In silico and in vitro study of the inhibitory effect of anti-inflammatory drug betamethasone on two lipases.

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Summary of "In silico and in vitro study of the inhibitory effect of anti-inflammatory drug betamethasone on two lipases."

•Background: For the first time, the anti-inflammatory drugs: celecoxib, aspirin DL-lysine, niflumic acid, naproxen sodium, ibuprofen, and betamethasone are investigated for their inhibition activity against lipase. • Objective: This work aims to demonstrate the inhibitory effect in vitro & in silico of six anti-inflammatory drugs on the enzymatic activity of two lipases. • Method: In vitro study using p-nitrophenyllaurate as lipase substrate is used to determine inhibition potency. Molecular Docking is performed using the Autodock Vina for six drug molecules and two enzymes Candida rugosa lipase and human pancreatic lipase. • Results: Bethametasone is the only one that represents an important inhibition effect with a value of IC50 of 0.36±0.01 mg/ml; while the other drugs represent values of IC50 > 2 mg/ml, signifying a very low inhibitory effect. Molecular docking allowed us to understand inhibitory - enzyme interactions and to confirm in vitro obtained results. • Conclusion: These experiments showed that betamethasone can be used in the treatment of obesity and other diseases related to lipase activity.


Journal Details

This article was published in the following journal.

Name: Anti-inflammatory & anti-allergy agents in medicinal chemistry
ISSN: 1875-614X


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Medical and Biotech [MESH] Definitions

Anti-inflammatory agents that are not steroids. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions. They are used primarily in the treatment of chronic arthritic conditions and certain soft tissue disorders associated with pain and inflammation. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects. Certain NSAIDs also may inhibit lipoxygenase enzymes or TYPE C PHOSPHOLIPASES or may modulate T-cell function. (AMA Drug Evaluations Annual, 1994, p 1814-5)

A dual inhibitor of both cyclooxygenase and lipoxygenase pathways. It exerts an anti-inflammatory effect by inhibiting the formation of prostaglandins and leukotrienes. The drug also enhances pulmonary hypoxic vasoconstriction and has a protective effect after myocardial ischemia.

A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.

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A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619)

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