Li J, Liang N, Mo L, Zhang X, He C
Institute of Medical Biochemistry, Guangdong Medical College, Zhanjiang 524023.
Yao Xue Xue Bao. 1998 Sep;33(9):641-4.
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 IC50 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 microgram.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 alpha, beta-methylene cyclopentanone moiety, and the site and number of the hydroxy groups affect the cytotoxicity of these agents significantly.
从中国传统草药半边旗（Pteris semipinnata L.，PsL）中分离出抗肿瘤成分，并采用四氮唑盐（MTT）法进行筛选。研究了它们在体外对几种人类肿瘤细胞系的细胞毒性作用。化合物5F、6F、A以及PsL的乙醇提取物（PSE）对五种细胞系显示出较强的细胞毒性：人肝腺癌细胞系（HePG II）、人肺腺癌细胞系（SPC-A-1）、人胃腺癌细胞系（MGC-803）、低分化人鼻咽癌细胞（CNE-2Z）和人肝腺癌细胞系（BEL-7402），且呈剂量依赖性；化合物6F活性最强，对上述五种细胞系处理72小时后的IC50分别为0.343±0.003、0.115±0.022、0.590±0.032、0.328±0.066和0.221±0.058微克·毫升-1。化合物A和5F活性较低；未检测到化合物4F和B对这五种细胞系的细胞毒性。结构与活性关系分析表明，结构中的抗肿瘤活性部分是α，β-亚甲基环戊酮部分，羟基的位置和数量对这些药物的细胞毒性有显著影响。
