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植物源 mPGES-1 抑制剂或调节剂:小分子抗炎症治疗的新趋势。

Plant-derived mPGES-1 inhibitors or suppressors: A new emerging trend in the search for small molecules to combat inflammation.

机构信息

Department of Pharmacy, Abdul Wali Khan University Mardan, 23200, Pakistan.

REEF Environmental Consultancy, #2 Kamaraj Street, S.P. Nagar, Puducherry 605 001, India.

出版信息

Eur J Med Chem. 2018 Jun 10;153:2-28. doi: 10.1016/j.ejmech.2017.12.059. Epub 2017 Dec 23.

DOI:10.1016/j.ejmech.2017.12.059
PMID:29329790
Abstract

Inflammation comprises the reaction of the body to injury, in which a series of changes of the terminal vascular bed, blood, and connective tissue tends to eliminate the injurious agent and to repair the damaged tissue. It is a complex process, which involves the release of diverse regulatory mediators. The current anti-inflammatory agents are challenged by multiple side effects and thus, new effective therapies are highly needed. The aim of this review is to summarize the described microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors or transcriptional suppressors from medicinal plants, which could be an ideal approach in the management of inflammatory disorders, but need further clinical trials in order to be ultimately validated.

摘要

炎症包括机体对损伤的反应,其中终末血管床、血液和结缔组织的一系列变化旨在消除有害因子并修复受损组织。这是一个复杂的过程,涉及多种调节介质的释放。目前的抗炎药物存在多种副作用的挑战,因此,非常需要新的有效治疗方法。本综述的目的是总结从药用植物中描述的微粒体前列腺素 E 合酶-1(mPGES-1)抑制剂或转录抑制剂,这可能是治疗炎症性疾病的理想方法,但需要进一步的临床试验来最终验证。

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Plant-derived mPGES-1 inhibitors or suppressors: A new emerging trend in the search for small molecules to combat inflammation.植物源 mPGES-1 抑制剂或调节剂:小分子抗炎症治疗的新趋势。
Eur J Med Chem. 2018 Jun 10;153:2-28. doi: 10.1016/j.ejmech.2017.12.059. Epub 2017 Dec 23.
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Structure-based discovery of mPGES-1 inhibitors suitable for preclinical testing in wild-type mice as a new generation of anti-inflammatory drugs.基于结构的 mPGES-1 抑制剂发现,适合在野生型小鼠中进行临床前测试,作为新一代抗炎药物。
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