Abstract
To evaluate the invitro and invivo inhibitory effects of two commonly used herbs, Aframomum melegueta (A.melengueta) and Dennettia tripetala (D.tripetala) on CYP 3A enzymes. Invitro inhibition of the enzymes were assessed with microsomes extracted from female albino rats using erythromycin-N-demethylation assay (EMND) method while their invivo effects were measured by estimating simvastatin plasma concentrations in rats. Pharmacokinetic parameters were determined using non-compartmental analysis as implemented in WinNonlin pharmacokinetic program. EMND assay with intestinal microsomes indicated that aqueous extracts of D.tripetala and A.melengueta significantly (P<0.05) inhibited intestinal CYP 3A activity at both 50μg and 100μg concentrations. Petroleum ether extract of D.tripetala and ethanol extracts of A.melengueta inhibited intestinal CYP3A activity at 100μg but not at 50μg concentrations. All the extracts showed an invitro dose dependent CYP 3A inhibition with liver microsomes. Invivo analysis showed that pre-treatment with the extracts enhanced systemic absorption of simvastatin with reductions in metabolizing enzymes activity as indicated in significant increases in maximal concentration, area under curve, area under moment curve and mean resident time of simvastatin (P<0.05). Herbal preparations containing these plants' extracts should be used with caution especially in patients on CYP450 3A substrate medications.
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