Literature DB >> 27156623

Activity of nitazoxanide and tizoxanide against Mycobacterium tuberculosis in vitro and in whole blood culture.

Elizabeth P Harausz1, Keith A Chervenak2, Caryn E Good3, Michael R Jacobs4, Robert S Wallis5, Manuel Sanchez-Felix6, W Henry Boom7.   

Abstract

Nitazoxanide (NTZ) and its metabolite tizoxanide (TIZ) were studied as antimycobacterial agents in vitro (in mycobacterial growth indicator tube [MGIT] cultures) and in a whole blood bactericidal assay. Both NTZ and TIZ show high protein binding. In MGIT cultures (albumin concentration = 78 μM), inhibition of Mycobacterium tuberculosis growth occurred at total drug concentrations of ≥16 μg/ml, whereas in whole blood cultures (albumin concentration = 350 μM), ≥128 μg/ml was required. Free drug fractions at these two conditions were estimated to be 69% and 2%, respectively. Co-incubation of NTZ and TIZ in human plasma for 72 h nearly completely eliminated their ability to inhibit mycobacterial growth in MGIT. Interactions with plasma proteins may limit the potential of NTZ and TIZ as drugs for human tuberculosis.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  BCG; Mycobacteria growth indicator tube; Mycobacterium tuberculosis; Nitazoxanide; Tizoxanide; Whole blood assay

Mesh：

Substances：

Year:  2016        PMID： 27156623      PMCID： PMC4864490          DOI： 10.1016/j.tube.2016.03.002

Source DB:  PubMed          Journal:  Tuberculosis (Edinb)        ISSN： 1472-9792            Impact factor:   3.131


  15 in total

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