أعرض في EDS

Balancing antioxidant, hypolipidemic and anti-inflammatory activity in a single agent: The example of 2-hydroxy-2-substituted morpholine, 1,4-benzoxazine and 1,4-benzothiazine derivatives as a potential therapeutic approach against atherosclerosis

التفاصيل البيبلوغرافية
العنوان: Balancing antioxidant, hypolipidemic and anti-inflammatory activity in a single agent: The example of 2-hydroxy-2-substituted morpholine, 1,4-benzoxazine and 1,4-benzothiazine derivatives as a potential therapeutic approach against atherosclerosis
المؤلفون: Matralis, A.N. Bavavea, E.-I. Incerpi, S. Pedersen, J.Z. Kourounakis, A.P.
سنة النشر: 2016
الوصف: In line with our previous studies, we have developed through a rational design approach novel morpholine and benzoxa(or thia)zine lead compounds that modulate a multiplicity of targets against atherosclerosis. We have evaluated the most promising compounds for their efficiency to a) interact and scavenge free radicals, b) inhibit the metal ion (Cu2+)- induced LDL oxidation c) act intracellularly as antioxidants in THP-1 monocytes from a leukemic patient and d) inhibit the pro-inflammatory enzymes cycloxygenase-1 (COX-1) and -2 (COX-2) in vitro. Furthermore, two representative compounds were tested for their potential to decrease lipidemic parameters (TC, LDL and TG) in hyperlipidemic mice. Most derivatives indicated a remarkable antioxidant activity, while at the same time exhibited a significant in vitro anti-inflammatory activity, inhibiting COX-1 or/and COX-2 activity at 20 μM. Furthermore, after their long-term administration, compounds 6 and 8 afforded a considerable activity in a chronic experimental animal model of hyperlipidemia (after high fat diet administration). The multifunctional pharmacological profile exhibited by the compounds of this study renders them interesting lead compounds for the development of novel agents against atherosclerosis. © 2016 Bentham Science Publishers.
اللغة: English
URL الوصول: https://explore.openaire.eu/search/publication?articleId=od______2127::523054229dd6f5d5218fb8a0c50f8056
https://pergamos.lib.uoa.gr/uoa/dl/object/uoadl:3022518
حقوق: OPEN
رقم الأكسشن: edsair.od......2127..523054229dd6f5d5218fb8a0c50f8056
قاعدة البيانات: OpenAIRE
الوصف
الوصف غير متاح.