期刊
XENOBIOTICA
卷 41, 期 4, 页码 290-296出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/00498254.2010.529180
关键词
Coptis chinensis; isoquinoline alkaloids; transport; Caco-2 cells; P-gp; MRP2
资金
- Doctor Subject Foundation of the Ministry of Education of China [200802680010]
- Shanghai Natural Science Founding [10ZR1430800]
- National Major Program for Clinical Evaluation Research Technology platform of Viral Hepatitis Novel Traditional Chinese Medicine Production [2008ZX09312-023]
- Shanghai Leading Academic Discipline Project [J50303]
- Construction Program for Innovative Research Team in Shanghai Institutions of Higher Education
The absorption and transport mechanisms of berberine, palmatine, jateorhizine, and coptisine were studied using a Caco-2 cells uptake and transport model, with the addition of cyclosporin A and verapamil as P-glycoprotein (P-gp) inhibitors and MK-571 as a multidrug resistance-associated protein 2 (MRP2) inhibitor. In the uptake experiment, berberine, palmatine, jateorhizine, and coptisine were all taken into Caco-2 cells, and their uptakes were increased in the presence of cyclosporin A or verapamil. In the transport experiment, P-app (AP-BL) was between 0.1 and 1.0 xx 10 2. Cyclosporin A and verapamil both increased P-app (AP-BL) but decreased P-app (BL-AB) for berberine, palmatine, jateorhizine, and coptisine; ER values were decreased by > 50%. MK-571 had no influence on the transmembrane transport of berberine, palmatine, jateorhizine, and coptisine. At a concentration of 1--100 mu mu M, berberine, palmatine, jateorhizine, and coptisine had no significant effects on the bidirection transport of Rho123. Berberine, palmatine, jateorhizine, and coptisine were all P-gp substrates; and at the range of 1--100 mu mu M, berberine, palmatine, jateorhizine, and coptisine had no inhibitory effects on P-gp.
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