The interaction of Trans -resveratrol and its glucoside Trans peceid with drug transporters

Abstract

Abstract: AIM: To study the two stilbenes'(trans resveratrol, TR and its glucoside trans piceid,TP) interaction with A BC transporters in cell models.METHODS: The concentrations of TR，TP， and Rhodimin123 (Rh123) in cells were measured by HPLC or fluorescence spectrophotometer. Cytotoxicity was determined with MTT. The expression of P-gp was evaluated using Westem blot. RESULTS: Pgp's inhibitor and substrate (Verapamil and Rh123) had no impact on the accumulation of the two stilbenes. Pro-benecid, the inhibitor of multidrug resistance -associated protein2 (Mrp-2)，increased accumulation of TR and TP to 1.3 and 1.6 folds. TR andTP increased the uptake of Rh123 in RBMECs. Adriamycin's (ADM) cytotoxicity was also enhanced by the two stilbenes.The expression of Pgp in K562/A02 cells wasn't changed noticeably by∞- incubating with TR or TP.The stilbenes also didn' t change the cytotoxicity of Mitoxantrone (MIT) in Human non -small cell lung cancer cell (NCIH460).CONCLUSION: TR and TP inhibited P-gp from excreting substrates. They were effluent by Mrp2，not P-gp. They didn't affet the effluent of BCRP.

Key words: trans-resveratrol, trans-pecied, multidrug resistance-associated protein, P-gp, breast cancer research program

CLC Number:

R969

HE Hui, CHEN Xi-jing, WANG Guang-ji. The interaction of Trans -resveratrol and its glucoside Trans peceid with drug transporters[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2008, 13(4): 366-372.

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