喜树中两个DNA拓扑异构酶Ⅰ抑制剂(英文)  

Two DNA Topoisomerase I Inhibitors from Camptotheca acuminata Decne.(Nyssaceae)

作　　者：尹锋[1] 胡立宏[1] 

机构地区：[1]中国科学院上海生命科学院上海药物所国家新药筛选中心,上海201203

出　　处：《中国天然药物》2005年第1期21-24,共4页

基　　金：国家自然科学基金资助项目(No.30371679)~~

摘　　要：目的以生物活性为向导在喜树中寻找天然的DNA拓扑异构酶I抑制剂。方法用各种层析方法和波谱方法从喜树中分离并鉴定了14个化合物。结果其结构分别鉴定为喜树碱(1),肌醇(2),喜果苷(3),3′甲基3,4O,O亚甲基鞣花酸4′OβD吡喃葡萄糖苷(4),2氧1,2二氢喹啉4酸(5),马钱子酸(6),4甲基1,2环己烷二甲醇(7),strictosamide(8),獐芽菜苷(9),乙酰胺(10),氯原酸(11),strictosidinicacid(12),1咖啡酰基奎宁酸(13)和10羟基喜树碱(14)。结论化合物413为首次从该植物中分得,化合物4的核磁数据在文献[5]中有误,本文对其进行了重新归属。经体外活性测试,化合物1对DNA拓扑异构酶Ⅰ有中等程度的抑制作用,化合物4,14对DNA拓扑异构酶I有强的抑制作用。AIM: To find natural DNA topoisomerase I inhibitors from Camptotheca acuminata Decne.(Nyssaceae)with bioassay-directed methods.METHOD: The chemical constituents were isolated by various column chromatographic methods.The structures of these compounds were elucidated by spectral analysis.RESULT:Fourteen compounds were obtained and the structures were identified as camptothecin(1),inositol(2),vincoside-lactam(3),3′-O-methyl-3,4-O,O-metheneellagic acid-4′-O-β-D-glucopynanoside(4),1,2-dihydro-2-oxoquinoline-4-carboxylic acid(5),loganic acid(6),4-methyl-1,2-cyclohexanedimethanol(7),strictosamide(8),sweroside(9),acetamide(10),chlorogenic acid(11),strictosidinic acid(12),1-caffeoylquinic acid(13)and 10-hydroxycamptothecin(14).CONCLUSION:Compounds 4-13 have not been reported previously from this plant.The NMR data of compound 4 in literature~[5] were re-assigned based on 2D-NMR.Among these isolated compounds,1 showed moderate activity against Topo I in vitro and 4,14 showed strong activity against Topo I in vitro.

关 键 词：喜树 珙桐科 化学成分 DNA拓扑异构酶Ⅰ 抑制剂 中药化学 

分 类 号：R284[医药卫生—中药学]