Synthesis, Structure Elucidation and H+/K+-ATPase Inhibitory Activity of Bisabolangelone Reduction Derivatives

被引：13

作者：

Huang Nianyu ^{[1
]}

Chen Lei ^{[1
]}

Liao Zhaojiang ^{[1
]}

Fang Hubiao ^{[1
]}

Wang Junzhi ^{[1
]}

Zou Kun ^{[1
]}

机构：

[1] China Three Gorges Univ, Hubei Key Lab Nat Prod Res & Dev, Coll Chem & Life Sci, Yichang 443002, Hubei, Peoples R China

来源：

CHINESE JOURNAL OF CHEMISTRY | 2012年 / 30卷 / 01期

基金：

中国国家自然科学基金;

关键词：

bisabolangelone derivatives; reduction; structure elucidation; X-ray diffraction; H; K plus -ATPase; STRUCTURE-TOXICITY RELATIONSHIPS; CYTOPROTECTIVE ACTIVITY; SESQUITERPENES; LARVAE; PUMP; RATS;

D O I：

10.1002/cjoc.201100051

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Nine bisabolangelone reduction derivatives were synthesized and separated as potential anti-ulcer agent. Their structures were characterized by 2D NMR, IR, ESI-MS, elemental analysis and single-crystal X-ray diffraction analysis. Preliminarily H+/K+-ATPase activity evaluation indicated that all the target compounds had a certain inhibitory effect, and compounds II and IV exhibited the better inhibitory activity against H+/K+-ATPase than bisabolangelone and the commercial omeprazole with the IC50 of 23.21 and 65.32 mu mol/L, respectively. The initial structure-activity analysis suggested that the presence of carbonyl group in six-membered ring and double bond in side-chain seemed to be necessary to the activity.

引用

页码：71 / 76

页数：6

共 23 条

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[2]

Ahn YJ, 2008, Natural insecticide composition containing bisabolangelone and its derivative, Patent No. 2008011958

[3] Protection of gastric mucosal damage by Coriandrum sativum L. pretreatment in Wistar albino rats [J].