当前位置: X-MOL 学术RSC Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Recent development of lipoxygenase inhibitors as anti-inflammatory agents
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-11-29 00:00:00 , DOI: 10.1039/c7md00390k
Chaoyu Hu 1 , Shutao Ma 1
Affiliation  

Inflammation is favorable in most cases, because it is a kind of body defensive response to external stimuli; sometimes, inflammation is also harmful, such as attacks on the body's own tissues. It could be that inflammation is a unified process of injury and resistance to injury. Inflammation brings extreme pain to patients, showing symptoms of rubor, swelling, fever, pain and dysfunction. As the specific mechanism is not clear yet, the current anti-inflammatory agents are given priority for relieving suffering of patients. Thus it is emergent to find new anti-inflammatory agents with rapid effect. Lipoxygenase (LOX) is a kind of rate-limiting enzyme in the process of arachidonic acid metabolism into leukotriene (LT) which mediates the occurrence of inflammation. The inhibition of LOX can reduce LT, thereby producing an anti-inflammatory effect. In this review, the LOX inhibitors reported in recent years are summarized, and, in particular, their activities, structure–activity relationships and molecular docking studies are emphasized, which will provide new ideas to design novel LOX inhibitors.

中文翻译:

脂氧合酶抑制剂作为抗炎剂的最新进展

炎症在大多数情况下是有利的,因为它是身体对外界刺激的一种防御反应;有时,炎症也是有害的,比如攻击人体自身组织。炎症可能是损伤和抵抗损伤的统一过程。炎症给患者带来极度痛苦,表现为红肿、发热、疼痛和功能障碍等症状。由于具体机制尚不明确,目前抗炎药物以减轻患者痛苦为主。因此寻找新的、快速起效的抗炎药物刻不容缓。脂氧合酶(LOX)是花生四烯酸代谢为白三烯(LT)过程中的限速酶,介导炎症的发生。抑制LOX可以降低LT,从而产生抗炎作用。本文对近年来报道的LOX抑制剂进行了综述,特别重点介绍了它们的活性、构效关系和分子对接研究,为设计新型LOX抑制剂提供新思路。
更新日期:2017-11-29
down
wechat
bug