School of Biotechnology and Biomolecular Sciences, University of New South Wales, Sydney, NSW 2052, Australia.
Department of Chemistry and Virginia Tech Centre for Drug Discovery, Virginia Tech, Blacksburg, VA 24061, USA.
Biochim Biophys Acta Mol Basis Dis. 2024 Jan;1870(1):166908. doi: 10.1016/j.bbadis.2023.166908. Epub 2023 Oct 2.
Metabolic disorders such as type 2 diabetes, fatty liver disease, hyperlipidemia, and obesity commonly co-occur but clinical treatment options do not effectively target all disorders. Calorie restriction, semaglutide, rosiglitazone, and mitochondrial uncouplers have all demonstrated efficacy against one or more obesity-related metabolic disorders, but it currently remains unclear which therapeutic strategy best targets the combination of hyperglycaemia, liver fat, hypertriglyceridemia, and adiposity. Herein we performed a head-to-head comparison of 5 treatment interventions in the female db/db mouse model of severe metabolic disease. Treatments included ∼60 % calorie restriction (CR), semaglutide, rosiglitazone, BAM15, and niclosamide ethanolamine (NEN). Results showed that BAM15 and CR improved body weight and liver steatosis to levels superior to semaglutide, NEN, and rosiglitazone, while BAM15, semaglutide, and rosiglitazone improved glucose tolerance better than CR and NEN. BAM15, CR, semaglutide, and rosiglitazone all had efficacy against hypertriglyceridaemia. These data provide a comprehensive head-to-head comparison of several key treatment strategies for metabolic disease and highlight the efficacy of mitochondrial uncoupling to correct multiple facets of the metabolic disease milieu in female db/db mice.
代谢紊乱疾病,如 2 型糖尿病、脂肪肝、高脂血症和肥胖症通常同时发生,但临床治疗方案并不能有效地针对所有疾病。热量限制、司美格鲁肽、罗格列酮和线粒体解偶联剂均已证明对一种或多种与肥胖相关的代谢紊乱疾病有效,但目前尚不清楚哪种治疗策略最能针对高血糖、肝脂肪、高甘油三酯血症和肥胖症的组合。在此,我们在严重代谢疾病的 db/db 雌性小鼠模型中对头对头比较了 5 种治疗干预措施。治疗方法包括约 60%的热量限制(CR)、司美格鲁肽、罗格列酮、BAM15 和尼克酰胺乙醇胺(NEN)。结果表明,BAM15 和 CR 改善了体重和肝脂肪变性,使其达到优于司美格鲁肽、NEN 和罗格列酮的水平,而 BAM15、司美格鲁肽和罗格列酮改善葡萄糖耐量的效果优于 CR 和 NEN。BAM15、CR、司美格鲁肽和罗格列酮均对高甘油三酯血症有效。这些数据提供了对代谢疾病几种关键治疗策略的全面头对头比较,并突出了线粒体解偶联在纠正雌性 db/db 小鼠代谢疾病环境的多个方面的疗效。