1887

Abstract

The antibacterial activity of the nitrogen heterocyclic sponge constituent cribrostatin 6 was examined. Cribrostatin 6 was bacteriostatic for a variety of Gram-positive species and was bactericidal for the majority of clinical isolates of , including penicillin-resistant strains. Minimum bactericidal concentration/MIC ratios were ⩽2 for 75 % of clinical isolates. Kill-curve analysis confirmed the bactericidal action of cribrostatin 6. Bactericidal activity was rather slow, beginning at 2, 4 or 8 h, depending on the strain. The frequency of occurrence of bacterial spontaneous mutations to resistance was ⩽10. The maximum tolerated dose of cribrostatin 6 in mice was 750–1000 μg kg day. Cribrostatin 6 is a promising lead antibiotic for Gram-positive bacteria, particularly , a leading cause of infection and mortality worldwide.

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2004-01-01
2019-11-21
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