Symmetrical and un-symmetrical curcumin analogues as selective COX-1 and COX-2 inhibitor

Mohan, Monisha and Hussain, Mulla Althafh and Khan, Faiz Ahmed and Anindya, Roy (2021) Symmetrical and un-symmetrical curcumin analogues as selective COX-1 and COX-2 inhibitor. European Journal of Pharmaceutical Sciences, 160. p. 105743. ISSN 09280987

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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.

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IITH Creators:

IITH Creators	ORCiD
Mohan, Monisha	UNSPECIFIED
Hussain, Mulla Althafh	UNSPECIFIED
Khan, Faiz Ahmed	UNSPECIFIED
Anindya, Roy	UNSPECIFIED

Item Type:

Article

Uncontrolled Keywords:

Article; binding affinity; complex formation; controlled study; drug protein binding; drug selectivity; drug synthesis; enzyme active site; enzyme inhibition; enzyme repression; hydrogen bond; IC50; molecular docking; priority journal

Subjects:

Others > Biotechnology

Divisions:

Department of Biotechnology

Depositing User:

. LibTrainee 2021

Date Deposited:

08 Jul 2021 06:37

Last Modified:

08 Jul 2021 06:37

URI:

http://raiithold.iith.ac.in/id/eprint/8173