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 CONSTITUENTSFROM PTERIS SEMIPINNATA L. IN VITRO AND THE ANALYSISOF THEIR STRUCTUREACTIVITY RELATIONSHIPS

作　　者：李金华[1] 梁念慈[1] 莫丽儿[1] 张晓[1] 何承伟[1] 

机构地区：[1]广东医学院医用生化研究所

出　　处：《药学学报》1998年第9期641-644,共4页Acta Pharmaceutica Sinica

基　　金：广东省科委重点科技攻关项目

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，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。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 (SPCA1), human gastric adenocarcinoma cell line (MGC803), human nasopharyngeal carcinoma cells in low differentiation (CNE2Z) and human liver adenocarcinoma cell line (BEL7402) in different degrees in a dosedependent manner; compound 6F was the most active one, whose IC50 after 72 h treatment for the above five cell lines were 0343±0003, 0115±0022, 0590±0032, 0328±0066 and 0221±0058 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,βmethylene cyclopentanone moiety, and the site and number of the hydroxy groups affect the cytotoxicity of these agents significantly.

关 键 词：半边旗 二萜 细胞毒 构效关系 中草药 药理学 

分 类 号：R285.5[医药卫生—中药学]