Laboratory of Microbiology, Biomedical Research Center of the South (IMSS), Argentina 1, Col. Centro, 62790 Xochitepec, Morelos, Mexico.
Molecules. 2011 Aug 29;16(9):7357-64. doi: 10.3390/molecules16097357.
The increased incidence of Multidrug-Resistant Mycobacterium tuberculosis (MDR-MT) requires the search for alternative antimycobacterial drugs. The main aim of this study was to evaluate the dichloromethane extract from Aristolochia brevipes (Rhizoma) and the compounds isolated from this extract against several mycobacterial strains, sensitive, resistant (monoresistant), and clinical isolates (multidrug-resistant), using the alamarBlue™ microassay. The extract was fractionated by column chromatography, yielding the following eight major compounds: (1) 6α-7-dehydro-N-formylnornantenine; (2) E/Z-N-formylnornantenine; (3) 7,9-dimethoxytariacuripyrone; (4) 9-methoxy-tariacuripyrone; (5) aristololactam I; (6) β-sitosterol; (7) stigmasterol; and (8) 3-hydroxy-α-terpineol. The structures of these compounds were elucidated by 1H- and 13C- (1D and 2D) Nuclear Magnetic Resonance (NMR) spectroscopy. This study demonstrates that the dichloromethane extract (rhizome) of A. brevipes possesses strong in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (Minimum Inhibitory Concentration value [MIC], 12.5 µg/mL). The most active compound against all mycobacterial strains tested was the compound aristolactam I (5), with MIC values ranging between 12.5 and 25 µg/mL. To our knowledge, this the first report of antimycobacterial activity in this plant.
多药耐药结核分枝杆菌（MDR-MT）发病率的增加需要寻找替代抗分枝杆菌药物。本研究的主要目的是评估马兜铃科植物关木通（Rhizoma）的二氯甲烷提取物以及从该提取物中分离得到的化合物对几种分枝杆菌菌株（敏感、耐药（单耐药）和临床分离株（多药耐药））的抗菌活性，使用alamarBlue™微量测定法。提取物通过柱色谱法进行分离，得到以下八种主要化合物：（1）6α-7-去氢-N-甲酰基去甲乌药碱；（2）E/Z-N-甲酰基去甲乌药碱；（3）7,9-二甲氧基塔里考林酮；（4）9-甲氧基-塔里考林酮；（5）马兜铃内酰胺 I；（6）β-谷甾醇；（7）豆甾醇；和（8）3-羟基-α-松油醇。这些化合物的结构通过 1H-和 13C-（1D 和 2D）NMR 光谱确定。本研究表明，关木通（Rhizoma）的二氯甲烷提取物具有很强的体外抗结核分枝杆菌 H37Rv 活性（最低抑菌浓度值 [MIC]，12.5 µg/mL）。对所有测试的分枝杆菌菌株最有效的化合物是马兜铃内酰胺 I（5），其 MIC 值在 12.5 和 25 µg/mL 之间。据我们所知，这是该植物具有抗分枝杆菌活性的首次报道。
