Influence and Mechanism of Bioactive Ingredients of Ligusticum chuan-xiong Hort. on the Transport of Gastrodin in MDCK-MDR1 Monolayer Cells / 中国药学杂志
Chinese Pharmaceutical Journal
;
(24): 1234-1240, 2017.
Artigo
em Chinês
| WPRIM
| ID: wpr-858641
ABSTRACT
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 I and senkyunolide A were detected by MTT assay. The transport mechanism of gastrodin and the influence of ligustilide, senkyunolide I 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 I 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 Papp(B→A)/Papp(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 μg·mL-1) or senkyunolide I(120 μg·mL-1), the Papp(A→B) of gastrodin in MDCK-MDR1 were significantly increased(P<0.01). In the presence of senkyunolide A(120 μg·mL-1), the Papp(A→B) of gastrodin in MDCK-MDR1 were markedly increased(P<0.05). High, medium and low dose of ligustilide, senkyunolide A and senkyunolide I 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 I increase the transport of gastrodin attribute to down-regulate P-gp expression.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Idioma:
Chinês
Revista:
Chinese Pharmaceutical Journal
Ano de publicação:
2017
Tipo de documento:
Artigo
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