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海绵胺类,即海洋海绵生物碱,作为抗休眠分枝杆菌物质。

Aaptamines, marine spongean alkaloids, as anti-dormant mycobacterial substances.

作者信息

Arai Masayoshi, Han Chisu, Yamano Yoshi, Setiawan Andi, Kobayashi Motomasa

机构信息

Graduate School of Pharmaceutical Sciences, Osaka University, Yamada-oka 1-6, Suita, Osaka, 565-0871, Japan,

出版信息

J Nat Med. 2014 Apr;68(2):372-6. doi: 10.1007/s11418-013-0811-y. Epub 2014 Jan 12.

Abstract

A new aaptamine class alkaloid, designated 2-methoxy-3-oxoaaptamine (1), together with seven known aaptamines (2-8) were isolated from a marine sponge of Aaptos sp. as anti-mycobacterial substances against active and dormant bacilli. The chemical structure of 1 was determined on the basis of spectroscopic analysis. Compound 1 was anti-mycobacterial against Mycobacterium smegmatis in both active growing and dormancy-inducing hypoxic conditions with a minimum inhibitory concentration (MIC) of 6.25 μg/ml, and compounds 2, 5, 6, and 7 showed anti-mycobacterial activities under hypoxic condition selectively, with MIC values of 1.5-6.25 μg/ml.

摘要

从海绵属的一种海洋海绵中分离出一种新的aaptamine类生物碱,命名为2-甲氧基-3-氧代aaptamine(1),以及七种已知的aaptamines(2-8),作为抗活性和休眠杆菌的抗分枝杆菌物质。1的化学结构通过光谱分析确定。化合物1在活跃生长和诱导休眠的低氧条件下对耻垢分枝杆菌均具有抗分枝杆菌活性,最低抑菌浓度(MIC)为6.25μg/ml,化合物2、5、6和7在低氧条件下选择性地表现出抗分枝杆菌活性,MIC值为1.5-6.25μg/ml。

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