Identification of inhibitory component in cinnamon--O-methoxycinnamaldehyde inhibits CYP1A2 and CYP2E1-.
Identification of inhibitory component in cinnamon--O-methoxycinnamaldehyde inhibits CYP1A2 and CYP2E1-.
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DOI：
10.2133/dmpk.17.229
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发表时间：
2002
影响因子：
2.1
通讯作者：
A. Hasegawa;M. Yoshino;Hiroyoshi Nakamura;I. Ishii;Toshiko Watanabe;M. Kiuchi;T. Ishikawa;S. Ohmori;M. Kitada
中科院分区：
文献类型：
--
作者：
A. Hasegawa;M. Yoshino;Hiroyoshi Nakamura;I. Ishii;Toshiko Watanabe;M. Kiuchi;T. Ishikawa;S. Ohmori;M. Kitada
研究发现，肉桂皮和麻黄对大鼠肝微粒体氨基吡啶n -去甲基化的抑制作用强于shoseiru -to中的其他成分。从肉桂皮中分离到由CYP1A2和CYP2E1催化的抑制药物氧化的成分，鉴定为o-甲氧基肉桂醛（OMCA）。以非那西丁和4-硝基酚分别作为CYP1A2和CYP2E1的探针底物时，发现OMCA对CYP1A2是竞争性抑制剂，而对CYP2E1是混合型抑制剂。OMCA对大鼠肝微粒体中4-硝基苯酚2-羟基化（K(i)=6.3 μ m）的抑制作用强于对非那西丁o -去乙基化（K(i)=13.7 μ m）的抑制作用。
The Cinnamomi Cortex and Ephedra Herba were found to more strongly inhibit aminopyrine N-demethylation in rat liver microsomes compared to other constituents included in Sho-seiryu-to. The component inhibiting drug oxidations catalyzed by CYP1A2 and CYP2E1 was isolated from Cinnamomi Cortex, and was identified as o-methoxycinnamaldehyde (OMCA). When phenacetin and 4-nitrophenol were used as probe substrates for CYP1A2 and CYP2E1, respectively, the OMCA was shown to be a competitive inhibitor against CYP1A2 while it was a mixed type inhibitor against CYP2E1. The inhibitory effect of OMCA on 4-nitrophenol 2-hydroxylation (K(i)=6.3 microM) was somewhat potent compared to that observed on phenacetin O-deethylation (K(i)=13.7 microM) in rat liver microsomes.