Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno D'Alcontres 31, 98166 Messina, Italy.
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno D'Alcontres 31, 98166 Messina, Italy; School of Medicine, 1402 South Grand Blvd, St Louis, MO 63104, USA.
Phytomedicine. 2019 Feb 15;54:27-42. doi: 10.1016/j.phymed.2018.09.191. Epub 2018 Sep 19.
Myocardial ischemia/reperfusion (I/R) injury is the principal cause of death, happens after prolonged obstruction of the coronary arteries. The first intervention to limit myocardial damage is directed to restoration of perfusion, to avoid inflammatory response and a significant oxidative stress triggered by infarction. Palmitoylethanolamide (PEA), is a well-known fatty acid amide-signaling molecule that possess an important anti-inflammatory and analgesic effects. PEA does not hold the ability to inhibit free radicals formation. Baicalein, a bioactive component isolated from a Chinese herbal medicine, has multiple pharmacological activities, such as a strong anti-oxidative effects.
A combination of PEA and Baicalein could have beneficial effects on oxidative stress produced by inflammatory response.
In the present study we explored the effects of composite containing PEA and Baicalein in a model of myocardial I/R injury.
Myocardial ischemia/reperfusion injury was induced by occlusion of the left anterior descending coronary artery for 30 min followed by 2 h of reperfusion. PEA-Baicalein (9:1), was administered (10 mg/kg) 5 min before the end of ischemia and 1 h after reperfusion.
In this study, we clearly demonstrated that PEA-Baicalein treatment decreases myocardial tissue injury, neutrophils infiltration, markers for mast cell activation expression as chymase and tryptase and pro-inflammatory cytokines production (TNF-α, IL-1β). Moreover, PEA-Baicalein treatment reduces stress oxidative and modulates Nf-kB and apoptosis pathways.
These results support the idea that the association between PEA and Baicalein should be a potent candidate for the treatment of myocardial I/R injury.
心肌缺血/再灌注（I/R）损伤是死亡的主要原因，发生在冠状动脉长时间阻塞后。限制心肌损伤的首要干预措施是恢复灌注，以避免梗塞引发的炎症反应和显著的氧化应激。棕榈酸乙醇酰胺（PEA）是一种众所周知的脂肪酸酰胺信号分子，具有重要的抗炎和镇痛作用。PEA 没有抑制自由基形成的能力。黄芩素是一种从中药中分离出来的生物活性成分，具有多种药理活性，如强烈的抗氧化作用。
PEA 和黄芩素的联合使用可能对炎症反应引起的氧化应激产生有益影响。
本研究探讨了含有 PEA 和黄芩素的复合物在心肌 I/R 损伤模型中的作用。
通过结扎左前降支冠状动脉 30 分钟后再灌注 2 小时诱导心肌缺血/再灌注损伤。在缺血结束前 5 分钟和再灌注后 1 小时给予 PEA-Baicalein（9:1）（10mg/kg）。
在这项研究中，我们清楚地表明，PEA-Baicalein 治疗可减少心肌组织损伤、中性粒细胞浸润、肥大细胞激活标志物糜蛋白酶和胰蛋白酶以及促炎细胞因子（TNF-α、IL-1β）的表达。此外，PEA-Baicalein 治疗可减轻应激氧化并调节 Nf-kB 和细胞凋亡途径。
这些结果支持 PEA 和黄芩素联合使用应该是治疗心肌 I/R 损伤的有力候选药物的观点。
