摘要
目的探讨山姜素能否通过活化孕烷X受体(PXR)诱导CYP3A4的转录表达及对CYP3A4 mRNA的实际诱导作用。方法在人结肠癌LS174T细胞中,用瞬时共转染报告基因实验研究山姜素(1～50μmol.L-1)对PXR介导的CYP3A4基因的转录激活;用荧光定量RT-PCR方法检测其对CYP3A4 mRNA的实际诱导。结果 10μmol.L-1浓度山姜素能够通过活化PXR诱导CYP3A4的转录(1.63倍);10和20μmol.L-1山姜素能够明显上调CYP3A4 mRNA(2.28倍和1.65倍)的表达。结论 PXR途径也许是山姜素诱导CYP3A4基因表达的调控因素之一。
Aim To investigate the effects of alpinetin on pregnane x receptor（PXR） mediated transcriptional activation of CYP3A4 and the influence on CYP3A4 mRNA expression in LS174T cells.Methods Transient cotransfection reporter assays were performed in LS174T cells following alpinetin（1～50 μmol·L-1） treatment and the CYP3A4 activation was confirmed by measuring the activity of luciferase.CYP3A4 mRNA expression was assayed by real-time PCR.Results Alpinetin at 10 μmol·L-1 significantly transactivated the CYP3A4 reporter constructed in LS174T cells（1.63-fold）.The CYP3A4 mRNA expression was markedly increased（2.28-fold and 1.65-fold） by alpinetin at 10 μmol·L-1 and 20 μmol·L-1 respectively.Conclusion Activation of the PXR pathway might played a role in the up-regulation of CYP3A4 mRNA.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2012年第6期761-763,共3页
Chinese Pharmacological Bulletin
基金
国家自然科学基金资助项目(No U1032604
81150040)
