Document Detail


Absorption Mechanism of Ginsenoside Compound K and Its Butyl and Octyl Ester Prodrugs in Caco-2 Cells.
MedLine Citation:
PMID:  23013417     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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 (8.65×10-7 cm/s) for apical-to-basolated (AP-BL) transport at 10-50 µM, while the transport rates for AP to BL flux of CK-B (2.97×10-6 cm/s) and CK-O (2.84×10-6 cm/s) were 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.
Authors:
Bing Zhang; Xue-Mei Zhu; Jiang-Ning Hu; Hui Ye; Ting Luo; Xiao-Ru Liu; Hong-Yan Li; Wei Li; Yinan Zheng; Ze-Yuan Deng
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-9-27
Journal Detail:
Title:  Journal of agricultural and food chemistry     Volume:  -     ISSN:  1520-5118     ISO Abbreviation:  J. Agric. Food Chem.     Publication Date:  2012 Sep 
Date Detail:
Created Date:  2012-9-27     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0374755     Medline TA:  J Agric Food Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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