Rens Céline, Laval Françoise, Daffé Mamadou, Denis Olivier, Frita Rosangela, Baulard Alain, Wattiez Ruddy, Lefèvre Philippe, Fontaine Véronique
Université Libre de Bruxelles (ULB), Unit of Pharmaceutical Microbiology and Hygiene, Brussels, Belgium.
Institute of Pharmacology and Structural Biology, University of Toulouse, CNRS, University Paul Sabatier (UMR 5089), Department of Tuberculosis and Infection Biology, Toulouse Cedex 04, France.
Antimicrob Agents Chemother. 2016 Sep 23;60(10):6193-9. doi: 10.1128/AAC.00872-16. Print 2016 Oct.
Tuberculosis is still a cause of major concern, partly due to the emergence of multidrug-resistant strains. New drugs are therefore needed. Vancomycin can target mycobacteria with cell envelope deficiency. In this study, we used a vancomycin susceptibility assay to detect drugs hampering lipid synthesis in Mycobacterium bovis BCG and in Mycobacterium tuberculosis We tested three drugs already used to treat human obesity: tetrahydrolipstatin (THL), simvastatin, and fenofibrate. Only vancomycin and THL were able to synergize on M. bovis BCG and on M. tuberculosis, although mycobacteria could also be inhibited by simvastatin alone. Lipid analysis allowed us to identify several lipid modifications in M. tuberculosis H37Rv treated with those drugs. THL treatment mainly reduced the phthiocerol dimycocerosate (PDIM) content in the mycobacterial cell wall, providing an explanation for the synergy, since PDIM deficiency has been related to vancomycin susceptibility. Proteomic analysis suggested that bacteria treated with THL, in contrast to bacteria treated with simvastatin, tried to recover, inducing, among other reactions, lipid synthesis. The combination of THL and vancomycin should be considered a promising solution in developing new strategies to treat multidrug-resistant tuberculosis.
结核病仍然是一个主要的关注点,部分原因是多重耐药菌株的出现。因此需要新药。万古霉素可以靶向具有细胞壁缺陷的分枝杆菌。在本研究中,我们使用万古霉素敏感性测定法来检测阻碍牛分枝杆菌卡介苗(Mycobacterium bovis BCG)和结核分枝杆菌(Mycobacterium tuberculosis)脂质合成的药物。我们测试了三种已用于治疗人类肥胖症的药物:四氢脂抑素(THL)、辛伐他汀和非诺贝特。尽管分枝杆菌也可被单独的辛伐他汀抑制,但只有万古霉素和THL能够在牛分枝杆菌卡介苗和结核分枝杆菌上产生协同作用。脂质分析使我们能够鉴定用这些药物处理的结核分枝杆菌H37Rv中的几种脂质修饰。THL处理主要降低了分枝杆菌细胞壁中结核硬脂酸二霉菌酸酯(PDIM)的含量,这为协同作用提供了解释,因为PDIM缺陷与万古霉素敏感性有关。蛋白质组学分析表明,与用辛伐他汀处理的细菌相比,用THL处理的细菌试图恢复,除其他反应外,还诱导脂质合成。THL和万古霉素的联合应用应被视为开发治疗多重耐药结核病新策略的一个有前景的解决方案。