当前位置: X-MOL 学术Inflammopharmacology › 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.)
Limitations of drug concentrations used in cell culture studies for understanding clinical responses of NSAIDs
Inflammopharmacology ( IF 5.8 ) Pub Date : 2021-09-12 , DOI: 10.1007/s10787-021-00871-2
Garry G Graham 1, 2 , Kieran F Scott 3, 4
Affiliation  

In this review, the in vitro cellular effects of six nonsteroidal anti-inflammatory drugs (NSAIDs), salicylate, ibuprofen, naproxen, indomethacin, celecoxib and diclofenac, are examined. Inhibition of prostanoid synthesis in vitro generally occurs within the therapeutic range of plasma concentrations that are observed in vivo, consistent with the major action of NSAIDs being inhibition of prostanoid production. An additional probable cellular action of NSAIDs has been discovered recently, viz. decreased oxidation of the endocannabinoids, 2-arachidonoyl glycerol and arachidonyl ethanolamide. Many effects of NSAIDs, other than decreased oxidation of arachidonic acid and endocannabinoids, have been put forward but almost all of these additional processes are observed at supratherapeutic concentrations when the concentration of albumin, the major protein that binds NSAIDs, is taken into account. However, one exception is salicylate, a very potent inhibitor of the neutrophilic enzyme, myeloperoxidase, the inhibition of which leads to reduced production of the inflammatory mediator, hypochlorous acid, and inhibition of the inflammation associated with rheumatoid arthritis.



中文翻译:

细胞培养研究中用于了解 NSAID 临床反应的药物浓度限制

在这篇综述中,研究了六种非甾体抗炎药 (NSAID)、水杨酸盐、布洛芬、萘普生、消炎痛、塞来昔布和双氯芬酸的体外细胞作用。体外前列腺素合成的抑制通常发生在体内观察到的血浆浓度的治疗范围内,这与非甾体抗炎药的主要作用是抑制前列腺素的产生一致。最近发现了非甾体抗炎药的另一种可能的细胞作用,即。减少内源性大麻素、2-花生四烯酰甘油和花生四烯酰乙醇酰胺的氧化。NSAIDs 的许多作用,除了减少花生四烯酸和内源性大麻素的氧化外,已经被提出,但几乎所有这些额外的过程都在超治疗浓度下观察到,当白蛋白的浓度,考虑到结合非甾体抗炎药的主要蛋白质。然而,一个例外是水杨酸盐,它是一种非常有效的中性粒细胞酶髓过氧化物酶抑制剂,其抑制会导致炎症介质次氯酸的产生减少,并抑制与类风湿性关节炎相关的炎症。

更新日期:2021-09-13
down
wechat
bug