Methyl protogracillin (NSC-698792) 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 urinary bladder and renal tumor for centuries, in our previous studies. In order to systematically evaluate its potential anticancer activity, methyl protogracillin was tested for its cytotoxicity in vitro against 60 human cancer cell lines in the National Cancer Institute (NCI)'s anticancer drug screen. As a result, it was found that methyl protogracillin was cytotoxic against all the tested cell lines from leukemia and solid tumors in the NCI's human cancer panel; it showed particular selectivity against one colon cancer line (KM12), one central nervous system (CNS) cancer line (U251), two melanoma lines (MALME-3M and M14), two renal cancer lines (786-0 and UO-31) and one breast cancer line (MDA-MB-231) with GI50< or =2.0 microM. The selectivity between these seven most sensitive lines and the least sensitive line (CCRF-CEM) ranged from 26- to 56-fold. In the same cancer subpanel, selectivity more than 15-fold was observed between MDA-MB-231 and MCF-7, NCI-ADR-RES, BT-549 in breast cancer. From a general view of the mean graph, CNS cancer is the most sensitive subpanel, while ovarian cancer and renal cancer are the least sensitive subpanels. Based on an analysis of the COMPARE computer program with methyl protogracillin as a seed compound, no compounds in the NCI's anticancer drug screen database have similar cytotoxicity patterns (mean graph) to that of methyl protogracillin, indicating a potential novel mechanism of the anticancer action involved.

中文翻译：

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甲基原格拉西林（NSC-698792）：在美国国家癌症研究所的抗癌药物筛选小组中，针对60种人类癌细胞系的细胞毒性光谱。

甲基原香豆素（NSC-698792）是从山药薯the的根茎中分离得到的呋喃甾醇皂苷。hypoglauca（Dioscoreaceae），在我们以前的研究中，用于治疗宫颈癌，膀胱癌和肾肿瘤的中草药已有数百年历史。为了系统地评估其潜在的抗癌活性，在美国国家癌症研究所（NCI）的抗癌药物筛选中，对甲基protogracillin在体外对60种人类癌细胞系的细胞毒性进行了测试。结果发现，在NCI的人类癌症研究小组中，甲基原香茅素对所有测试的白血病和实体瘤细胞系均具有细胞毒性。它显示出对一种结肠癌系（KM12），一种中枢神经系统（CNS）系（U251）的选择性，两条GI50 <或= 2.0 microM的黑色素瘤系（MALME-3M和M14），两条肾癌系（786-0和UO-31）和一条乳腺癌系（MDA-MB-231）。这七个最敏感线和最不敏感线（CCRF-CEM）之间的选择性范围为26倍至56倍。在同一癌症亚组中，乳腺癌中MDA-MB-231与MCF-7，NCI-ADR-RES，BT-549之间的选择性超过15倍。从平均值图的一般角度来看，CNS癌症是最敏感的子面板，而卵巢癌和肾癌是最不敏感的子面板。根据对COMPARE计算机程序的分析，该程序以甲基原禾草素为种子化合物，因此NCI的抗癌药物筛选数据库中没有化合物具有与甲基原禾草素相似的细胞毒性模式（均值图），