苦味叶下珠素，一种天然存在的裂环烯醚萜苷，也是一种新发现的来自杜氏利什曼原虫的拓扑异构酶I抑制剂。
Amarogentin, a naturally occurring secoiridoid glycoside and a newly recognized inhibitor of topoisomerase I from Leishmania donovani.
作者信息
Ray S, Majumder H K, Chakravarty A K, Mukhopadhyay S, Gil R R, Cordell G A
机构信息
Indian Institute of Chemical Biology, Calcutta, India.
出版信息
J Nat Prod. 1996 Jan;59(1):27-9. doi: 10.1021/np960018g.
PMID:8984149
Abstract
A MeOH extract of Swertia chirata found to inhibit the catalytic activity of topoisomerase I of Leishmania donovani was subjected to fractionation to yield three secoiridoid glycosides: amarogentin (1), amaroswerin (2), and sweroside (3). Amarogentin is a potent inhibitor of type I DNA topoisomerase from Leishmania and exerts its effect by interaction with the enzyme, preventing binary complex formation.
摘要
已发现印度獐牙菜的甲醇提取物可抑制杜氏利什曼原虫拓扑异构酶I的催化活性，对其进行分离得到三种裂环烯醚萜苷：苦味质（1）、苦獐牙菜苷（2）和獐牙菜苷（3）。苦味质是杜氏利什曼原虫I型DNA拓扑异构酶的有效抑制剂，通过与该酶相互作用发挥作用，阻止二元复合物的形成。
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