Institute for Cardiovascular Physiology, Goethe-University, Frankfurt, Germany.
Curr Opin Pharmacol. 2010 Apr;10(2):173-8. doi: 10.1016/j.coph.2009.12.002. Epub 2010 Jan 14.
Epoxyeicosatrienoic acids (EETs) build a family consisting of four arachidonic acid derived regioisomers that are generated by P450 epoxygenases. In the past years, growing interest in influencing EET level arose since EETs possess numerous beneficial effects in the cardiovascular system, for example, vasodilation, anti-inflammation and elicit renal and myocardial protection. Because EETs are primarily metabolized by the soluble epoxide hydrolase (sEH) and potent inhibitors of this enzyme are currently available, pharmacological sEH inhibition seems to be a feasible approach to elevate EET level in vivo. Hence, first clinical trials on sEH inhibition in man have begun. This review focuses on sEH inhibition as a novel pharmacological cardiovascular protective strategy with special regard to in vivo investigations.
环氧二十碳三烯酸（EETs）构成了一个由 P450 环氧化物酶生成的四种花生四烯酸衍生的区域异构体组成的家族。在过去的几年中，人们对影响 EET 水平的兴趣日益浓厚，因为 EETs 在心血管系统中具有许多有益的作用，例如血管舒张、抗炎和引起肾和心肌保护。由于 EETs 主要被可溶性环氧化物水解酶（sEH）代谢，并且目前有这种酶的有效抑制剂，因此药理学 sEH 抑制似乎是一种可行的方法，可以在体内提高 EET 水平。因此，首例人类 sEH 抑制的临床试验已经开始。本文综述了 sEH 抑制作为一种新的药理学心血管保护策略，特别是体内研究。
