藤黄酸构效关系的研究(英文)  

Structure-activity Relationship of Gambogic Acid

作　　者：李念光[1] 尤启冬[1] 黄雪峰[1] 王进欣[1] 郭青龙[1] 陈晓光[2] 李燕[2] 李洪燕[2] 

机构地区：[1]江苏省肿瘤发生与干预重点实验室 [2]中国医学科学院中国协和医科大学药物研究所,北京100050

出　　处：《中国天然药物》2008年第1期37-42,共6页

基　　金：国家高技术研究发展计划("863"计划)资助项目(No.2002AA2Z3112)(No.2004AA2Z3A10);国家教育委员会重大科技攻关项目基金资助项目(No.2006-106094);江苏自然科学基金资助项目(No.BK2006149)~~

摘　　要：目的:研究藤黄酸的构效关系。方法:通过对天然产物藤黄酸的结构剖析,在去除复杂桥环结构的基础上,合成了色酮和?酮2个系列的化合物。并通过MTT法对其进行了初步的药理实验活性筛选。结果:这些具有平面环结构的小分子化合物的活性虽然比藤黄酸的活性要低,但是引入异戊烯基能显著提高其抗肿瘤活性。结论:藤黄酸结构中的异戊烯基和桥环结构对其抗肿瘤活性有着很重要的作用。AIM： To investigate the basic structure-activity relationship of gambogic acid. METHODS： Through simplifying the complex skeleton of the natural gambogic acid, two series of derivatives of chromone and xanthone were synthesized and examined for their antitumor activities against several cancer cells in vitro by MTT method. RESULTS： The cytotoxic activities of all these small compounds with planar ring were much less potent than those of the natural gambogic acid, and the introduction of prenyl to these small molecular compounds could increase their antitumor activities. CONCLUSION： The structure-activity relationship of synthesized compounds indicated that the prenyl groups and the bridgecore in gambogic acid were very important for keeping its antitumor activities.

关 键 词：藤黄酸 小分子化合物 抗肿瘤活性 

分 类 号：R284.3[医药卫生—中药学] R965.1[医药卫生—中医学]