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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。
Objective To search for natural DNA topoisomerase I inhibitors in Camptotheca acuminata with biological activity as a guide. Methods 14 compounds were isolated and identified from Camptotheca acuminata using various chromatographic and spectroscopic methods. Results The structures were identified as camptothecin (1), inositol (2), hipuside (3), 3’-methyl-3,4O, O-methylene ellagic acid 4’OβD glucopyranoside (4 ), 2 Oxygen 1,2 dihydroquinoline 4 acid (5), Brucine acid (6), 4-methyl 1,2 cyclohexane dimethanol (7), strictosamide (8), sapogenin ( 9), acetamide (10), chlorogenic acid (11), strictosidinicacid (12), 1 caffeoylquinic acid (13) and 10 hydroxycamptothecin (14). Conclusion Compound 413 was isolated from the plant for the first time. The nuclear magnetic data of compound 4 was incorrect in the literature [5]. This article was re-attributed. In vitro activity test showed that Compound 1 had a moderate inhibitory effect on DNA topoisomerase I, and Compounds 4, 14 had a strong inhibitory effect on DNA topoisomerase I.