Lam Ian P Y, Lee Leo T O, Choi Hueng-Sik, Alpini Gianfranco, Chow Billy K C
School of Biological Sciences, The Univerity of Hong Kong, Pokfulam Rd., Hong Kong.
Am J Physiol Gastrointest Liver Physiol. 2009 Jul;297(1):G90-7. doi: 10.1152/ajpgi.00094.2009. Epub 2009 Apr 16.
Small heterodimer partner (SHP) is an orphan nuclear receptor in which gene expression can be upregulated by bile acids. It regulates its target genes by repressing the transcriptional activities of other nuclear receptors including NeuroD, which has been shown to regulate secretin gene expression. Here, we evaluated the regulation on duodenal secretin gene expression by SHP and selected bile acids, cholic acid (CA) and chenodeoxycholic acid (CDCA). In vitro treatment of CDCA or fexaramine elevated the SHP transcript level and occupancy on secretin promoter. The increase in the SHP level, induced by bile acid treatment or overexpression, reduced secretin gene expression, whereas this gene inhibitory effect was reversed by silencing of endogenous SHP. In in vivo studies, double-immunofluorescence staining demonstrated the coexpression of secretin and SHP in mouse duodenum. Feeding mice with 1% CA-enriched rodent chow resulted in upregulation of SHP and a concomitant decrease in secretin transcript and protein levels in duodenum compared with the control group fed with normal chow. A diet enriched with 5% cholestyramine led to a decrease in SHP level and a corresponding increase in secretin expression. Overall, this study showed that bile acids via SHP inhibit duodenal secretin gene expression. Because secretin is a key hormone that stimulates bile flow in cholangiocytes, this pathway thus provides a novel means to modulate secretin-stimulated choleresis in response to intraduodenal bile acids.
小异源二聚体伴侣蛋白(SHP)是一种孤儿核受体,其基因表达可被胆汁酸上调。它通过抑制包括NeuroD在内的其他核受体的转录活性来调节其靶基因,NeuroD已被证明可调节促胰液素基因的表达。在此,我们评估了SHP以及选定的胆汁酸——胆酸(CA)和鹅去氧胆酸(CDCA)对十二指肠促胰液素基因表达的调控作用。体外给予CDCA或非诺贝特可提高SHP转录水平及其在促胰液素启动子上的占有率。胆汁酸处理或过表达诱导的SHP水平升高会降低促胰液素基因的表达,而内源性SHP的沉默可逆转这种基因抑制作用。在体内研究中,双重免疫荧光染色显示促胰液素和SHP在小鼠十二指肠中共表达。与喂食正常饲料的对照组相比,给小鼠喂食富含1% CA的啮齿动物饲料会导致十二指肠中SHP上调,同时促胰液素转录本和蛋白水平降低。富含5%消胆胺的饮食会导致SHP水平降低,促胰液素表达相应增加。总体而言,本研究表明胆汁酸通过SHP抑制十二指肠促胰液素基因表达。由于促胰液素是刺激胆管细胞胆汁流动的关键激素,因此该途径提供了一种新的方式来调节对十二指肠内胆汁酸作出反应的促胰液素刺激的胆汁分泌。