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塞来昔布和安吡昔康瓜氨酸酯的潜在抗氧化活性:体外研究

Potential antioxidant activity of celecoxib and amtolmetin guacyl: in vitro studies.

作者信息

Kirkova M, Alexandova A, Kesiova M, Tsvetanova E, Georgieva A, Todorov S

机构信息

Institute of Physiology, Bulgarian Academy of Sciences, 23 Acad. G. Bonchev st, 1113 Sofia, Bulgaria.

出版信息

Auton Autacoid Pharmacol. 2007 Jan;27(1):13-8. doi: 10.1111/j.1474-8673.2006.00391.x.

Abstract
  1. In vitro studies of the potential antioxidant activity of the selective cyclo-oxygenase-2 inhibitor celecoxib and the non-steroid anti-inflammatory drug amtolmetin guacyl (AMG) were carried out. The study included experiments on the ability of these drugs to affect some indices of the oxidative stress [lipid peroxidation (LP), activity of antioxidant enzymes, glutathione (GSH) level] in rat stomach and colon mucosa and in liver. 2. Celecoxib and AMG did not change the activity of the enzymes GSH-peroxidase, oxidased glutathione (GSSG)-reductase and glucose-6-phosphate-dehydrogenase, as well as the GSH level in all tissue preparations. An increased superoxide dismutase (SOD) activity and a tendency to a decreased Fe/ascorbic acid-induced LP in stomach and colon mucosa were found, but only in the presence of AMG. 3. In the liver, both celecoxib and AMG decreased spontaneous and Fe/ascorbic acid-induced LP. SOD activity was enhanced only in the presence of AMG. 4. Experiments aimed at studying celecoxib and AMG in free oxygen radical-generating systems were also carried out. AMG and tolmetin (the main metabolite of AMG) inhibited OH*-provoked deoxyribose degradation in a Fenton system. Celecoxib had no effect on free radicals when tested in the same system. 5. In conclusion, the results of the present in vitro studies suggest that AMG and celecoxib possess antioxidant and metal-chelating abilities, which might contribute to their beneficial effects.
摘要
  1. 开展了选择性环氧化酶-2抑制剂塞来昔布和非甾体抗炎药安托尔美汀胍基(AMG)潜在抗氧化活性的体外研究。该研究包括这些药物对大鼠胃、结肠黏膜及肝脏氧化应激的某些指标[脂质过氧化(LP)、抗氧化酶活性、谷胱甘肽(GSH)水平]影响的实验。2. 塞来昔布和AMG均未改变所有组织制剂中谷胱甘肽过氧化物酶、氧化型谷胱甘肽(GSSG)还原酶和葡萄糖-6-磷酸脱氢酶的活性以及GSH水平。发现超氧化物歧化酶(SOD)活性增加,且胃和结肠黏膜中Fe/抗坏血酸诱导的LP有降低趋势,但仅在存在AMG时出现。3. 在肝脏中,塞来昔布和AMG均降低了自发的以及Fe/抗坏血酸诱导的LP。仅在存在AMG时SOD活性增强。4. 还开展了旨在研究塞来昔布和AMG在自由基生成系统中的实验。AMG和托美汀(AMG的主要代谢产物)在芬顿系统中抑制OH*引发的脱氧核糖降解。在同一系统中测试时,塞来昔布对自由基无影响。5. 总之,目前体外研究结果表明,AMG和塞来昔布具有抗氧化和金属螯合能力,这可能有助于它们产生有益作用。

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