ABSTRACT
Objective: To explore the effect of arecoline hydrobromide (AH) on the expression of rat hepatic and renal transporters. Methods: The effect of AH on the mRNA expression of 13 hepatic and renal transporters was studied after orally giver AH (0.8, 4, and 20 mg/kg/d) to rats for 21 d. Results: The results from the real-time PCR indicated that, AH treatment at low dose significantly decreased the mRNA levels of hepatic MRP2 and MDR1A, while significantly increased renal MRP5 mRNA level. On the other hand, AH treatment at high dose significantly inhibited the mRNA expression of hepatic OCT2, OAT2, OCTN2, OATP1A1, OATP1A4, OATP2B1, MRP2, and MDR1A, as well as renal MRP2, BCRP, and MDR1A. However, the mRNA expression of renal OCTN2, OATP1A1, OATP1A4, and MRP5 were significantly up-regulated following the treatment of high dose of AH. And the AH-induced effect on the above transporters was dose dependent in some extent. Conclusion: Due to the drug interaction caused by the alteration in expression and function of hepatic and renal transporters, it is suggested that the betel nut addicts should be paid more attention in case of adverse drug interactions.