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Recent development of lipoxygenase inhibitors as anti-inflammatory agents

机译:脂氧合酶抑制剂作为抗炎药的最新进展

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摘要

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.
机译:在大多数情况下,炎症是有利的,因为它是对外部刺激的一种身体防御反应。有时,炎症也有害,例如对人体自身组织的攻击。炎症可能是伤害和抵抗伤害的统一过程。炎症给患者带来极大的痛苦,表现出红疹,肿胀,发烧,疼痛和功能障碍的症状。由于具体机制尚不清楚,因此当前的抗炎药被优先用于减轻患者的痛苦。因此出现了寻找具有快速作用的新抗炎药的迫切需求。脂氧合酶(LOX)是花生四烯酸代谢成白三烯(LT)过程中的一种限速酶,介导炎症的发生。抑制LOX可以降低LT,从而产生抗炎作用。在这篇综述中,总结了近年来报道的LOX抑制剂,特别是它们的活性,结构-活性关系和分子对接研究,这些将为设计新型LOX抑制剂提供新的思路。

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