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  • Title: Increased bioavailability of tricin-amino acid derivatives via a prodrug approach.
    Author: Ninomiya M, Tanaka K, Tsuchida Y, Muto Y, Koketsu M, Watanabe K.
    Journal: J Med Chem; 2011 Mar 10; 54(5):1529-36. PubMed ID: 21319803.
    Abstract:
    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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