A. A. Nagargoje, Satish V Akolkar, M. Shaikh, H. Akolkar, D. Raut, Parshuram M. Pisal, V. Khedkar, B. Shingate
{"title":"Investigation of the Anti-inflammatory potential of Mono-carbonyl Analogues of Curcumin","authors":"A. A. Nagargoje, Satish V Akolkar, M. Shaikh, H. Akolkar, D. Raut, Parshuram M. Pisal, V. Khedkar, B. Shingate","doi":"10.1080/22297928.2022.2132877","DOIUrl":null,"url":null,"abstract":"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","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"33 1","pages":"586 - 598"},"PeriodicalIF":0.0000,"publicationDate":"2022-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Analytical Chemistry Letters","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1080/22297928.2022.2132877","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 2
Abstract
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
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
