Future microbiology · 2017
Biological evaluation of novel curcumin-pyrazole-mannich derivative active against drug-resistant Mycobacterium tuberculosis.
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Singh Alok Kumar, Yadav Pragya, Karaulia Pratiksha, Singh Vinay Kumar, Gupta Pushpa, Puttrevu Santosh Kumar, Chauhan Sanjay, Bhatta Rabi S, Tadigoppula Narender, Gupta Umesh D, Chopra Sidharth, Dasgupta Arunava
Аннотация
AIM: Our objective was to identify a more potent curcumin derivative with specific activity against Mycobacterium tuberculosis.
MATERIALS & METHODS: A total of 21 curcumin derivatives were synthesized and detailed bio-evaluation was carried out including determination of static/cidality, synergy with front-line antituberculosis drugs and determination of efficacy in the murine model of M. tuberculosis infection.
RESULTS: We identified CPMD-6d dihydrochloride exhibiting concentration-dependent bactericidal activity against M. tuberculosis (MIC 2 μg/ml), even against drug-resistant strains. In addition, it synergizes with front-line antituberculosis drugs as well as significantly reduces bacterial load in mice lungs and spleen at 25 mg/kg as compared with ethambutol at 100 mg/kg.
CONCLUSION: Taken together, CPMD-6d dihydrochloride exhibits all properties to be positioned as a novel molecule of interest for treatment of tuberculosis. Graphical abstract: [Formula: see text].
MATERIALS & METHODS: A total of 21 curcumin derivatives were synthesized and detailed bio-evaluation was carried out including determination of static/cidality, synergy with front-line antituberculosis drugs and determination of efficacy in the murine model of M. tuberculosis infection.
RESULTS: We identified CPMD-6d dihydrochloride exhibiting concentration-dependent bactericidal activity against M. tuberculosis (MIC 2 μg/ml), even against drug-resistant strains. In addition, it synergizes with front-line antituberculosis drugs as well as significantly reduces bacterial load in mice lungs and spleen at 25 mg/kg as compared with ethambutol at 100 mg/kg.
CONCLUSION: Taken together, CPMD-6d dihydrochloride exhibits all properties to be positioned as a novel molecule of interest for treatment of tuberculosis. Graphical abstract: [Formula: see text].