| Increased Bioavailability of Tricin-Amino Acid Derivatives via a Prodrug Approach. | |
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MedLine Citation:
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PMID: 21319803 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Tricin (4',5,7-trihydroxy-3',5'-dimethoxyflavone) has demonstrated diverse biological activities. This compound has a high anti-human cytomegalovirus (HCMV) activity; however, its oral availability is low. To improve its bioavailability, we synthesized tricin-amino acid derivatives as prodrugs and investigated their cell permeability, stability in vitro, and oral availability in vivo. The results demonstrated that the tricin-alanine-glutamic acid conjugate exhibited enhanced permeability, stability in MDCK cells, and excellent bioavailability after oral administration in Crl:CD (SD) male rats. Tricin-alanine-glutamic acid conjugate is a potential new anti-HCMV drug. |
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Authors:
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Masayuki Ninomiya; Kaori Tanaka; Yuzo Tsuchida; Yoshinori Muto; Mamoru Koketsu; Kunitomo Watanabe |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-2-14 |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: - ISSN: 1520-4804 ISO Abbreviation: - Publication Date: 2011 Feb |
Date Detail:
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Created Date: 2011-2-15 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Department of Materials Science and Technology, Faculty of Engineering, ‡Department of Functional Bioscience, School of Medicine, §Division of Anaerobe Research, Life Science Research Center, and ∥United Graduate School of Drug Discovery and Medical Information Sciences, Gifu University , 1-1 Yanagido, Gifu 501-1194, Japan. |
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