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Studies on the Genotoxic and Mutagenic Potentials of Mefloquine.
Abstract
Method: The mutagenicity potentials was investigated in the Escherichia coli WP2 trp and WP2 uvrA trp tester strains containing the plasmids, pEB017 and pKM101, and the Salmonella typhimurium TA97 containing pKM101. The genotoxicity potential was determined using the microscreen phage-induction assay.
Results: The presence of plasmids pEBO17 and pKM101 enhanced the detection of mutagenicity of mefloquine. Microsomal-activated mefloquine unequivocally elicited base-pair substitution mutagenicity. The genotoxicity test indicated that mefloquine was generally not genotoxic but was of the same potential mutagenicity as chloroquine phosphate.
Conclusion: Melfloquine hydrochloride exhibits base pair substitution mutagenesis, but not potentially genotoxic, even though it showed concentration dependent cytotoxicity. Its use as a last line antimalarial agent should still be encouraged.
Keywords: Base-pair substitution, genotoxicity, mefloquine hydrochloride, mutagenicity, R-plasmid pEB017
Tropical Journal of Pharmaceutical Research 2002; 1(2):91-98
