The design of novel anti-inflammatory drugs remains a critical area of research in the development of effective treatments for inflammatory diseases. In this study, a series of 1,2-benzothiazine was evaluated through a multifaceted approach. In particular, we investigated the potential interactions of the potential drugs with lipid bilayers, an important consideration for membrane permeability and overall pharmacokinetics. In addition, we evaluated their ability to inhibit cyclooxygenase 1 and cyclooxygenase 2 activity and selectivity using both a cyclooxygenase inhibition assay and molecular docking simulations. To evaluate their therapeutic potential, we performed in vitro assays to measure cytokine mRNA expression in inflamed cells. The antioxidant activity was evaluated using both in vitro assays, such as 2,2-diphenyl-1-picrylhydrazyl and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid scavenging, to determine the compounds' capacity to neutralize free radicals and reduce oxidative stress. Theoretical calculations, including density functional theory, were used to predict the reactivity profiles of the compounds.
Anti-Inflammatory Properties of Novel 1,2-Benzothiazine Derivatives and Their Interaction with Phospholipid Model Membranes.
新型1,2-苯并噻嗪衍生物的抗炎特性及其与磷脂模型膜的相互作用
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作者:SzczÄÅniak-SiÄga Berenika M, Maniewska Jadwiga, Wiatrak Benita, Janek Tomasz, Nowotarska Paulina, Czyżnikowska Å»aneta
| 期刊: | Membranes | 影响因子: | 3.600 |
| 时间: | 2024 | 起止号: | 2024 Dec 18; 14(12):274 |
| doi: | 10.3390/membranes14120274 | 研究方向: | 免疫/内分泌 |
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