Department of Agricultural, Food and Nutritional Sciences, University of Alberta, Edmonton, Canada.
Division of Geriatrics, Department of Medicine, UCLA, Los Angeles, California, USA.
Rejuvenation Res. 2021 Dec;24(6):434-440. doi: 10.1089/rej.2021.0052.
Metformin, a commonly used well-tolerated treatment for type 2 diabetes, is being deployed in clinical trials to ameliorate aging in older nondiabetic humans. Concerningly, some experiments in model organisms have suggested that metformin use at old ages shortens life span and is toxic to mitochondria. The demonstrated safety of metformin therapy in humans and the conflicting data from model organisms compelled us to test the hypothesis that metformin treatment would be toxic to older rats. To define an effective dose in 30-month-old hybrid rats, we evaluated two doses of metformin (0.1%, 0.75% of the diet) and treated the rats for 4 months. Body mass decreased at the 0.75% dose. Neither dose affected mortality between 30 and 34 months of age. We assessed mitochondrial integrity by measuring mitochondrial DNA (mtDNA) copy number and deletion mutation frequency, and mitochondrial respiration in skeletal muscle and the heart. In skeletal muscle, we observed no effect of metformin on quadriceps mass, mtDNA copy number, or deletion frequency. In the heart, metformin-treated rats had higher mtDNA copy number, lower cardiac mass, with no change in mtDNA deletion frequency. Metformin treatment resulted in lower mitochondrial complex I-dependent respiration in the heart. We found that, in old rats, metformin did not compromise mtDNA integrity, did not affect mortality, and may have cardiac benefits. These data provide some reassurance that a metformin intervention in aged mammals is not toxic at appropriate doses.
二甲双胍是一种常用于治疗 2 型糖尿病的耐受性良好的药物,目前正在临床试验中用于改善非糖尿病老年人群的衰老。令人担忧的是,一些模型生物的实验表明,老年时使用二甲双胍会缩短寿命并对线粒体有毒。二甲双胍在人类中的治疗安全性和来自模型生物的相互矛盾的数据,促使我们检验二甲双胍治疗是否会对老年大鼠有毒的假设。为了确定 30 月龄杂交大鼠的有效剂量,我们评估了二甲双胍的两种剂量(饮食的 0.1%和 0.75%),并对大鼠进行了 4 个月的治疗。0.75%剂量组的体重下降。在 30 至 34 月龄之间,两种剂量均未影响死亡率。我们通过测量线粒体 DNA(mtDNA)拷贝数和缺失突变频率以及骨骼肌和心脏的线粒体呼吸来评估线粒体的完整性。在骨骼肌中,我们没有观察到二甲双胍对股四头肌质量、mtDNA 拷贝数或缺失频率的影响。在心脏中,接受二甲双胍治疗的大鼠 mtDNA 拷贝数更高,心脏质量更低,但 mtDNA 缺失频率没有变化。二甲双胍治疗导致心脏中线粒体复合物 I 依赖性呼吸降低。我们发现,在老年大鼠中,二甲双胍不会损害 mtDNA 完整性,不会影响死亡率,并且可能对心脏有益。这些数据提供了一些保证,即在适当剂量下,对老年哺乳动物进行二甲双胍干预不会有毒性。