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首页> 外文期刊>Journal of natural products >Cytotoxic activities of hypocretenolides from Leontodon hispidus.
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Cytotoxic activities of hypocretenolides from Leontodon hispidus.

机译：雷公藤的次降丁烯内酯的细胞毒活性。

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The hypocretenolides are a small group of sesquiterpene lactones with an unusual ring structure and are constituents of several species from the tribe Lactuceae of the family Asteraceae. In the present communication we report on the cytotoxic effects of three hypocretenolides (1-3) from Leontodon hispidus on: (a) eight solid-tumor cell lines (A431, HEP2, MCF7, OVCAR3, SK28, SK37, SW872, ZR75-1), tested by a (3)H-thymidine incorporation assay; (b) two different leukemia cell lines (GTB, HL60), measured by a MTT assay; and (c) CD34(+) bone-marrow cells, assessed by scoring the number of colonies derived from primitive and late erythroid progenitors (BFU-E and CFU-E) as well as from granulocytic/macrophagic progenitor cells (CFU-GM). The aglycon 14-hydroxyhypocretenolide (1) exhibited pronounced activities, although its beta-D-glucoside (2) showed no activity, even at the highest concentration tested (2 microM). 14-Hydroxyhypocretenolide-beta-D-glucoside-4',14' '-hydroxyhypocretenoate (3), the ester of the glucoside esterified with the open-chain form of the aglycon, was the most potently cytotoxic substance and proved to be even more active than the positive-control substance helenalin.
机译：次降丁烯内酯是一小组具有不同寻常的环结构的倍半萜烯内酯，并且是菊科（Asteraceae）的乳杆菌科的几个物种的组成部分。在本通讯中，我们报道了来自Leontodon hispidus的三种降胆固醇药（1-3）对以下细胞的细胞毒性作用：（a）八种实体肿瘤细胞系（A431，HEP2，MCF7，OVCAR3，SK28，SK37，SW872，ZR75-1 ），通过（3）H-胸苷掺入试验进行测试; （b）通过MTT测定法测量的两种不同的白血病细胞系（GTB，HL60）; （c）CD34（+）骨髓细胞，通过对原始和晚期红系祖细胞（BFU-E和CFU-E）以及粒细胞/巨噬细胞祖细胞（CFU-GM）衍生的集落数量进行评分来评估。糖苷配基14-羟基降丁烯内酯（1）表现出明显的活性，尽管其β-D-葡萄糖苷（2）即使在最高测试浓度（2 microM）下也没有表现出活性。 14-羟基低聚丁烯内酯-β-D-葡萄糖苷-4'，14'-羟基低聚丁烯酸酯（3）是糖苷的酯，被糖苷配基的开链形式酯化，是最强的细胞毒性物质，被证明具有更大的细胞毒性。活性比阳性对照物质Helenalin强。

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