Inhibitory effect of caffeic acid and its derivatives on human liver cytochrome P450 3A4 activity

被引：0

作者：

Jaikang, Churdsak ^{[1
]}

Niwatananun, Kanokporn ^{[2
]}

Narongchai, Paitoon ^{[3
]}

Narongchai, Siripun ^{[3
]}

Chaiyasut, Chaiyavat ^{[1
]}

机构：

[1] Chiang Mai Univ, Dept Pharmaceut Sci, Fac Pharm, Chiang Mai 50200, Thailand

[2] Chiang Mai Univ, Dept Pharmaceut Care, Fac Pharm, Chiang Mai 50200, Thailand

[3] Chiang Mai Univ, Dept Forens Med, Fac Med, Chiang Mai 50200, Thailand

来源：

JOURNAL OF MEDICINAL PLANTS RESEARCH | 2011年 / 5卷 / 15期

关键词：

Cytochrome P450 3A4; caffeic acid; caffeic acid amide; caffeic acid ester; MICROSOMES; DRUGS;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Effects of caffeic acid (CAF) and its derivatives on human liver CYP3A4 activity were evaluated by using diazepam as a substrate. It was found that CAF inhibited CYP3A4 activity by uncompetitive inhibition with IC50 0.72 mu M, whereas ester and amide analogues inhibited CYP3A4 by competitive inhibition with IC50 value of 0.31, 0.37, 0.46, 0.49, 0.53, 0.58, 0.75 and 0.82 mu M for ethyl 1- (3',4'-dihydroxyphenyl) propen amide (EDPA), phenmethyl 1- (3',4'-dihydroxyphenyl) propen amide (PMDPA), phenethyl 1- (3',4'-dihydroxyphenyl) propen amide (PEDPA), phenylethyl 1- (3',4'-dihydroxyphenyl) propenate (PC), ethyl 1- (3',4'-dihydroxyphenyl) propenate (EC), octyl 1- (3',4'-dihydroxyphenyl) propen amide (ODPA), octyl 1- (3',4'-dihydroxyphenyl) propenate (OC) and phenylmethyl 1- (3',4'-dihydroxyphenyl) propenate (BC), respectively. The K-i values of CAF, PMDPA, EC, PC, ODPA, PEDPA, OC, EDPA and BC were 0.24, 0.29, 0.49, 0.56, 0.57, 0.59, 0.62, 0.62 and 1.03 mu M, respectively. However, CAF and its derivatives had high potential to inhibit CYP3A4. Therefore, consumption of herbal medicine containing CAF and its derivatives that are concomitant with other medications should be cautiously monitored.

引用

页码：3530 / 3536

页数：7

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