Department of Pharmacology and Toxicology, Maastricht University, 6229 ER Maastricht, The Netherlands.
Nutrients. 2023 Jul 26;15(15):3330. doi: 10.3390/nu15153330.
The androgen receptor (AR) is a member of the family of ligand-activated transcription factors. Selective androgen receptor modulators (SARMs) exert their biological function through complex interactions with the AR. It has been speculated that overexertion of AR signaling cascades as a result of SARM abuse can be a risk factor for the development of various cardiovascular diseases. The present literature review explores the implications of the interaction between SARMs and the AR on cardiovascular health by focusing on the AR structure, function, and mechanisms of action, as well as the current clinical literature on various SARMs. It is shown that SARMs may increase the risk of cardiovascular diseases through implications on the renin-angiotensin system, smooth muscle cells, sympathetic nervous system, lipid profile, inflammation, platelet activity, and various other factors. More research on this topic is necessary as SARM abuse is becoming increasingly common. There is a noticeable lack of clinical trials and literature on the relationship between SARMs, cardiovascular diseases, and the AR. Future in vivo and in vitro studies within this field are vital to understand the mechanisms that underpin these complex interactions and risk factors.
雄激素受体(AR)是配体激活转录因子家族的成员。选择性雄激素受体调节剂(SARM)通过与 AR 的复杂相互作用发挥其生物学功能。有人推测,由于滥用 SARM 导致 AR 信号级联过度激活可能是各种心血管疾病发展的一个风险因素。本文献综述通过关注 AR 的结构、功能和作用机制,以及各种 SARM 的当前临床文献,探讨了 SARM 与 AR 相互作用对心血管健康的影响。结果表明,SARM 可能通过对肾素-血管紧张素系统、平滑肌细胞、交感神经系统、血脂谱、炎症、血小板活性和其他各种因素的影响,增加患心血管疾病的风险。由于 SARM 滥用越来越普遍,因此需要对这一课题进行更多的研究。关于 SARM、心血管疾病和 AR 之间关系的临床试验和文献明显缺乏。未来在该领域进行体内和体外研究对于理解这些复杂相互作用和风险因素的机制至关重要。