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Introduction: Pueraria candollei Wall. ex Benth. var. mirifica (family Leguminosae), as known Kwao Kruea Khaw in Thai, has been widely used in Thai traditional medicine and is supplied in commercial health products for rejuvenation. It is interesting to investigate the potential effect of P. candollei and its component, miroestrol, on P-glycoprotein function to provide the important drug-herb interaction data for applying in clinical relevance. Objective: This present study is investigated the effect of P. candollei extract and miroestro, the potent phytoestrogen found in P. candollei on P-glycoprotein, the efflux transporter, function. Materials and Methods: Determine effect of substances on P-glycoprotein function by employing the in vitro transport of rhodamine 123, a substrate of P-glycoprotein, across everted intestinal sac was studied in mice. The ability of P. candollei tincture and the P. candollei ethyl acetate extract fraction to inhibit p-glycoprotein function were examined. Results: P. candollei extract has no effect on P-glycoprotein function. Miroestrol showed negligible inhibitory effect on P-glycoprotein function at the concentration at 100 µM and higher. For expression of P-glycoprotein, change in expression of ABCB1 and ABCB2 mRNAs in mice administered with miroestrol at 0.5 mg/kg/day subcutaneously for 7 days was not observed. Conclusion: Miroestrol, and P. candollei extracts have negligible effect on p-glycoprotein function. However, the effect of phytoestrogens contained in the tuberous root of P. candollei on P-glycoprotein and other protein transporters after long term of administration should be further investigated.
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