Pomelo fruit juice and pomelo ethylacetate extract have been shown to increase the bioavailability of some
CYP3A substrates. The purpose of this study was to investigate if this effect might be contributed to by changes in
CYP3A and p-glycoprotein mRNAs levels in the liver and proximal small intestine. The ethyl acetate extract of pomelo
mix was administered for 7 days to 10 rabbits. Nine rabbits were administered tap water for 7 days. The administration
was through oral intubation to the stomach. On the 8th day, the rabbits were sacrificed, and the liver and the proximal 15
cm of the small intestine were dissected. Total RNA was extracted from the specimens and cDNA was prepared by
quantitative real-time-polymerase chain reaction (RT-PCR) using specific primers. The ethyl acetate extract of pomelo
mix reduced the mRNA expression of CYP3A6 almost 5-folds in the intestine and 2-folds in the liver. In contrast, a 1-fold
increase to the p-glycoprotein mRNA expression was observed under the same experimental conditions. In conclusion, the
ethyl acetate extract of pomelo mix reduced the mRNA expression of CYP3A6 in both intestine and liver but to different
degrees, while the p-glycoprotein mRNA expression was not reduced.
Keywords: CYP3A6, mRNA, P-glycoprotein, Pomelo mix, Rabbits.
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