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Influence and Mechanism of Bioactive Ingredients of Ligusticum chuan-xiong Hort. on the Transport of Gastrodin in MDCK-MDR1 Monolayer Cells

??OBJECTIVE To study the influence and mechanism of bioactive ingredients of Ligusticum chuanxiong Hort. on the transport of gastrodin based on cell culture model in vitro. METHODS Cell toxicity of gastrodin, ligustilide, senkyunolide ?? and senkyunolide A were detected by MTT assay. The transport mechanism of gastrodin and the influence of ligustilide, senkyunolide ?? and senkyunolide A on the transport of gastrodin were studied in MDCK-MDR1 monolayer cells. The changed expressions of P-gp caused by ligustilide, senkyunolide ?? and senkyunolide A were analyzed by Western blotting.RESULTS Gastrodin showed relatively poor absorption in MDCK-MDR1 cells for its apparent permeability coefficients were less than 1??10^-6 cm??s^-1. P-gp inhibitor made the P_app(B??A)/P_app(A??B) of gastrodin reduced from 1.29 to 0.79, which indicated that the transport of gastrodin was influenced by P-gp. In the presence of ligustilide(30 ??g??mL^-1) or senkyunolide ??(120 ??g??mL^-1), the P_app(A??B) of gastrodin in MDCK-MDR1 were significantly increased(P<0.01). In the presence of senkyunolide A(120 ??g??mL^-1), the P_app(A??B) of gastrodin in MDCK-MDR1 were markedly increased(P<0.05). High, medium and low dose of ligustilide, senkyunolide A and senkyunolide ?? could significantly inhibit the expression of P-gp protein.CONCLUSION The results indicate that the transport mechanism of gastrodin might be passive diffusion as the dominating process with the active transportation mediated mechanism involved. Ligustilide, senkyunolide A and senkyunolide ?? increase the transport of gastrodin attribute to down-regulate P-gp expression.