期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 60, 期 41, 页码 10278-10284出版社
AMER CHEMICAL SOC
DOI: 10.1021/jf303160y
关键词
compound K; ginsenosides; butyl and octyl ester; Caco-2 cells; intestinal absorption; P-glycoprotein
资金
- Ministry of Education, China [20103601120004]
- Chinese Post-Doctorate Science Fund 47th Surface Fund [20100471424]
- 4th Special Fund [201104590]
- Research Program of State Key Laboratory of Food Science and Technology, Nanchang University [SKLF-MB-201003]
Ginsenoside compound K (CK) is a bioactive compound with poor oral bioavailability due to its high polarity, while its novel ester prodrugs, the butyl and octyl ester (CK-B and CK-O), are more lipophilic than the original drug and have an excellent bioavailability. The aim of this study was to examine the transport mechanisms of CK, CK-B, and CK-O using human Caco-2 cells. Results showed that CK had a low permeability coefficient (8.65 x 10(-7) cm/s) for apical-to-basolated (AP-BL) transport at 10-50 mu M, while the transport rate for AP to BL flux of CK-B (2.97 x 10(-6) cm/s) and CK-O (2.84 x 10(-6) cm/s) was significantly greater than that of CK. Furthermore, the major transport mechanism of CK was found as passive transcellular diffusion with active efflux mediated by P-glycoprotein (P-gp). In addition, it was found that CK-B and CK-O were not the substrate of efflux transporter since the selective inhibitors (verapamil and MK-571) of efflux transporter had little effects on the transport of CK-B and CK-O in the Caco-2 cells. These results suggest that improving the lipophilicity of CK by acylation can significantly improve the transport across Caco-2 cells.
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