Wang Lai, Zheng Zu-Guo, Meng Lingchang, Zhu Lijun, Li Ping, Chen Jun, Yang Hua
State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, China.
Cell Biol Toxicol. 2021 Jun;37(3):441-460. doi: 10.1007/s10565-020-09558-w. Epub 2020 Oct 9.
Myopathy is the major adverse effect of statins. However, the underlying mechanism of statin-induced skeletal muscle atrophy, one of statin-induced myopathy, remains to be elucidated. Myostatin is a negative regulator of skeletal muscle mass and functions. Whether myostatin is involved in statin-induced skeletal muscle atrophy remains unknown. In this study, we uncovered that simvastatin administration increased serum myostatin levels in mice. Inhibition of myostatin with follistatin, an antagonist of myostatin, improved simvastatin-induced skeletal muscle atrophy. Simvastatin induced myostatin expression not only in skeletal muscle but also in brown adipose tissue (BAT). Mechanistically, simvastatin inhibited the phosphorylation of forkhead box protein O1 (FOXO1) in C2C12 myotubes, promoting the nuclear translocation of FOXO1 and thereby stimulating the transcription of myostatin. In differentiated brown adipocytes, simvastatin promoted myostatin expression mainly by inhibiting the expression of interferon regulatory factor 4 (IRF4). Moreover, the stimulative effect of simvastatin on myostatin expression was blunted by geranylgeranyl diphosphate (GGPP) supplementation in both myotubes and brown adipocytes, suggesting that GGPP depletion was attributed to simvastatin-induced myostatin expression. Besides, the capacities of statins on stimulating myostatin expression were positively correlated with the lipophilicity of statins. Our findings provide new insights into statin-induced skeletal muscle atrophy. Graphical headlights 1. Simvastatin induces skeletal muscle atrophy via increasing serum myostatin levels in mice; 2. Simvastatin promotes myostatin expression in both skeletal muscle and brown adipose tissue through inhibiting GGPP production; 3. The stimulating effect of statins on myostatin expression is positively correlated with the lipophilicity of statins.
肌病是他汀类药物的主要不良反应。然而,他汀类药物引起的肌病之一——他汀类药物诱导的骨骼肌萎缩的潜在机制仍有待阐明。肌肉生长抑制素是骨骼肌质量和功能的负调节因子。肌肉生长抑制素是否参与他汀类药物诱导的骨骼肌萎缩尚不清楚。在本研究中,我们发现给予小鼠辛伐他汀会增加血清肌肉生长抑制素水平。用肌肉生长抑制素拮抗剂卵泡抑素抑制肌肉生长抑制素可改善辛伐他汀诱导的骨骼肌萎缩。辛伐他汀不仅在骨骼肌中诱导肌肉生长抑制素表达,还在棕色脂肪组织(BAT)中诱导其表达。机制上,辛伐他汀抑制C2C12肌管中叉头框蛋白O1(FOXO1)的磷酸化,促进FOXO1的核转位,从而刺激肌肉生长抑制素的转录。在分化的棕色脂肪细胞中,辛伐他汀主要通过抑制干扰素调节因子4(IRF4)的表达来促进肌肉生长抑制素的表达。此外,在肌管和棕色脂肪细胞中,补充香叶基香叶基二磷酸(GGPP)可减弱辛伐他汀对肌肉生长抑制素表达的刺激作用,表明GGPP耗竭归因于辛伐他汀诱导的肌肉生长抑制素表达。此外,他汀类药物刺激肌肉生长抑制素表达的能力与他汀类药物的亲脂性呈正相关。我们的研究结果为他汀类药物诱导的骨骼肌萎缩提供了新的见解。图1. 辛伐他汀通过增加小鼠血清肌肉生长抑制素水平诱导骨骼肌萎缩;2. 辛伐他汀通过抑制GGPP生成促进骨骼肌和棕色脂肪组织中肌肉生长抑制素的表达;3. 他汀类药物对肌肉生长抑制素表达的刺激作用与他汀类药物的亲脂性呈正相关。