天然和半合成木脂素的抗分枝杆菌活性。

Antimycobacterial activity of natural and semi-synthetic lignans.

机构信息

Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201, CEP 14404-600--Franca, SP, Brazil.

出版信息

Z Naturforsch C J Biosci. 2009 Nov-Dec;64(11-12):779-84. doi: 10.1515/znc-2009-11-1204.

DOI:10.1515/znc-2009-11-1204

PMID:20158145

Abstract

The antimycobacterial activity of (-)-cubebin (1), hinokinin (2), and some of their semisynthetic derivatives, namely (-)-O-acetyl-cubebin (3), (-)-O-methyl-cubebin (4), (-)-O-(N,N-dimethylamine-ethyl)-cubebin (5) and (-)-6,6'-dinitrohinokinin (6), was evaluated against Mycobacterium tuberculosis (ATCC 27294), M. kansasii (ATCC 12478), and M. avium (ATCC 15769). The MIC values ranged from 31.25 to 2000 microg/mL. Among the evaluated compounds, 2 displayed a MIC value of 62.5 microg/mL against M. tuberculosis, while 3 and 4 displayed MIC values of 62.5 and 31.25 microg/mL, respectively, against M. avium. All compounds were inactive against M. kansasii. These are promising results concerning the search for biologically active natural products, highlighting that new approaches to the prevention, treatment, and cure of tuberculosis are extremely important.

摘要

(-)-麻黄油（1）、扁柏酚（2）及其部分半合成衍生物（即(-)-O-乙酰麻黄油（3）、(-)-O-甲基麻黄油（4）、(-)-O-（N，N-二甲胺乙基）麻黄油（5）和(-)-6,6'-二硝基扁柏酚（6））的抗分枝杆菌活性针对结核分枝杆菌（ATCC 27294）、堪萨斯分枝杆菌（ATCC 12478）和鸟分枝杆菌（ATCC 15769）进行了评估。MIC 值范围为 31.25 至 2000 μg/mL。在所评估的化合物中，2 对结核分枝杆菌的 MIC 值为 62.5 μg/mL，而 3 和 4 对鸟分枝杆菌的 MIC 值分别为 62.5 和 31.25 μg/mL。所有化合物对堪萨斯分枝杆菌均无活性。这些结果表明，寻找具有生物活性的天然产物是有希望的，突显了预防、治疗和治愈结核病的新方法极其重要。