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从秦艽中分离出的抗分枝杆菌新木脂素。

Antimycobacterial neolignans isolated from Aristolochia taliscana.

机构信息

Unidad Investigación Médica en Farmacología de Productos Naturales, Cuauhtémoc, México DF, México.

出版信息

Mem Inst Oswaldo Cruz. 2010 Feb;105(1):45-51. doi: 10.1590/s0074-02762010000100006.

DOI:10.1590/s0074-02762010000100006
PMID:20209328
Abstract

Tuberculosis (TB - Mycobacterium tuberculosis) is an ancient infectious disease that has appeared once again as a serious worldwide health problem and now comprises the second leading cause of death resulting from a single infection. The prevalence of multidrug resistance (MDR) TB is increasing and therapeutic options for treatment are not always accessible; in fact, some patients do not respond to the available drugs. Therefore, there is an urgent need to develop novel anti-TB agents. The aim of the present study was to screen extracts of Aristolochia taliscana, a plant used in traditional Mexican medicine to treat cough and snake bites, for antimycobacterial activity. The hexanic extract of A. taliscana was tested by microdilution alamar blue assay against Mycobacterium strains and bioguided fractionation led to the isolation of the neolignans licarin A, licarin B and eupomatenoid-7, all of which had antimycobacterial activity. Licarin A was the most active compound, with minimum inhibitory concentrations of 3.12-12.5 microg/mL against the following M. tuberculosis strains: H37Rv, four mono-resistant H37Rv variants and 12 clinical MDR isolates, as well as against five non-tuberculous mycobacteria (NTM) strains. In conclusion, licarin A represents a potentially active anti-TB agent to treat MDR M. tuberculosis and NTM strains.

摘要

结核病(TB-结核分枝杆菌)是一种古老的传染病,它再次成为一个严重的全球健康问题,现在是导致单一感染死亡的第二大主要原因。耐多药结核病(MDR-TB)的流行率正在上升,治疗选择并不总是可行的;事实上,有些患者对现有药物没有反应。因此,迫切需要开发新的抗结核药物。本研究的目的是筛选传统墨西哥医学中用于治疗咳嗽和蛇咬伤的马兜铃属植物马兜铃的提取物的抗分枝杆菌活性。采用微量稀释 alamar blue 法对马兜铃属植物的正己烷提取物进行了分枝杆菌菌株的检测,生物导向的馏分分离导致分离出具有抗分枝杆菌活性的新木脂素 licarin A、licarin B 和 eupomatenoid-7。Licarin A 是最活跃的化合物,对 H37Rv、四种单耐药 H37Rv 变体和 12 株临床 MDR 分离株以及五种非结核分枝杆菌(NTM)菌株的最小抑菌浓度为 3.12-12.5 μg/mL。总之,licarin A 代表了一种潜在的抗结核药物,可用于治疗 MDR-TB 和 NTM 菌株。

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