|Tropical Journal of Pharmaceutical Research|
|Official Journal of Pharmacotherpy Group|
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Studies on the Genotoxic and Mutagenic
Potentials of Mefloquine
John O Akerele † and Emmanuel E Obaseiki-EborDepartment of Pharmaceutical Microbiology, University of Benin, PMB 1154, Benin City, Nigeria
Journal of Pharmaceutical Research 2002; 1(2): 91-98
The detection of mefloquine
mutagenicity has not been achieved by the use of Salmonella typhimurium his
TA1535, TA1537 as tester strains. With
the introduction of improved and more sensitive strains, it is of interest to
evaluate the current mutagenic and genotoxic status of the drug.
This study presents data on the in-vitro mutagenic and genotoxic
potentials of mefloquine hydrochloride clinically used as an antimalarial agent.
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.
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.
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.
Base-pair substitution, genotoxicity, mefloquine hydrochloride, mutagenicity,
†To whom correspondence should be addressed:
E-mail: email@example.com or firstname.lastname@example.org
|@2002. TJPR Faculty of Pharmacy, University of Benin, Benin City, Nigeria|
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|Last updated: January 09, 2003|