- Increased bioavailability of tricin-amino acid derivatives via a prodrug approach
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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.
- Ninomiya, Masayuki,Tanaka, Kaori,Tsuchida, Yuzo,Muto, Yoshinori,Koketsu, Mamoru,Watanabe, Kunitomo
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p. 1529 - 1536
(2011/05/12)
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