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来自印度人参的具有胆碱酯酶抑制作用的睡茄内酯

Cholinesterase inhibiting withanolides from Withania somnifera.

作者信息

Choudhary Muhammad Iqbal, Yousuf Sammer, Nawaz Sarfraz Ahmad, Ahmed Shakil

机构信息

H.E.J. Research Institute of Chemistry, International Center for Chemical Sciences, University of Karachi, Karachi-75270, Pakistan.

出版信息

Chem Pharm Bull (Tokyo). 2004 Nov;52(11):1358-61. doi: 10.1248/cpb.52.1358.

DOI:10.1248/cpb.52.1358
PMID:15520512
Abstract

A total of two new (1, 2) and four known (3-6) withanolides were isolated from the whole plant of Withania somnifera. Their structures were elucidated on the basis of spectroscopic techniques and were characterized as 6alpha,7alpha-epoxy-3beta,5alpha,20beta-trihydroxy-1-oxowitha-24-enolide (1), 5beta,6beta-epoxy-4beta,17alpha,27-trihydroxy-1-oxowitha-2,24-dienolide (2), withaferin-A (3), 2,3-dihydrowithaferin-A (4), 6alpha,7alpha-epoxy-5alpha,20beta-dihydroxy-1-oxowitha-2,24-dienolide (5), and 5beta,6beta-epoxy-4beta-hydroxy-1-oxowitha-2,14,24-trienolide (6), respectively. Compounds 2, 3, 5, and 6 displayed inhibitory potential against butyrylcholinesterase, but only compounds 3, 4, and 6 were found to be active against acetylcholinesterase.

摘要

从睡茄全株中总共分离出两种新的(1, 2)和四种已知的(3 - 6)睡茄内酯。基于光谱技术阐明了它们的结构,并分别将其表征为6α,7α - 环氧 - 3β,5α,20β - 三羟基 - 1 - 氧代 - 威 - 24 - 烯醇内酯(1)、5β,6β - 环氧 - 4β,17α,27 - 三羟基 - 1 - 氧代 - 威 - 2,24 - 二烯醇内酯(2)、睡茄素A(3)、2,3 - 二氢睡茄素A(4)、6α,7α - 环氧 - 5α,20β - 二羟基 - 1 - 氧代 - 威 - 2,24 - 二烯醇内酯(5)和5β,6β - 环氧 - 4β - 羟基 - 1 - 氧代 - 威 - 2,14,24 - 三烯醇内酯(6)。化合物2、3、5和6对丁酰胆碱酯酶显示出抑制潜力,但仅发现化合物3、4和6对乙酰胆碱酯酶有活性。

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