Department of Pharmacology, New York Medical College, Valhalla, NY 10595, USA.
Department of Pharmacology, New York Medical College, Valhalla, NY 10595, USA; Department of Medicine, New York Medical College, Valhalla, NY 10595, USA; Department of Pharmacology and Medicine, Joan C. Edwards School of Medicine, Huntington, WV 25701, USA.
Trends Pharmacol Sci. 2016 Nov;37(11):945-962. doi: 10.1016/j.tips.2016.08.001. Epub 2016 Sep 13.
Cardiovascular disease remains the leading cause of death worldwide. Among many potential targets for pharmacological intervention, a promising strategy involves epoxyeicosatrienoic acid (EET) and soluble epoxide hydroxylase (sEH) inhibition. sEH is the enzyme that converts EET to its less potent metabolite; therefore, EET is upregulated by its inhibitor. EET has pleotropic effects that collectively reduce inflammation, while increasing vasodilation and insulin sensitivity. Recent reports indicate that EET agonists and sEH inhibitors are capable of not only reversing endothelial dysfunction and hypertension, but also of reversing cardiac remodeling, which is a hallmark of cardiomyopathy and the metabolic syndrome. EET agonists and sEH inhibitors are in development as potential therapies, and at least one drug is already in clinical trials. This review examines the activity of EET in biological systems, proposes a series of pathways to explain its mechanism of action, and discusses how these might be exploited for potential therapeutic use.
心血管疾病仍然是全球范围内的主要死亡原因。在许多潜在的药物干预靶点中,一种有前途的策略涉及环氧二十碳三烯酸 (EET) 和可溶性环氧化物水解酶 (sEH) 的抑制。sEH 是将 EET 转化为其效力较低的代谢物的酶;因此,EET 的抑制剂会使其上调。EET 具有多种作用,这些作用共同减少炎症,同时增加血管舒张和胰岛素敏感性。最近的报告表明,EET 激动剂和 sEH 抑制剂不仅能够逆转内皮功能障碍和高血压,还能够逆转心脏重构,这是心肌病和代谢综合征的标志。EET 激动剂和 sEH 抑制剂正在开发中作为潜在的治疗方法,至少有一种药物已经在临床试验中。这篇综述检查了 EET 在生物系统中的活性,提出了一系列途径来解释其作用机制,并讨论了如何将这些途径用于潜在的治疗用途。