Abstract:
:Despite bioavailability issues, tea catechins have emerged as promising chemopreventive agents because of their efficacy in various animal models. We synthesized two catechin-derived compounds, 3-O-(3,4,5-trimethoxybenzoyl)-(-)-catechin (TMCG) and 3-O-(3,4,5-trimethoxybenzoyl)-(-)-epicatechin (TMECG), in an attempt to improve the stability and cellular absorption of tea polyphenols. The antiproliferative and pro-apoptotic activities of both compounds were analyzed with various cancer cell systems, and TMCG, which was easily synthesized in excellent yield, was more active than TMECG in both melanoma and non-melanoma cell lines. TMCG was also a better inhibitor of dihydrofolate reductase and was more efficiently oxidized by tyrosinase, potentially explaining the difference in activity between these epimers.
journal_name
ChemMedChemjournal_title
ChemMedChemauthors
Sáez-Ayala M,Sánchez-del-Campo L,Montenegro MF,Chazarra S,Tárraga A,Cabezas-Herrera J,Rodríguez-López JNdoi
10.1002/cmdc.201000482subject
Has Abstractpub_date
2011-03-07 00:00:00pages
440-9issue
3eissn
1860-7179issn
1860-7187journal_volume
6pub_type
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