Department of Animal Physiology, Biochemistry and Biostructure, Poznan University of Life Sciences, 60-637, Poznan, Poland.
Department of Animal Physiology, Biochemistry and Biostructure, Poznan University of Life Sciences, 60-637, Poznan, Poland.
Mol Cell Endocrinol. 2023 Nov 1;577:112037. doi: 10.1016/j.mce.2023.112037. Epub 2023 Aug 3.
Ostarine is the most popular compound in the selective androgen receptor modulator group (SARMs). Ostarine is used as a physical performance-enhancing agent. The abuse of this agent in higher doses may lead to severe side effects. Here, we evaluate the effects of ostarine on the heart. We utilized a cardiomyocyte H9C2 cell line, isolated primary female and male cardiac fibroblast cells, as well as hearts obtained from rats. Ostarine increased the accumulation of two fibrosis protein markers, αSMA and fibronectin (p < 00.1) in male, but not in female fibroblast cells. Ostarine increased the expression of the cardiomyopathy marker βMhc in the H9C2 cell line (p < 0.05) and in the heart in rats (p < 0.01). The unfavorable changes were observed at high ostarine doses. Moreover, a decrease in viability and an increase in cytotoxicity marker LDH were observed already at lowest dose (1 nmoL/l). Taken together, our results suggest that ostarine is cardiotoxic which may be more relevant in males than in females.
Ostarine 是选择性雄激素受体调节剂 (SARMs) 组中最受欢迎的化合物。Ostarine 被用作一种提高身体机能的药物。这种药物在高剂量下滥用可能会导致严重的副作用。在这里，我们评估了 Ostarine 对心脏的影响。我们利用心肌细胞 H9C2 细胞系、分离的原代雌性和雄性心脏成纤维细胞以及来自大鼠的心脏进行研究。Ostarine 增加了雄性而非雌性成纤维细胞中两种纤维化蛋白标志物 αSMA 和纤维连接蛋白的积累（p<0.01）。Ostarine 增加了 H9C2 细胞系（p<0.05）和大鼠心脏中心肌病标志物 βMhc 的表达（p<0.01）。在高 Ostarine 剂量下观察到不利的变化。此外，在最低剂量（1nmoL/L）下就观察到细胞活力下降和细胞毒性标志物 LDH 增加。总之，我们的结果表明 Ostarine 具有心脏毒性，在男性中可能比在女性中更为相关。
