Antiarthritic and antiinflammatory propensity of 4-methylesculetin, a coumarin derivative

Hemshekhar, M. and Sunitha, K. and Thushara, R. M. and Sebastin Santhosh, M. and Shanmuga Sundaram, M. and Kemparaju, K. and Girish, K. S. (2013) Antiarthritic and antiinflammatory propensity of 4-methylesculetin, a coumarin derivative. Biochimie, 95 (6). pp. 1326-1335.

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Coumarins are a group of natural compounds widely distributed in plants. Of late, coumarins and their derivatives have grabbed much attention from the pharmacological and pharmaceutical arena due to their broad range of therapeutical qualities. A coumarin derivative 4-methylesculetin (4-ME) has known to possess effective antioxidant and radical-scavenging properties. Recently they have also shown to down regulate nuclear factor-kappa B (NF-κB) and protein kinase B (Akt) that play a vital role in inflammation and apoptosis. In view of this, the present study investigated the anti-arthritic potentiality of 4-ME by assessing its ability to inhibit cartilage and bone degeneration, inflammation and associated oxidative stress. Arthritis being a debilitating joint disease, results in the deterioration of extracellular matrix (ECM) of cartilage and synovium. Participation of both enzymatic and non-enzymatic factors in disease perpetuation is well documented. The present study demonstrated the mitigation of augmented serum levels of hyaluronidase and matrix metalloproteinases (MMP-13, MMP-3 and MMP-9) responsible for cartilage degeneration by 4-ME. It also protected bone resorption by reducing the elevated levels of bone-joint exoglycosidases, cathepsin-D and tartrate resistant acid phosphatases. Further, 4-ME significantly ameliorated the upregulated non-enzymatic inflammatory markers like TNF-α, IL-1β, IL-6, COX-2 and PGE2. Besides, 4-ME effectively stabilized the arthritis-induced oxidative stress by restoring the levels of reactive oxygen species, lipid and hydro peroxides and antioxidant enzymes such as superoxide dismutase, catalase and glutathione-S-transferase. Thus, the study suggests that 4-ME could be an effective agent to treat arthritis and associated secondary complications like oxidative stress. © 2013 Elsevier Masson SAS. All rights reserved.

Item Type: Article
Uncontrolled Keywords: article, male, animal experiment, animal model, controlled study, nonhuman, rat, antiinflammatory activity, unclassified drug, acid phosphatase tartrate resistant isoenzyme, Animals, arthritis, Arthritis, Cartilage, cartilage degeneration, catalase, cathepsin D, collagenase 3, Experimental, gelatinase B, glutathione transferase, hyaluronidase, ibuprofen, inflammation, Inflammation, interleukin 1beta, interleukin 6, osteolysis, oxidative stress, prostaglandin E2, Rats, reactive oxygen metabolite, stromelysin, superoxide dismutase, tumor necrosis factor alpha, Wistar, Male, Animal, animal tissue, Disease Models, Oxidative Stress, Anti-Inflammatory Agents, enzyme blood level, disease course, synovium, lipid, coumarin derivative, extracellular matrix, Coumarins, clinical evaluation, bone atrophy, 4 methylesculetin, Bone and Bones, hydroperoxide, Umbelliferones
Subjects: C Chemical Science > Biochemistry
Divisions: Department of > Biochemistry
Depositing User: Arshiya Kousar Library Assistant
Date Deposited: 14 Sep 2019 11:34
Last Modified: 14 Sep 2019 11:34

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