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Journal of Antimicrobial Chemotherapy (2001) 47, 199-202
© 2001 The British Society for Antimicrobial Chemotherapy

Brief report

Antimycobacterial action of B4128, a novel tetramethylpiperidyl-substituted phenazine

N. M. Matlola, H. C. Steel and R. Anderson*

Medical Research Council Unit for Inflammation and Immunity, Department of Immunology, Institute for Pathology, University of Pretoria, PO Box 2034, Pretoria 0001, South Africa

The effects of the novel tetramethylpiperidyl (TMP)-substituted phenazine, B4128 (0.6–2.5 mg/L), on growth, phospholipase A2(PLA2) activity, cation (K+, Ca2+) fluxes and energy metabolism (ATP) of Mycobacterium aurum A+ and Mycobacterium tuberculosis (H37Ra) have been investigated in vitro. Growth, PLA2 and cation fluxes were measured radiometrically, while microbial ATP was assayed by means of a luciferin/luciferase chemiluminescence method. Exposure of the mycobacteria to B4128 resulted in immediate, dose-related enhancement of microbial PLA2 activity and inhibition of K+-influx, which preceded effects on microbial ATP, influx of Ca2+ and growth. These results demonstrate that B4128 possesses membrane-directed antimycobacterial properties that are similar to those of clofazimine.

* Corresponding author. Tel: +27-12-319-2425; Fax: +27-12-323-0732; E-mail: randerso{at}postillion.up.ac.za


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