Department of Internal Medicine I, University of Bonn Bonn, Germany.
Front Physiol. 2013 Jul 30;4:195. doi: 10.3389/fphys.2013.00195. eCollection 2013.
Progression of liver fibrosis is characterized by synthesis and degradation of extracellular matrix (ECM). Matrix-metalloproteinases (MMP) cleave collagen fibers at a specific site and thereby generate soluble fragments of ECM (neo-epitopes). The levels of these neo-epitopes might reflect the stage of liver fibrosis and may allow monitoring of anti-fibrotic therapies. Here we analyzed these neo-epitopes as read-out for a liver directed therapy with statins.
Bile duct ligation (BDL) was performed on wild type rats, which received atorvastatin (15 mg/kg(*)d) for 1 week starting at 1, 2, 3, 4 and 5 weeks after BDL (T1-T5), while controls remained untreated. Hepatic fibrosis was analyzed by immunohistochemistry and hepatic hydroxyproline content. TGFβ levels were measured by RT-PCR. Proteolytic activity of MMP-2 was examined by zymography. Levels of degradation MMP driven type I, III, IV and VI collagen degradation (C1M, C3M, C4M, and C6M) and type III and IV collagen formation (PRO-C3 and P4NP7S) markers were assessed by specific ELISAs in serum probes.
Serum markers of ECM neo-epitopes reflected significantly the deposition of ECM in the liver and were able to distinguish between early (T1-T3) and severe fibrosis (T4-T5). Statin treatment resulted in reduction of neo-epitope markers, especially when therapy was started in the stage of severe fibrosis (T4-T5). Furthermore, these markers correlated with hepatic expression of profibrotic cytokines TGFβ1 and TGFβ2. Formation markers of type III and IV collagen (PRO-C3 and P4NP7S) and degradation markers C4M and C6M correlated significantly with hepatic MMP-2 activity in rats with severe fibrosis.
Determination of ECM remodeling turnover markers in serum allowed a distinction between mild and severe fibrosis. With respect to statin therapy, the markers may serve as read-out for efficacy of anti-fibrotic treatment.
肝纤维化的进展以细胞外基质(ECM)的合成和降解为特征。基质金属蛋白酶(MMP)在特定部位切割胶原纤维,从而产生 ECM 的可溶性片段(新表位)。这些新表位的水平可能反映肝纤维化的阶段,并可能允许监测抗纤维化治疗。在这里,我们分析了这些新表位作为他汀类药物靶向肝脏治疗的指标。
对野生型大鼠进行胆管结扎(BDL),从 BDL 后 1、2、3、4 和 5 周(T1-T5)开始,每天给予阿托伐他汀(15mg/kg(*)d)治疗 1 周,而对照组则未治疗。通过免疫组织化学和肝羟脯氨酸含量分析肝纤维化。通过 RT-PCR 测量 TGFβ 水平。通过明胶酶谱法检查 MMP-2 的蛋白水解活性。通过特定 ELISA 评估降解 MMP 驱动的 I 型、III 型、IV 型和 VI 型胶原降解(C1M、C3M、C4M 和 C6M)和 III 型和 IV 型胶原形成(PRO-C3 和 P4NP7S)标志物在血清探针中的水平。
ECM 新表位的血清标志物显著反映了 ECM 在肝脏中的沉积,并能够区分早期(T1-T3)和严重纤维化(T4-T5)。他汀类药物治疗导致新表位标志物减少,尤其是在严重纤维化阶段(T4-T5)开始治疗时。此外,这些标志物与肝纤维化促纤维化细胞因子 TGFβ1 和 TGFβ2 的表达相关。严重纤维化大鼠中 III 型和 IV 型胶原形成标志物(PRO-C3 和 P4NP7S)和降解标志物 C4M 和 C6M 与肝 MMP-2 活性显著相关。
血清中 ECM 重塑周转率标志物的测定可区分轻度和严重纤维化。关于他汀类药物治疗,这些标志物可作为抗纤维化治疗疗效的指标。