Department of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia, USA,
Department of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia, USA.
Front Biosci (Landmark Ed). 2016 Jun 1;21(7):1296-313. doi: 10.2741/4458.
Sphingosine-1-phosphate (S1P) is a bioactive sphingolipid metabolite generated by phosphorylation of sphingosine catalyzed by sphingosine kinase. S1P acts mainly through its high affinity G-protein-coupled receptors and participates in the regulation of multiple systems, including cardiovascular system. It has been shown that S1P signaling is involved in the regulation of cardiac chronotropy and inotropy and contributes to cardioprotection as well as cardiac remodeling; S1P signaling regulates vascular function, such as vascular tone and endothelial barrier, and possesses an anti-atherosclerotic effect; S1P signaling is also implicated in the regulation of blood pressure. Therefore, manipulation of S1P signaling may offer novel therapeutic approaches to cardiovascular diseases. As several S1P receptor modulators and sphingosine kinase inhibitors have been approved or under clinical trials for the treatment of other diseases, it may expedite the test and implementation of these S1P-based drugs in cardiovascular diseases.
鞘氨醇-1-磷酸（S1P）是一种生物活性鞘脂代谢物，由鞘氨醇激酶催化鞘氨醇磷酸化生成。S1P 主要通过其高亲和力 G 蛋白偶联受体发挥作用，并参与包括心血管系统在内的多个系统的调节。已经表明，S1P 信号参与了心脏变时性和变力性的调节，并有助于心脏保护和心脏重塑；S1P 信号调节血管功能，如血管张力和内皮屏障，并具有抗动脉粥样硬化作用；S1P 信号也参与血压的调节。因此，对 S1P 信号的操纵可能为心血管疾病提供新的治疗方法。由于几种 S1P 受体调节剂和鞘氨醇激酶抑制剂已被批准或正在临床试验中用于治疗其他疾病，因此可能会加快这些基于 S1P 的药物在心血管疾病中的测试和实施。
