MODULATION OF RAT HEPATIC AND INTESTINAL CYP3A4 ACTIVITY BY CNIDOSCOLUS ACONITIFOLIUS LEAF ETHANOLEXTRACTS

Abstract

Background: CYP3A4 is a major cytochrome P450 enzymes involved in the metabolism of
several clinically prescribed drugs that have been implicated in herb-drug interactions.
Aim: Thisstudy investigated the in vitro effect of ethanol extract of Cnidoscolus aconitifolius
Leaf on CYP3A4 activity in rat liver and intestinal microsomes.
Method: The hepatic and intestinal microsomes were obtained through differential
centrifugation method. The concentration of formaldehyde obtained from the erythromycin N
demethylation reaction catalyzed by CYP3A4 was determined using spectrophotometer.
Results: Based on the results obtained, C. aconitifoliusextract at 0.25, 0.5, and 1 mg/mL
significantly reduced metabolism of erythromycin by inhibiting CYP3A4 activity in rat liver and
intestinal microsomes when compared to the control group.
Conclusion: The findings from this study suggest that ethanol extract of C. aconitifolius leaf
may interact with the metabolism of erythromycin in both rat liver and intestinal microsomes.
Thus, this plant should be used with caution for drugs metabolized by CYP3A4 enzymes.