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Symmetrical and un-symmetrical curcumin analogues as selective COX-1 and COX-2 inhibitor.
- Source :
-
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [Eur J Pharm Sci] 2021 May 01; Vol. 160, pp. 105743. Date of Electronic Publication: 2021 Feb 01. - Publication Year :
- 2021
-
Abstract
- Curcumin, a popular herbal medicine derived from turmeric, blocks the synthesis of prostaglandins by inhibiting Cyclooxygenase-1 and 2 (COX-1 and COX2). We have recently reported an efficient method of synthesizing curcumin and synthesised analogues. In the present study, we have investigated sixteen novel analogues of curcumin for their ability to inhibit COX-1 and COX-2. We report here that most of the curcumin analogues display selective inhibition of COX-2, whereas a few suppress COX-1 activity. Further, we examined the binding of these inhibitors by molecular docking and observed that the compound with pronounced selectivity for COX-2 displayed better binding to COX-2 compared to curcumin.<br /> (Copyright © 2021 Elsevier B.V. All rights reserved.)
Details
- Language :
- English
- ISSN :
- 1879-0720
- Volume :
- 160
- Database :
- MEDLINE
- Journal :
- European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
- Publication Type :
- Academic Journal
- Accession number :
- 33540041
- Full Text :
- https://doi.org/10.1016/j.ejps.2021.105743