Effects of Kampo extracts on drug metabolism in rat liver microsomes:: Rhei Rhizoma extract and Glycyrrhizae Radix extract inhibit drug oxidation

Effects of Kampo extracts on drug metabolism in rat liver microsomes:: Rhei Rhizoma extract and Glycyrrhizae Radix extract inhibit drug oxidation
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DOI:
10.1254/jjp.89.164
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发表时间:
2002-06-01
期刊:
JAPANESE JOURNAL OF PHARMACOLOGY
影响因子:
--
通讯作者:
Kitada, M
Kitada, M
中科院分区:
其他
文献类型:
--
作者:
Hasegawa, A;Kawaguchi, Y;Kitada, M

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在本研究中,使用126汉方提取物在体外对大鼠肝微粒体药物氧化的影响进行了研究。虽然抑制药物氧化的效果依赖于汉方提取物和探针反应的研究,大多数汉方提取物显示出抑制作用的N-去甲基氨基比林和红霉素在大鼠肝微粒体。在本文研究的汉方提取物中,Daio-kanzo-to对这两种反应表现出最显著的抑制效果。甘草提取物不仅能抑制氨基比林和红霉素的N-去甲基化,而且能抑制非那西丁O-去乙基化、7-乙氧基香豆素O-去乙基化、乙醇氧化和甲苯磺丁脲4-羟基化。黄芪提取物对非那西丁O-脱乙基反应、氨基比林和红霉素N-脱甲基反应也有明显的抑制作用。与此相反,黄芪提取物几乎没有表现出对乙醇氧化的影响。
In the present study, the effects on drug oxidations in rat liver microsomes in vitro using 126 Kampo extracts were investigated. Although the effects of inhibition on drug oxidations were dependent on the Kampo extracts and probe reactions studied, most of the Kampo extracts showed inhibitory effects on both N-demethylations of aminopyrine and erythromycin in rat liver microsomes. Among the Kampo extracts studied herein, Daio-kanzo-to exhibited the most remarkable inhibitory effect on both reactions. The Rhei Rhizoma extract inhibited not only aminopyrine and erythromycin N-demethylations, but also phenacetin O-deethylation, 7-ethoxycoumarin O-deethylation, ethanol oxidation and tolbutamide 4-hydroxylation in rat liver microsomes. The Glycyrrhizae Radix extract also showed a remarkable inhibitory effect on phenacetin O-deethylation as well as aminopyrine and erythromycin N-demethylations. In contrast, the Glycyrrhizae Radix extract virtually showed no effect on ethanol oxidation.