticancer drug screen. As a result, methyl protodioscin showed strong cytotoxicity against most cell lines from solid tumors with GI50 < or = 10.0 microM, especially selectively against one colon cancer line (HCT-15) and one breast cancer line (MDA-MB-435) with GI50 < 2.0 microM but moderate cytotoxicity was shown against leukemia cell lines with GI50 10-30 microM. The data are consistent with the fact that the rhizome of D. collettii var. hypoglauca has been employed for the treatment of solid tumors rather than leukemia in China for centuries. Based on an analysis using the COMPARE computer program with methyl protodioscin as a seed compound, no compounds in the NCI's anticancer drug screen database have cytotoxicity patterns similar to those of methyl protodioscin, indicating a potential novel mechanism of anticancer action.
甲基原薯蓣皂苷（NSC - 698790）是一种呋甾烷醇皂苷，从粉背薯蓣（薯蓣科）的根茎中分离得到，几个世纪以来，它一直作为一种中草药用于治疗宫颈癌、膀胱癌和肾肿瘤。为了系统地评估其潜在的抗癌活性，通过美国国立癌症研究所（NCI）的抗癌药物筛选，对甲基原薯蓣皂苷在体外针对人癌细胞系的细胞毒性进行了测试。结果显示，甲基原薯蓣皂苷对大多数实体瘤细胞系具有较强的细胞毒性，其半数生长抑制浓度（GI50）≤10.0微摩尔，尤其对一种结肠癌细胞系（HCT - 15）和一种乳腺癌细胞系（MDA - MB - 435）具有选择性，其GI50＜2.0微摩尔，但对白血病细胞系的细胞毒性中等，GI50为10 - 30微摩尔。这些数据与粉背薯蓣根茎在中国几个世纪以来一直用于治疗实体瘤而非白血病这一事实相符。基于使用COMPARE计算机程序以甲基原薯蓣皂苷作为种子化合物进行的分析，NCI抗癌药物筛选数据库中没有化合物具有与甲基原薯蓣皂苷相似的细胞毒性模式，这表明其抗癌作用可能存在新机制。
