节点文献
半边旗5种成分体外细胞毒活性比较及构效关系分析
COMPARISON OF THE CYTOTOXICITY OF FIVE CONSTITUENTSFROM PTERIS SEMIPINNATA L. IN VITRO AND THE ANALYSISOF THEIR STRUCTUREACTIVITY RELATIONSHIPS
【摘要】 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,αβ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。
【Abstract】 The antitumor constituents were isolated from Pteris semipinnata L. (PsL), a Chinese traditional herb, and screened using tetrazolium salt (MTT) method. Their cytotoxic effects in vitro on several human tumor cell lines were studied. Compounds 5F, 6F, A and the ethanolic extract of PsL (PSE) were shown to have strong cytotoxicity against five cell lines: human liver adenocarcinoma cell line (HePG II), human lung adenocarcinom a cell line (SPCA1), human gastric adenocarcinoma cell line (MGC803), human nasopharyngeal carcinoma cells in low differentiation (CNE2Z) and human liver adenocarcinoma cell line (BEL7402) in different degrees in a dosedependent manner; compound 6F was the most active one, whose IC50 after 72 h treatment for the above five cell lines were 0343±0003, 0115±0022, 0590±0032, 0328±0066 and 0221±0058 μg·ml-1, respectively. Compounds A and 5F were less active; no cytotoxicity of compounds 4F and B were detected on the five cell lines. Analysis of the relationship between structure and activity revealed that the antitumor activity portion in the structure is the α,βmethylene cyclopentanone moiety, and the site and number of the hydroxy groups affect the cytotoxicity of these agents significantly.
【Key words】 Pteris semipinnata L.; Diterpenoids; Cytotoxicity; Structureactivity relationship;
- 【文献出处】 药学学报 ,ACTA PHARMACEUTICA SINICA , 编辑部邮箱 ,1998年09期
- 【分类号】R965
- 【被引频次】73
- 【下载频次】258