Mohan Monisha, Hussain Mulla Althafh, Khan Faiz Ahmed, Anindya Roy
Department of Biotechnology, Indian Institute of Technology Hyderabad, Kandi, Sangareddy 502285, India.
Department of Chemistry, Indian Institute of Technology Hyderabad, Kandi, Sangareddy 502285, India.
Eur J Pharm Sci. 2021 May 1;160:105743. doi: 10.1016/j.ejps.2021.105743. Epub 2021 Feb 1.
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.
姜黄素是一种源自姜黄的常用草药，它通过抑制环氧化酶-1和2（COX-1和COX2）来阻断前列腺素的合成。我们最近报道了一种合成姜黄素及其类似物的有效方法。在本研究中，我们研究了16种新型姜黄素类似物抑制COX-1和COX-2的能力。我们在此报告，大多数姜黄素类似物对COX-2具有选择性抑制作用，而少数则抑制COX-1的活性。此外，我们通过分子对接研究了这些抑制剂的结合情况，发现对COX-2具有明显选择性的化合物与COX-2的结合比姜黄素更好。
