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7-甲基胡桃酮与抗结核药物联合对结核分枝杆菌的活性。

Activity of 7-methyljuglone in combination with antituberculous drugs against Mycobacterium tuberculosis.

作者信息

Bapela N B, Lall N, Fourie P B, Franzblau S G, Van Rensburg C E J

机构信息

Department of Pharmacology, University of Pretoria, PO Box 2034, Pretoria, 0001, South Africa.

出版信息

Phytomedicine. 2006 Nov;13(9-10):630-5. doi: 10.1016/j.phymed.2006.08.001. Epub 2006 Sep 20.

Abstract

The recent increase in the incidence of tuberculosis with the emergence of multidrug-resistant (MDR) cases has lead to the search for new drugs that are effective against MDR strains of Mycobacterium tuberculosis and can augment the potential of existing drugs against tuberculosis. In the present study, we investigated the activities of a naphthoquinone, 7-methyljuglone, isolated from the roots of Euclea natalensis alone and in combination with other antituberculous drugs against extracellular and intracellular M. tuberculosis. Combinations of 7-methyljuglone with isoniazid or rifampicin resulted in a four to six-fold reduction in the minimum inhibitory concentration of each compound. Fractional inhibitory concentration (FIC) indexes obtained were 0.2 and 0.5, respectively, for rifampicin and isoniazid, suggesting a synergistic interaction between 7-methyljuglone and these anti-TB drugs. The ability of 7-methyljuglone to enhance the activity of isoniazid and rifampicin against both extracellular and intracellular organisms suggests that 7-methyljuglone may serve as a promising compound for development as an anti-tuberculous agent.

摘要

随着多重耐药(MDR)结核病例的出现,近期结核病发病率上升,这促使人们寻找对结核分枝杆菌多重耐药菌株有效的新药,并增强现有抗结核药物的潜力。在本研究中,我们单独研究了从纳塔尔核果树根中分离出的萘醌7-甲基胡桃醌以及它与其他抗结核药物联合使用时对细胞外和细胞内结核分枝杆菌的活性。7-甲基胡桃醌与异烟肼或利福平联合使用时,每种化合物的最低抑菌浓度降低了四到六倍。利福平和异烟肼的部分抑菌浓度(FIC)指数分别为0.2和0.5,表明7-甲基胡桃醌与这些抗结核药物之间存在协同相互作用。7-甲基胡桃醌增强异烟肼和利福平对细胞外和细胞内生物体活性的能力表明,7-甲基胡桃醌可能是一种有前景的抗结核药物开发化合物。

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