Elafibranor 可通过恢复肠道屏障功能缓解酒精相关肝纤维化。

IF 4.3 3区 医学 Q1 GASTROENTEROLOGY & HEPATOLOGY
Yu-Qi Sun, Yang Wu, Meng-Ran Li, Yu-Yao Wei, Mei Guo, Zi-Li Zhang
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引用次数: 0

摘要

我们讨论了 Koizumi 等人发表在《世界胃肠病学杂志》上的文章。我们的重点是酒精相关肝病(ALD)纤维化的治疗靶点以及艾拉非布然诺(EFN)的作用机制,艾拉非布然诺是过氧化物酶体增殖激活受体α(PPARα)和过氧化物酶体PPARδ(PPARδ)的双重激动剂。EFN 目前正处于治疗代谢功能障碍相关性脂肪肝和原发性胆汁性胆管炎的 III 期临床试验阶段。ALD 由酒精性脂肪肝发展为酒精性脂肪性肝炎(ASH),慢性 ASH 最终会导致肝纤维化、肝硬化,在某些情况下还会导致肝细胞癌。酒精性脂肪肝的发病机制主要是肝脏脂肪变性、氧化应激和乙醛毒性。饮酒会使 PPARα 失活,从而破坏脂质代谢,加剧 ALD 的进展。EFN 主要激活 PPARα,促进乙醇刺激的 HepG2 细胞的脂肪分解和 β 氧化,从而显著减轻 ALD 小鼠模型的肝脏脂肪变性、细胞凋亡和纤维化。此外,酒精在几个相互关联的层面上破坏了肠道-肝脏轴,导致肝脏内的促炎环境。EFN 通过恢复紧密连接蛋白的表达和自噬,抑制细胞凋亡和炎症反应,并通过激活 PPARδ 增强肠道屏障功能,从而帮助缓解肠道高渗透性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Elafibranor alleviates alcohol-related liver fibrosis by restoring intestinal barrier function.

We discuss the article by Koizumi et al published in the World Journal of Gastroenterology. Our focus is on the therapeutic targets for fibrosis associated with alcohol-related liver disease (ALD) and the mechanism of action of elafibranor (EFN), a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and peroxisome PPAR δ (PPARδ). EFN is currently in phase III clinical trials for the treatment of metabolic dysfunction-associated fatty liver disease and primary biliary cholangitis. ALD progresses from alcoholic fatty liver to alcoholic steatohepatitis (ASH), with chronic ASH eventually leading to fibrosis, cirrhosis, and, in some cases, hepatocellular carcinoma. The pathogenesis of ALD is driven by hepatic steatosis, oxidative stress, and acetaldehyde toxicity. Alcohol consumption disrupts lipid metabolism by inactivating PPARα, exacerbating the progression of ALD. EFN primarily activates PPARα, promoting lipolysis and β-oxidation in ethanol-stimulated HepG2 cells, which significantly reduces hepatic steatosis, apoptosis, and fibrosis in an ALD mouse model. Additionally, alcohol disrupts the gut-liver axis at several interconnected levels, contributing to a proinflammatory environment in the liver. EFN helps alleviate intestinal hyperpermeability by restoring tight junction protein expression and autophagy, inhibiting apoptosis and inflammatory responses, and enhancing intestinal barrier function through PPARδ activation.

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来源期刊
World Journal of Gastroenterology
World Journal of Gastroenterology 医学-胃肠肝病学
CiteScore
7.80
自引率
4.70%
发文量
464
审稿时长
2.4 months
期刊介绍: The primary aims of the WJG are to improve diagnostic, therapeutic and preventive modalities and the skills of clinicians and to guide clinical practice in gastroenterology and hepatology.
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