姜黄素单羰基类似物抗炎作用的研究

A. A. Nagargoje, Satish V Akolkar, M. Shaikh, H. Akolkar, D. Raut, Parshuram M. Pisal, V. Khedkar, B. Shingate
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引用次数: 2

摘要

摘要本文报道了姜黄素单羰基类似物的合成、抗炎活性和分子对接。以双氯芬酸钠为参比标准物,采用蛋白变性法测定合成化合物的抗炎活性。其中,3d、3e、3f、3j、3k、3l和3m与标准DFS相比,具有良好的百分比抑制范围,表现出良好的抗炎活性。对环氧合酶(COX-2)的硅结合亲和性研究可以为其可能的作用机制提供有价值的见解。此外,合成的单羰基姜黄素类似物的ADME预测显示出良好的药代动力学参数,不违反Lipinski的五定律。图形抽象
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Investigation of the Anti-inflammatory potential of Mono-carbonyl Analogues of Curcumin
Abstract In the present investigation, we report the synthesis, anti-inflammatory activity and molecular docking of monocarbonyl analogues of curcumin. The anti-inflammatory activity of the synthesized compounds was gauzed using the protein denaturation assay using Diclofenac sodium as reference standard. Among the tested compounds, 3d, 3e, 3f, 3j, 3k, 3l and 3m displayed excellent anti-inflammatory activity by exhibiting good range of percentage inhibition as compared to the standard DFS. In silico binding affinity study against Cyclooxygenase (COX-2) enzyme could provide valuable insight into their plausible mechanism of action. Also, in silico ADME prediction of synthesized monocarbonyl curcumin analogues showed excellent pharmacokinetic parameters by not violating Lipinski’s rule of five. GRAPHICAL ABSTRACT
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CiteScore
2.30
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