Selvam C, Jachak Sanjay M, Thilagavathi Ramasamy, Chakraborti Asit K
Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, SAS Nagar, Punjab 160 062, India.
Bioorg Med Chem Lett. 2005 Apr 1;15(7):1793-7. doi: 10.1016/j.bmcl.2005.02.039.
Curcuminoids were isolated from Curcuma longa and their pyrazole and isoxazole analogues were synthesized and evaluated for antioxidant, COX-1/COX-2 inhibitory and anti-inflammatory activities. The designed analogues significantly enhance COX-2/COX-1 selectivity and possess significant anti-inflammatory activity in carrageenan induced rat paw edema assay. Pyrazole, isoxazole analogues of curcumin (4 and 7) exhibited higher antioxidant activity than trolox. Molecular docking study revealed the binding orientations of curcumin analogues in the active sites of COX and thereby helps to design novel potent inhibitors.
从姜黄中分离出姜黄素类化合物，并合成了它们的吡唑和异恶唑类似物，对其抗氧化、COX - 1/COX - 2抑制和抗炎活性进行了评估。所设计的类似物显著提高了COX - 2/COX - 1的选择性，并且在角叉菜胶诱导的大鼠足爪水肿试验中具有显著的抗炎活性。姜黄素的吡唑、异恶唑类似物（4和7）表现出比Trolox更高的抗氧化活性。分子对接研究揭示了姜黄素类似物在COX活性位点的结合取向，从而有助于设计新型强效抑制剂。
