| Absorption Mechanism of Ginsenoside Compound K and Its Butyl and Octyl Ester Prodrugs in Caco-2 Cells. | |
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MedLine Citation:
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PMID: 23013417 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: JOURNAL ARTICLE Date: 2012-9-27 |
Journal Detail:
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Title: Journal of agricultural and food chemistry Volume: - ISSN: 1520-5118 ISO Abbreviation: J. Agric. Food Chem. Publication Date: 2012 Sep |
Date Detail:
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Created Date: 2012-9-27 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0374755 Medline TA: J Agric Food Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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