Investigation of the Anti-inflammatory potential of Mono-carbonyl Analogues of Curcumin

被引：4
|
作者：
Nagargoje, Amol A. [1 ,2 ]
Akolkar, Satish V. [1 ]
Shaikh, Mubarak H. [1 ,3 ]
Akolkar, Hemant Kumar N. [3 ]
Raut, Deepak N. [4 ]
Pisal, Parshuram M. [5 ]
Khedkar, Vijay M. [6 ]
Shingate, Bapurao B. [1 ]
机构：
[1] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem, Aurangabad 431004, India
[2] Khopoli Municipal Council Coll, Dept Chem, Khopoli 410203, India
[3] Radhabai Kale Mahila Mahavidyalaya, Ahmednagar 414001, India
[4] Amrutvahini Coll Pharm, Sangamner 422605, India
[5] Punyashlok Ahilyadevi Holkar Solapur Univ, Sch Chem Sci, Solapur 413255, India
[6] Vishwakarma Univ, Sch Pharm, Pune 411048, India
来源：
ANALYTICAL CHEMISTRY LETTERS | 2022年 / 12卷 / 05期
关键词：
Monocarbonyl Curcumin analogues; Anti-inflammatory evaluation; Cyclooxygenase; Molecular docking; DERIVATIVES; INHIBITION;
D O I：
10.1080/22297928.2022.2132877
中图分类号：
O65 [分析化学];
学科分类号：
070302 ; 081704 ;
摘要：
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.
引用
收藏
页码：586 / 598
页数：13
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