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猪的CYP2A19、CYP2E1和CYP1A2亚型在重组系统中负责粪臭素的生物转化。

Porcine CYP2A19, CYP2E1 and CYP1A2 forms are responsible for skatole biotransformation in the reconstituted system.

作者信息

Matal Jaroslav, Matuskova Zuzana, Tunkova Alena, Anzenbacherova Eva, Anzenbacher Pavel

机构信息

Department of Pharmacology, Palacky University, Olomouc, Czech Republic.

出版信息

Neuro Endocrinol Lett. 2009;30 Suppl 1:36-40.

Abstract

OBJECTIVES

To study the contribution of individual purified porcine CYP1A2, 2E1 and 2A19 enzymes to the biotransformation of skatole.

METHODS

Individual porcine and human enzymes (CYP1A2, 2E1 or 2A6/19) were used to study their potential involvement in skatole metabolism. Furthermore, the inhibition experiments using specific inhibitors of CYP1A2, 2E1 or 2A6/19, were performed. For determination of skatole biotransformation by individual CYP forms in reconstituted systems, HPLC method with UV detection was used.

RESULTS

The data presented in this paper show that porcine and human CYPs are responsible for the formation of indole-3-carbinol and 3-methyloxindole. Whereas in pig CYP2A19 and CYP1A2 seem to be the most important for metabolism of skatole, in man CYP1A2 and CYP2E1 forms are mainly responsible for the production of the metabolites mentioned above.

CONCLUSIONS

The porcine and human CYP1A2, 2E1, 2A6/19 forms contribute to formation of 3-methyloxindole and indole-3-carbinol.

摘要

目的

研究纯化的猪源CYP1A2、2E1和2A19单酶对粪臭素生物转化的作用。

方法

使用猪源和人源单酶(CYP1A2、2E1或2A6/19)研究它们在粪臭素代谢中的潜在作用。此外,进行了使用CYP1A2、2E1或2A6/19特异性抑制剂的抑制实验。为了测定重组系统中各CYP亚型对粪臭素的生物转化,采用了带紫外检测的高效液相色谱法。

结果

本文数据表明,猪源和人源细胞色素P450酶负责吲哚 - 3 - 甲醇和3 - 甲基氧化吲哚的形成。在猪体内,CYP2A19和CYP1A2似乎对粪臭素代谢最为重要,而在人体内,CYP1A2和CYP2E1亚型主要负责上述代谢产物的生成。

结论

猪源和人源CYP1A2、2E1、2A6/19亚型有助于3 - 甲基氧化吲哚和吲哚 - 3 - 甲醇的形成。

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