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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.

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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