ANTIMYCOBACTERIAL AND CYTOTOXICITY ACTIVITIES OF FREE AND LIPOSOME-ENCAPSULATED 3-(4 '-BROMO[1,1 '-BIPHENYL-4-YL)-3-(4-BROMO-PHENYL)-N,N-DIMETHYL-2-PROPEN-1-AMINE

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)The antimycobacterial activity of 3-(4'-bromo[1,1'-bipheny1-4-yl)-3-(4-bromo-phenyl-N,N-dimethyl-2-propen-1-amine (BBAP), free or incorporated in preformed liposomes, on extracellular M. tuberculosis H37Rv was 8 and 25 mu M (MIC), respectively. Extracellular antimycobacterial activity was not significantly improved by entrapment of BBAP in liposomes, but there was a 6.1-fold reduction of BBAP cytotoxicity on J774 macrophages. Liposomal BBAP or its free form showed IC(50) values of 165 and 27 mu M, resulting in a selectivity index (SI=IC(50)/MIC) of 3.4 and 6.6, respectively. Free BBAP in concentrations from 10 to 80 mu M were quite effective in eliminating intracellular M. tuberculosis while liposomal formulation was less effective at these concentrations.334871874Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq