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Increased Bioavailability of Tricin-Amino Acid Derivatives via a Prodrug Approach.
MedLine Citation:
PMID:  21319803     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
Masayuki Ninomiya; Kaori Tanaka; Yuzo Tsuchida; Yoshinori Muto; Mamoru Koketsu; Kunitomo Watanabe
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-2-14
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  -     Publication Date:  2011 Feb 
Date Detail:
Created Date:  2011-2-15     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
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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