Briand François, Heymes Christophe, Bonada Lucile, Angles Thibault, Charpentier Julie, Branchereau Maxime, Brousseau Emmanuel, Quinsat Marjolaine, Fazilleau Nicolas, Burcelin Rémy, Sulpice Thierry
Physiogenex, Escalquens, France.
Inserm U1048 CHU Rangueil, Toulouse Cedex 4, France.
Clin Transl Sci. 2020 May;13(3):529-538. doi: 10.1111/cts.12735. Epub 2020 Jan 25.
The long duration of animal models represents a clear limitation to quickly evaluate the efficacy of drugs targeting nonalcoholic steatohepatitis (NASH). We, therefore, developed a rapid mouse model of liver inflammation (i.e., the mouse fed a high-fat/high-cholesterol diet, where cyclodextrin is co-administered to favor hepatic cholesterol loading, liver inflammation, and NASH within 3 weeks), and evaluated the effects of the dual peroxisome proliferator-activated receptor alpha/delta agonist elafibranor (ELA). C57BL6/J mice were fed a 60% high-fat, 1.25% cholesterol, and 0.5% cholic acid diet with 2% cyclodextrin in drinking water (HFCC/CDX diet) for 3 weeks. After 1 week of the diet, mice were treated orally with vehicle or ELA 20 mg/kg q.d. for 2 weeks. Compared with vehicle, ELA markedly reduced liver lipids and nonalcoholic fatty liver disease activity scoring, through steatosis, inflammation, and fibrosis (all P < 0.01 vs. vehicle). Flow cytometry analysis showed that ELA significantly improved the HFCC/CDX diet-induced liver inflammation by preventing the increase in total number of immune cells (CD45+), Kupffer cells, dendritic cells, and monocytes population, as well as the reduction in natural killer and natural killer T cells, and by blocking conversion of T cells in regulatory T cells. ELA did not alter pyroptosis (Gasdermin D), but significantly reduced necroptosis (cleaved RIP3) and apoptosis (cleaved caspase 3) in the liver. In conclusion, ELA showed strong benefits on NASH, including improvement in hepatic inflammation, necroptosis, and apoptosis in the 3-week NASH mouse. This preclinical model will be useful to rapidly detect the effects of novel drugs targeting NASH.
动物模型的长时间构建是快速评估治疗非酒精性脂肪性肝炎(NASH)药物疗效的一个明显限制。因此,我们开发了一种快速的肝脏炎症小鼠模型(即给小鼠喂食高脂/高胆固醇饮食,并同时给予环糊精以促进肝脏胆固醇蓄积、肝脏炎症以及在3周内诱发NASH),并评估了双重过氧化物酶体增殖物激活受体α/δ激动剂依拉贝隆(ELA)的作用。将C57BL6/J小鼠喂食含60%高脂肪、1.25%胆固醇和0.5%胆酸的饮食,并在饮用水中添加2%环糊精(HFCC/CDX饮食),持续3周。在饮食1周后,小鼠口服给予溶媒或20mg/kg的ELA,每日1次,持续2周。与溶媒组相比,ELA通过改善脂肪变性、炎症和纤维化,显著降低了肝脏脂质和非酒精性脂肪性肝病活动评分(与溶媒组相比,所有P<0.01)。流式细胞术分析显示,ELA通过防止免疫细胞(CD45+)、库普弗细胞、树突状细胞和单核细胞总数的增加,以及自然杀伤细胞和自然杀伤T细胞数量的减少,并通过阻止T细胞向调节性T细胞的转化,显著改善了HFCC/CDX饮食诱导的肝脏炎症。ELA并未改变细胞焦亡(Gasdermin D),但显著降低了肝脏中的坏死性凋亡(裂解的RIP3)和凋亡(裂解的半胱天冬酶3)。总之,ELA对NASH显示出强大的益处,包括改善3周龄NASH小鼠的肝脏炎症、坏死性凋亡和凋亡。这种临床前模型将有助于快速检测针对NASH的新型药物的效果。