半边旗中二萜类化合物5F葡糖糖苷的分离鉴定及其抗肿瘤作用  

Isolation and identification of glycoside of compound 5F from Pteris semipinnata L. and their antitumor activity

作　　者：龚先玲[1] 陈志红[2] 梁念慈[1] 邓亦峰[1] George G.Chen 

机构地区：[1]广东医学院天然药物研究与开发重点实验室,广东湛江524023 [2]广东医学院分析中心,广东湛江524023 [3]香港中文大学外科系

出　　处：《中成药》2010年第2期257-260,共4页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金(3987099);粤港科技合作基金项目(GHP/022/06);湛江市科技计划项目(2008C10002)

摘　　要：目的:进一步研究半边旗的抗肿瘤活性成分。方法:运用反复硅胶柱层析的方法对半边旗中的化学成分进行分离纯化,以LC-MS及各种有机波谱法鉴定化学单体结构;并通过MTT法对分离鉴定的单体化合物及其苷元进行抗肿瘤活性研究。结果:从中分离鉴定1个二萜苷类化合物,为11β-hydroxy-15-oxo-ent-kaur-16-en-19-oic acid 19-β-D-glucoside(Ⅰ);化合物Ⅰ及其苷元5F均可抑制两种肿瘤细胞A549和CNE-2Z的生长,且它们对两种肿瘤细胞的抑制作用呈一定剂量依赖关系和时间依赖关系,化合物5F的活性强于化合物Ⅰ。结论:α,β不饱和环戊酮结构是其活性部位,5F中19位碳上的羧基与糖连接形成酯苷,成为化合物Ⅰ后,其抗肿瘤活性大大降低。AIM： To further study the antitumor constituents of Pteris semipinnata L. METHODS： Compounds were isolated by consecutive silica gel column chromatography. Their structures were elucidated by spectroscopic methods. Tumor cytotoxicity of the compounds was screened by using standard MTT method. RESULTS： One compound was isolated from Pteris semipinnata L. , and its structure was identified as 11 β-hydroxy-15-oxo-ent-kaur- 16-en-19-oic acid 19-β-D-glucoside（ Ⅰ ）. Compound Ⅰ and its aglycone 5F showed to have inhibitory action against two cancer cell lines A549 and CNE-2Z and showed the dose-response relation. But the antitumor activity of compound 5F was stronger than that of compound Ⅰ. CONCLUSION： The antitumor active site in the stucture is OL, β-methylene cyclopentanone moiety. Nineteen position carboxylic group in 5F has to be uncombined with sugar residue to form ester linkage（ compound Ⅰ ） otherwise antitumour activity is lost.

关 键 词：半边旗 抗肿瘤成分 二帖化合物 成分分析 

分 类 号：R284.1[医药卫生—中药学]