Naphthofuroquinone derivatives show strong antimycobacterial activities against drug-resistant Mycobacteria.

Naphthofuroquinone derivatives show strong antimycobacterial activities against drug-resistant Mycobacteria.

J Chemother. 2017 Mar 10;:1-6

Authors: Jang WS, Choi YS, Kim S, Jyoti MA, Seo H, Han J, Kim YS, Lyu J, Nam KW, Lee BE, Lee KI, Song HY

Abstract
Tuberculosis, one of the world's major health problems, has become more serious due to the emergence of multi-drug resistant (MDR) and extensively drug-resistant (XDR) Mycobacterium tuberculosis (MTB). In this study, we performed three anti-MTB assays to evaluate the anti-mycobacterial activity of naphthofuroquinone derivatives against drug-resistant MTB. Among them, methyl 5-[2-(dimethylamino)ethoxy]-7,12-dioxo-7,12-dihydrodinaphtho[1,2-b:2',3'-d]furan-6-carboxylate (DFC2) exhibited strong anti-mycobacterial activity against MTB H37Ra, H37Rv and four drug-resistant MTB strains. The MIC of DFC2 ranged from 0.19-0.39 μg/ml to 0.78-1.56 μg/ml against all tested MTB strains. Moreover, DFC2 showed low cytotoxicity against fibroblast cells (L929) at concentrations 10-40-fold higher than their MICs. The IC50 value of DFC2 against L929 cells was 15.218 μg/ml. In addition, DFC2 reduced the number of intracellular M. tuberculosis in macrophages in a dose-dependent manner. Taken together, our results indicate DFC2 to be promising new candidate agents for the treatment of tuberculosis.

PMID: 28281912 [PubMed - as supplied by publisher]

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