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KMID : 0370220180620020077
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Yakhak Hoeji
2018 Volume.62 No. 2 p.77 ~ p.82
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In vitro assessment of cytochrome P450 inhibition by caffeic acid phenethyl ester
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Ryu Chang-Seon
Park Ji-Eun
Kim Sang-Kyum
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Abstract
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Caffeic acid phenethyl ester (CAPE) is one of the major active components of propolis showing inhibitory activity against cytochrome P450 (CYP). The purpose of this study was to determine CYP inhibitory potential and metabolic stability of CAPE using human liver microsomes (HLM) for characterization of its metabolic properties. Among CYP isoforms including CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4, CAPE exhibited strong inhibitory potential against CYP1A2 and 2C9, moderate against CYP2E1, 2B6, 2C8, 2C19 and 3A4, and weak against CYP 2D6 and 2A6, based on the IC50 values. The inhibition of CYP1A2 but not CYP2C9 was increased by preincubation with CAPE and NADPH, suggesting that the CAPE-induced CYP1A2 inhibition may be metabolism-dependent. In metabolic stability study using HLM, CAPE was rapidly hydrolyzed to caffeic acid in a NADPH-independent manner. Caffeic acid exhibited week CYP inhibitory activity, relative to CAPE. These results raise the possibility that CAPE plays a role in propolis-mediated CYP inhibition.
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KEYWORD
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cytochrome p450, drug-drug interaction, caffeic acid phenethyl ester, propolis
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