Icahn School of Medicine at Mount Sinai, 1425 Madison Ave., Rm. 11-70, Box 1123, New York, NY 10029.
Am J Physiol Gastrointest Liver Physiol. 2013 Sep 1;305(5):G375-82. doi: 10.1152/ajpgi.00185.2012. Epub 2013 Jun 27.
Liver fibrosis, with subsequent development of cirrhosis and ultimately portal hypertension, results in the death of patients with end-stage liver disease if liver transplantation is not performed. Hepatic stellate cells (HSCs), central mediators of liver fibrosis, resemble tissue pericytes and regulate intrahepatic blood flow by modulating pericapillary resistance. Therefore, HSCs can contribute to portal hypertension in patients with chronic liver disease (CLD). We have previously demonstrated that activated HSCs express functional chemokine receptor, CXCR4, and that receptor engagement by its ligand, CXCL12, which is increased in patients with CLD, leads to further stellate cell activation in a CXCR4-specific manner. We therefore hypothesized that CXCL12 promotes HSC contraction in a CXCR4-dependent manner. Stimulation of HSCs on collagen gel lattices with CXCL12 led to gel contraction and myosin light chain (MLC) phosphorylation, which was blocked by addition of AMD3100, a CXCR4 small molecule inhibitor. These effects were further mediated by the Rho kinase pathway since both Rho kinase knockdown or Y-27632, a Rho kinase inhibitor, blocked CXCL12 induced phosphorylation of MLC and gel contraction. BAPTA-AM, a calcium chelator, had no effect, indicating that this pathway is calcium sensitive but not calcium dependent. In conclusion, CXCL12 promotes stellate cell contractility in a predominantly calcium-independent fashion. Our data demonstrates a novel role of CXCL12 in stellate cell contraction and the availability of small molecule inhibitors of the CXCL12/CXCR4 axis justifies further investigation into its potential as therapeutic target for portal hypertension.
肝纤维化,随后发展为肝硬化,最终导致终末期肝病患者死亡,如果不进行肝移植。肝星状细胞(HSCs)是肝纤维化的主要调节细胞,类似于组织周细胞,通过调节肝内毛细血管周围阻力来调节肝内血流。因此,HSCs 可导致慢性肝病(CLD)患者发生门静脉高压。我们之前已经证明,活化的 HSCs 表达功能性趋化因子受体 CXCR4,其配体 CXCL12 在 CLD 患者中增加,通过 CXCR4 特异性方式导致星状细胞进一步活化。因此,我们假设 CXCL12 以 CXCR4 依赖的方式促进 HSC 收缩。用 CXCL12 刺激胶原凝胶格子上的 HSCs 导致凝胶收缩和肌球蛋白轻链(MLC)磷酸化,这可以通过添加 AMD3100(一种 CXCR4 小分子抑制剂)来阻断。这些作用进一步通过 Rho 激酶途径介导,因为 Rho 激酶敲低或 Rho 激酶抑制剂 Y-27632 阻断了 CXCL12 诱导的 MLC 磷酸化和凝胶收缩。BAPTA-AM,一种钙螯合剂,没有作用,表明该途径是钙敏感但不是钙依赖性的。总之,CXCL12 以主要不依赖钙的方式促进星状细胞收缩性。我们的数据表明 CXCL12 在星状细胞收缩中具有新的作用,并且 CXCL12/CXCR4 轴的小分子抑制剂的可用性证明了其作为门静脉高压治疗靶点的潜在价值。