Mefloquine and Its Enantiomers Are Active against Mycobacterium tuberculosis In Vitro and in Macrophages. (11th December 2014)

• Record Type: Journal Article
• Authors: Bermudez, Luiz E.; Meek, Laura
• Other Names: Ottenhoff T. Academic Editor.
• Is Part Of: Tuberculosis research and treatment. Volume 2014(2014)
• Publication Date: 2014-12-11
• Subjects: Tuberculosis -- Periodicals; Tuberculosis -- Prevention -- Periodicals; Tuberculosis -- Treatment -- Periodicals; Tuberculosis -- Social aspects -- Periodicals; 616.995005
• DOI: 10.1155/2014/530815
• Languages: English
• ISSNs: 2090-150X

Abstract

Abstract : Objective . Tuberculosis is a serious problem of public health. The increase on the number of clinical cases of tuberculosis infected with multidrug resistant (MDR) M. tuberculosis calls for the development of novel therapy. Design . We investigated the effect of mefloquine and two enantiomers, (+)erythro-mefloquine and (+)threo-mefloquine against M. tuberculosis strains in the environment resembling the aspects of the granuloma environment and in macrophages. Results . The results suggest that mefloquine (racemic mixture) and (+)erythro-mefloquine have bactericidal activity against M. tuberculosis strains both in acidic, low oxygen tension and in macrophages. The activity, however, was impaired under increased osmolarity. Conclusion . Identification of the target for mefloquine in the pathogen will allow for the development of novel drugs with antituberculosis activity.