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[四种抗癌中药提取物对大鼠肝脏CYP3A活性及mRNA表达的影响]

[Effects on the activities and mRNA expression of CYP3A in rat's liver by four kinds of extracts from anti-cancer Traditional Chinese Medicines].

作者信息

Dong Hai-yan, Shao Jing-wei, Wang Tao, Guo Yang-hao, Yan Ling-yan

机构信息

Institute of Pharmaceutical Biotechnology and Bioengineering, Fuzhou University, Fuzhou 350002, China.

出版信息

Zhong Yao Cai. 2008 Jan;31(1):68-71.

PMID:18589752
Abstract

OBJECTIVE

To study the effects of four kinds of extracts from anti-cancer Taditional Chinese Medicines on the activity and mRNA expression of CYP3A in rat's liver.

METHODS

Rat's liver microsomal cytochrome P450 and CYP3A isoemzymes--erythromycin N-demethylase(ERD) activities were determined by UV chromatography, the mRNA expression levels of CYP3Al and CYP3A2 were detected by reverse transcriptase-polymerase chain reaction (RT-PCR).

RESULTS

Extracts of Rhizoma Curcumae, Rhizoma Atractylodes and Rhizoma Atractylodes Macrocaphalae markedly increased the P450 content of liver microsomes and induced the enzyme activity of CYP3A, but extract of Poria cocos did not. At the mRNA level, extracts of Rhizoma Curcumae, Rhizoma Atractylodes Lanceae and Rhizoma Atractylodes Macraphalae induced the expression of CYP3A1, but extract of Poria cocos did not. The expression of CYP3A2 were induced by extracts of Rhizoma Curcumae and Rhizoma Atractylodes Lanceae, but extracts of Rhizoma Atractylodes Macrocaphalae and Poria cocos were found of remarkable inhibition of the mRNA expression of CYP3A2.

CONCLUSION

Extracts of Rhizoma Curcumae, Rhizoma Atractylodes Lanceae and Rhizoma Atractylodes Macrocaphalae can regulate CYP3A on the levels of enzyme activity and mRNA expression, but Poria cocos extract only regulated CYP3A on the level of mRNA expression, possibly by affecting the metabolism of other drugs in the body.

摘要

目的

研究四种抗癌中药提取物对大鼠肝脏CYP3A活性及mRNA表达的影响。

方法

采用紫外色谱法测定大鼠肝脏微粒体细胞色素P450及CYP3A同工酶——红霉素N-脱甲基酶(ERD)活性,逆转录聚合酶链反应(RT-PCR)检测CYP3A1和CYP3A2的mRNA表达水平。

结果

莪术、白术和苍术提取物显著增加肝脏微粒体P450含量,诱导CYP3A酶活性,而茯苓提取物无此作用。在mRNA水平,莪术、茅苍术和苍术提取物诱导CYP3A1表达,茯苓提取物无此作用。莪术和茅苍术提取物诱导CYP3A2表达,而苍术和茯苓提取物对CYP3A2的mRNA表达有显著抑制作用。

结论

莪术、茅苍术和苍术提取物可在酶活性和mRNA表达水平上调节CYP3A,而茯苓提取物仅在mRNA表达水平上调节CYP3A,可能通过影响体内其他药物的代谢发挥作用。

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