半边旗5种成分体外细胞毒活性比较及构效关系分析

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用多种人癌细胞株以MTT试验,体外筛选半边旗抗肿瘤活性成分。结果显示:化合物5F,6F,A及半边旗乙醇提取物PSE对5种人癌细胞均有不同程度的杀伤作用,且呈明显的剂量依赖关系。其中6F的活性最强,其次是A,5F,而化合物4F和B对5种细胞均无细胞毒活性。分析它们的构效关系可以推测,αβ亚甲基环戊酮结构是其活性部位,结构中羟基数目和位置的不同可以影响化合物的活性强度。 With a variety of human cancer cell lines to MTT test, in vitro selection Pentecost anti-tumor active ingredients. The results showed that compounds 5F, 6F, A and PSE ethanol extract PSE of 5 kinds of human cancer cells have different degrees of killing effect, and showed a significant dose-dependent manner. Among them, 6F was the most active, followed by A and 5F, while compounds 4F and B showed no cytotoxic activity on the 5 kinds of cells. Analysis of their structure-activity relationship can be speculated that α  β methylenecyclopentanone structure is the active site, the structure of the hydroxyl number and location of different compounds can affect the intensity of activity.
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