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首页> 外文期刊>Biochemistry >Endocannabinoid Virodhamine Is an Endogenous Inhibitor of Human Cardiovascular CYP2J2 Epoxygenase
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Endocannabinoid Virodhamine Is an Endogenous Inhibitor of Human Cardiovascular CYP2J2 Epoxygenase

机译：Endocannabinoid Virodhamine是人心血管CYP2J2环氧树脂酶的内源性抑制剂

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摘要

The human body contains endogenous cannabinoids (endocannabinoids) that elicit effects similar to those of Delta(9)-tetrahydrocanabinol, the principal bioactive component of cannabis. The endocannabinoid virodhamine (O-AEA) is the constitutional isomer of the well-characterized cardioprotective and anti-inflammatory endocannabinoid anandamide (AEA). The chemical structures of O-AEA and AEA contain arachidonic acid (AA) and ethanolamine; however, AA in O-AEA is connected to ethanolamine via an ester linkage, whereas AA in AEA is connected through an amide linkage. O-AEA is involved in regulating blood pressure and cardiovascular function. We show that O-AEA is found at levels 9.6-fold higher than that of AEA in porcine left ventricle. On a separate note, the cytochrome P450 (CYP) epoxygenase CYP2J2 is the most abundant CYP in the heart where it catalyzes the metabolism of AA and AA-derived eCBs to bioactive epoxides that are involved in diverse cardiovascular functions. Herein, using competitive binding studies, kinetic metabolism measurements, molecular dynamics, and wound healing assays, we have shown that O-AEA is an endogenous inhibitor of CYP2J2 epoxygenase. As a result, the role of O-AEA as an endogenous eCB inhibitor of CYP2J2 may provide a new mode of regulation to control the activity of cardiovascular CYP2J2 in vivo and suggests a potential cross-talk between the cardiovascular endocannabinoids and the cytochrome P450 system.
机译：人体含有内源性大麻素（Endocannaboids），其产生与δ--四氢二甲醛，大麻的主要生物活性成分相似的效果。 Endocannabinoid Virodhamine（O-AEA）是具有良好表征的心脏保护和抗炎endocannaboidAnandamide（AEA）的构成异构体。 O-AEA和AEA的化学结构含有花生素酸（AA）和乙醇胺;然而，O-AEA中的AA通过酯键连接到乙醇胺，而AEA中的AA通过酰胺键连接。 O-AEA参与调节血压和心血管功能。我们展示O-AEA的含量高于猪左心室的AEA水平。在单独的备注中，细胞色素P450（CYP）环氧树脂酶CYP2J2是心脏中最丰富的CYP，其中它催化AA和AA衍生的ECBS的代谢和AA衍生的ECBS对来自不同的心血管功能的生物活性环氧化物。在此，使用竞争性结合研究，动力学代谢测量，分子动力学和伤口愈合测定，我们已经表明，O-AEA是CYP2J2环氧树脂的内源性抑制剂。结果，O-AEA作为CYP2J2的内源ECB抑制剂的作用可以提供新的调节模式，以控制体内心血管CYP2J2的活性，并表明心血管内瘤素和细胞色素P450系统之间的潜在串扰。

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