Cargando…

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 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 lipa...

Descripción completa

Detalles Bibliográficos
Autores principales: Samira, Nia, Khedidja, Benarous, Zahra, Abdelalim Fatima, Elyakine, Chellali Khadidja Nour, Mohamed, Yousfi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Bentham Science Publishers 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7579250/
https://www.ncbi.nlm.nih.gov/pubmed/31518226
http://dx.doi.org/10.2174/1871523018666190906165944
_version_ 1783598546493112320
author Samira, Nia
Khedidja, Benarous
Zahra, Abdelalim Fatima
Elyakine, Chellali Khadidja Nour
Mohamed, Yousfi
author_facet Samira, Nia
Khedidja, Benarous
Zahra, Abdelalim Fatima
Elyakine, Chellali Khadidja Nour
Mohamed, Yousfi
author_sort Samira, Nia
collection PubMed
description 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.
format Online
Article
Text
id pubmed-7579250
institution National Center for Biotechnology Information
language English
publishDate 2020
publisher Bentham Science Publishers
record_format MEDLINE/PubMed
spelling pubmed-75792502020-11-30 In silico and in vitro Study of the Inhibitory Effect of Anti-inflammatory Drug Betamethasone on Two Lipases Samira, Nia Khedidja, Benarous Zahra, Abdelalim Fatima Elyakine, Chellali Khadidja Nour Mohamed, Yousfi Antiinflamm Antiallergy Agents Med Chem Article 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. Bentham Science Publishers 2020-12 2020-12 /pmc/articles/PMC7579250/ /pubmed/31518226 http://dx.doi.org/10.2174/1871523018666190906165944 Text en © 2020 Bentham Science Publishers https://creativecommons.org/licenses/by-nc/4.0/legalcode This is an open access article licensed under the terms of the Creative Commons Attribution-Non-Commercial 4.0 International Public License (CC BY-NC 4.0) (https://creativecommons.org/licenses/by-nc/4.0/legalcode), which permits unrestricted, non-commercial use, distribution and reproduction in any medium, provided the work is properly cited.
spellingShingle Article
Samira, Nia
Khedidja, Benarous
Zahra, Abdelalim Fatima
Elyakine, Chellali Khadidja Nour
Mohamed, Yousfi
In silico and in vitro Study of the Inhibitory Effect of Anti-inflammatory Drug Betamethasone on Two Lipases
title In silico and in vitro Study of the Inhibitory Effect of Anti-inflammatory Drug Betamethasone on Two Lipases
title_full In silico and in vitro Study of the Inhibitory Effect of Anti-inflammatory Drug Betamethasone on Two Lipases
title_fullStr In silico and in vitro Study of the Inhibitory Effect of Anti-inflammatory Drug Betamethasone on Two Lipases
title_full_unstemmed In silico and in vitro Study of the Inhibitory Effect of Anti-inflammatory Drug Betamethasone on Two Lipases
title_short In silico and in vitro Study of the Inhibitory Effect of Anti-inflammatory Drug Betamethasone on Two Lipases
title_sort in silico and in vitro study of the inhibitory effect of anti-inflammatory drug betamethasone on two lipases
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7579250/
https://www.ncbi.nlm.nih.gov/pubmed/31518226
http://dx.doi.org/10.2174/1871523018666190906165944
work_keys_str_mv AT samirania insilicoandinvitrostudyoftheinhibitoryeffectofantiinflammatorydrugbetamethasoneontwolipases
AT khedidjabenarous insilicoandinvitrostudyoftheinhibitoryeffectofantiinflammatorydrugbetamethasoneontwolipases
AT zahraabdelalimfatima insilicoandinvitrostudyoftheinhibitoryeffectofantiinflammatorydrugbetamethasoneontwolipases
AT elyakinechellalikhadidjanour insilicoandinvitrostudyoftheinhibitoryeffectofantiinflammatorydrugbetamethasoneontwolipases
AT mohamedyousfi insilicoandinvitrostudyoftheinhibitoryeffectofantiinflammatorydrugbetamethasoneontwolipases