Generic placeholder image

Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry


ISSN (Print): 1871-5230
ISSN (Online): 1875-614X

Research Article

In silico and in vitro Study of the Inhibitory Effect of Antiinflammatory Drug Betamethasone on Two Lipases

Author(s): Nia Samira*, Benarous Khedidja, Abdelalim Fatima Zahra, Chellali Khadidja Nour Elyakine and Yousfi Mohamed

Volume 19, Issue 4, 2020

Page: [387 - 392] Pages: 6

DOI: 10.2174/1871523018666190906165944


Background: For the first time, the anti-inflammatory drug betamethasone is investigated for its inhibitory activity against lipase.

Objective: This work aims to demonstrate the in vitro and in silico inhibitory effect of the anti-inflammatory drug betamethasone on the enzymatic activity of two lipases.

Methods: In vitro study using p-nitrophenyllaurate as lipase substrate is used to determine inhibition potency. Molecular Docking is performed using the Autodock Vina for drug molecule and two enzymes Candida rugosa lipase and human pancreatic lipase.

Results: Betamethasone represents a moderate inhibition effect with a value of IC50 of 0.36±0.01 mg/ml. 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 diseases related to lipase activity.

Keywords: Anti-inflammatory drugs, autodock vina, betamethasone, Candida rugosa, human pancreatic lipase, diseases related to lipase, inhibition, lipase, molecular docking.

Graphical Abstract
Nebeg, H.; Benarous, K.; Serseg, T.; Lazreg, A.; Hassani, H.; Yousfi, M. Seeds, leaves and roots of Thapsia garganica as a source of new potent lipases inhibitors: in vitro and in silico studies. Endocr. Metab. Immune Disord. Drug Targets, 2019, 19(5), 683-696.
[] [PMID: 30706829]
Nia, S.; Benguechoua, M.; Benarous, K.; Khacheba, I.; Chérif, J.K.; Trabelsi-Ayadi, M.; Yousfi, M. Screening of two Algerian spontaneous plants for anti-lipase and antioxidant activities. Curr. Enzym. Inhib., 2014, 10, 113-120.
Khedidja, B.; Madjda, B.; Abderrahmane, G. Antiallergy drugs as potent inhibitors of lipase with structure-activity relationships and molecular docking. Antiinflamm. Antiallergy Agents Med. Chem., 2018, 17(2), 95-101.
[] [PMID: 30198443]
Benguechoua, M.; Nia, S.; Benarous, K.; Khachba, I.; Yousfi, M. Inhibition of Candida rugosa lipase by different extracts of five Algerian plants and their antioxidant activities. Curr. Enzym. Inhib., 2014, 10, 121-128.
Serseg, T.; Benarous, K. The inhibitory effect of some drugs on Candida rugosa lipase and human pancreatic lipase: in vitro and in silico studies. Endocr. Metab. Immune Disord. Drug Targets, 2018, 18(6), 602-609.
[] [PMID: 29557755]
Jawed, A.; Singh, G.; Kohli, S.; Sumera, A.; Haque, S.; Parasad, R.; Paul, D. Therapeutic role of lipases and lipase inhibitors derived from natural resources for remedies against metabolic disorders and lifestyle diseases. S. Afr. J. Bot., 2019, 120, 25-32.
Panwar, U.; Singh, S.K. Identification of novel pancreatic lipase inhibitors using in silico studies. Endocr. Metab. Immune Disord. Drug Targets, 2019, 19, 449-457.
Sharma, N.; Sharma, V.K.; Seo, S.Y. Screening of some medicinal plants for anti-lipase activity. J. Ethnopharmacol., 2005, 97(3), 453-456.
[] [PMID: 15740880]
Alansari, W.S. Comparative biochemical study on the effect of ginger, orlistat or chitosan on obesity in experimental animals. Med. Sci., 2019, 23(98), 523-531.
Charlier, C.; Michaux, C. Dual inhibition of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) as a new strategy to provide safer non-steroidal anti-inflammatory drugs. Eur. J. Med. Chem., 2003, 38(7-8), 645-659.
[] [PMID: 12932896]
Benarous, K.; Bombarda, I.; Iriepa, I.; Moraleda, I.; Gaetan, H.; Linani, A.; Tahri, D.; Sebaa, M.; Yousfi, M. Harmaline and hispidin from Peganum harmala and Inonotus hispidus with binding affinity to Candida rugosa lipase: in silico and in vitro studies. Bioorg. Chem., 2015, 62, 1-7.
[] [PMID: 26151548]
Serseg, T.; Benarous, K.; Yousfi, M. The inhibitory effect of three essential oils on Candida rugosa lipase: in vitro and in silico studies. Nat. Prod. J., 2019, 10(3), 208-215.
Morris, G.M.; Huey, R.; Lindstrom, W.; Sanner, M.F.; Belew, R.K.; Goodsell, D.S.; Olson, A.J. AutoDock4 and AutoDockTools4: Automated docking with selective receptor flexibility. J. Comput. Chem., 2009, 30(16), 2785-2791.
[] [PMID: 19399780]
Trott, O.; Olson, A.J. AutoDock Vina: improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading. J. Comput. Chem., 2010, 31(2), 455-461.
[PMID: 19499576]
Dassault Systèmes, B.I.O.V.I.A. Discovery Studio Modeling Environment, Release 2017. San Diego: USA, , 2016.

© 2022 Bentham Science Publishers | Privacy Policy