From the news
- Chancellor Amma Addresses the Parliament of World’s Religions
- Amrita Students Qualify for the European Mars Rover Challenge
Publication Type : Journal Article
Thematic Areas : Nanosciences and Molecular Medicine
Publisher : Bioorganic Medicinal Chemistry Letters
Source : Bioorganic & Medicinal Chemistry Letters, Volume 21, Number 6, p.1612 - 1616 (2011)
Keywords : anti-inflammatory, antioxidant, Chromones, Cyclooxygenase (COX)-1 and -2, molecular docking, Stellatin
Campus : Kochi
School : Center for Nanosciences
Center : Amrita Center for Nanosciences and Molecular Medicine Move, Nanosciences
Department : Nanosciences and Molecular Medicine
Year : 2011
Abstract : Stellatin (4), isolated from Dysophylla stellata is a cyclooxygenase (COX) inhibitor. The present study reports the synthesis and biological evaluation of new stellatin derivatives for COX-1, COX-2 inhibitory and anti-inflammatory activities. Eight derivatives showed more pronounced COX-2 inhibition than stellatin and, 17 and 21 exhibited the highest COX-2 inhibition. They also exhibited the significant anti-inflammatory activity in TPA-induced mouse ear edema assay and their anti-inflammatory effects were more than that of stellatin and indomethacin at 0.5mg/ear. The derivatives were further evaluated for antioxidant activity wherein 16 and 17 showed potent free radical scavenging activity against DPPH and ABTS radicals. Molecular docking study revealed the binding orientations of stellatin and its derivatives into the active sites of COX-1 and COX-2 and thereby helps to design the potent inhibitors.
Cite this Research Publication : R. Gautam, Jachak, S. M., Kumar, V., and Dr. Gopi Mohan C., “Synthesis, Biological Evaluation and Molecular Docking Studies of Stellatin Derivatives as Cyclooxygenase (COX-1, COX-2) Inhibitors and Anti-inflammatory Agents”, Bioorganic & Medicinal Chemistry Letters, vol. 21, pp. 1612 - 1616, 2011.