Li Ning, Liu Jun-Yan, Qiu Hong, Harris Todd R, Sirish Padmini, Hammock Bruce D, Chiamvimonvat Nipavan
Division of Cardiovascular Medicine, Department of Internal Medicine, University of California, Davis, CA, USA.
Congest Heart Fail. 2011 Jan-Feb;17(1):42-6. doi: 10.1111/j.1751-7133.2010.00209.x. Epub 2011 Jan 27.
Arachidonic acid is one of the pivotal signaling molecules associated with inflammation, pain and homeostatic function. Drugs specifically targeting these signaling pathways represent more than 25% of annual pharmaceutical sales worldwide. However, chronic administration of nonsteroidal anti-inflammatory drugs (NSAIDs) and rofecoxib (Vioxx), a potent cyclooxygenase-2 inhibitor, have been associated with adverse cardiovascular events. Understanding the possible mechanisms underlying these adverse events is critical for evaluating the risks and benefits of this group of drugs and for development of safer drugs. Using a powerful metabolomics approach, 20-hydroxyeicosatetraenoic acid (20-HETE) was identified among many of arachidonic acid metabolic products as a likely culprit for adverse cardiovascular side effect associated with rofecoxib and NSAIDs. In addition, using a similar metabolomic approach, epoxyeicosatrienoic acids (EETs), which are lipid mediators derived from arachidonic acid through the cytochrome P450 epoxygenase pathway, have been shown to exhibit cardioprotective effects in a murine myocardial infarction (MI) model. Inhibitors of the soluble epoxide hydrolase increase titers of epoxy fatty acids and both block and reverse cardiac hypertrophy in rodent models. These highly potent, orally available compounds may be promising for treating heart failure and other cardiovascular disease. In this review, we will summarize some of the recent advances using metabolomic profiling to gain insights into the involvement of arachidonic acid pathways in cardiovascular disease.
花生四烯酸是与炎症、疼痛和稳态功能相关的关键信号分子之一。专门针对这些信号通路的药物占全球年度药品销售额的25%以上。然而,长期服用非甾体抗炎药(NSAIDs)和罗非昔布(万络,一种强效的环氧化酶-2抑制剂)与不良心血管事件有关。了解这些不良事件背后的可能机制对于评估这类药物的风险和益处以及开发更安全的药物至关重要。使用强大的代谢组学方法,在许多花生四烯酸代谢产物中,20-羟基二十碳四烯酸(20-HETE)被确定为与罗非昔布和NSAIDs相关的不良心血管副作用的可能元凶。此外,使用类似的代谢组学方法,环氧二十碳三烯酸(EETs),即通过细胞色素P450环氧化酶途径从花生四烯酸衍生而来的脂质介质,已在小鼠心肌梗死(MI)模型中显示出心脏保护作用。可溶性环氧化物水解酶抑制剂可提高环氧脂肪酸的滴度,并在啮齿动物模型中阻止和逆转心脏肥大。这些高效、口服可用的化合物可能有望用于治疗心力衰竭和其他心血管疾病。在这篇综述中,我们将总结一些利用代谢组学分析来深入了解花生四烯酸途径在心血管疾病中的作用的最新进展。