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丙酮酸乙酯是一种用于治疗多种炎症性器官损伤的新型抗炎剂。

Ethyl pyruvate is a novel anti-inflammatory agent to treat multiple inflammatory organ injuries.

作者信息

Yang Runkuan, Zhu Shengtao, Tonnessen Tor Inge

机构信息

Department of Intensive Care Medicine, Tampere University Hospital, University of Tampere, 10 Bio katu, Tampere, 33014 Finland ; Department of Critical Care Medicine, University of Pittsburgh Medical School, 3550 Terrace Street, Pittsburgh, PA 15261 USA ; Department of Emergencies and Critical Care, Rikshospital of Oslo University, PO Box 4950, Nydalen, Oslo 0424 Norway.

Department of Gastroenterology, Beijing Friendship Hospital, Capital Medical University, 95 Yong An Road, Beijing, 100050 China.

出版信息

J Inflamm (Lond). 2016 Dec 3;13:37. doi: 10.1186/s12950-016-0144-1. eCollection 2016.

Abstract

Ethyl pyruvate (EP) is a simple derivative of pyruvic acid, which is an important endogenous metabolite that can scavenge reactive oxygen species (ROS). Treatment with EP is able to ameliorate systemic inflammation and multiple organ dysfunctions in multiple animal models, such as acute pancreatitis, alcoholic liver injury, acute respiratory distress syndrome (ARDS), acute viral myocarditis, acute kidney injury and sepsis. Recent studies have demonstrated that prolonged treatment with EP can ameliorate experimental ulcerative colitis and slow multiple tumor growth. It has become evident that EP has pharmacological anti-inflammatory effect to inhibit multiple early inflammatory cytokines and the late inflammatory cytokine HMGB1 release, and the anti-tumor activity is likely associated with its anti-inflammatory effect. EP has been tested in human volunteers and in a clinical trial of patients undergoing cardiac surgery in USA and shown to be safe at clinical relevant doses, even though EP fails to improve outcome of the heart surgery, EP is still a promising agent to treat patients with multiple inflammatory organ injuries and the other clinical trials are on the way. This review focuses on how EP is able to ameliorate multiple organ injuries and summarize recently published EP investigations. Graphical AbstractThe targets of the anti-inflammatory agent EP.

摘要

丙酮酸乙酯(EP)是丙酮酸的一种简单衍生物,丙酮酸是一种重要的内源性代谢产物,能够清除活性氧(ROS)。在多种动物模型中,如急性胰腺炎、酒精性肝损伤、急性呼吸窘迫综合征(ARDS)、急性病毒性心肌炎、急性肾损伤和脓毒症,用EP进行治疗能够改善全身炎症和多器官功能障碍。最近的研究表明,长期用EP治疗可以改善实验性溃疡性结肠炎,并减缓多种肿瘤的生长。显而易见,EP具有药理学抗炎作用,可抑制多种早期炎症细胞因子和晚期炎症细胞因子高迁移率族蛋白B1(HMGB1)的释放,其抗肿瘤活性可能与其抗炎作用有关。EP已在美国的人体志愿者和心脏手术患者的临床试验中进行了测试,结果表明在临床相关剂量下是安全的,尽管EP未能改善心脏手术的预后,但它仍是治疗多器官炎症损伤患者的一种有前景的药物,其他临床试验也正在进行中。本综述重点关注EP如何改善多器官损伤,并总结最近发表的关于EP的研究。图形摘要抗炎剂EP的靶点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9861/5135784/0ff0a1a4fead/12950_2016_144_Figa_HTML.jpg

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