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In vitro and in vivo assessment of the antioxidant potential of isoxazole derivatives

Previously developed fluorophenyl-isoxazole-carboxamides derivatives were re-synthesized and their scavenging activity against DPPH free radical and inhibitory activity against lipase and α-amylase enzymes were evaluated. The inhibition of the tested enzymes was weak while the most potent activities...

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Autores principales: Hawash, Mohammed, Jaradat, Nidal, Abualhasan, Murad, Thaher, Manar, Sawalhi, Rawan, Younes, Nadeen, Shanaa, Amani, Nuseirat, Mariam, Mousa, Ahmed
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9617852/
https://www.ncbi.nlm.nih.gov/pubmed/36309576
http://dx.doi.org/10.1038/s41598-022-23050-x
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author Hawash, Mohammed
Jaradat, Nidal
Abualhasan, Murad
Thaher, Manar
Sawalhi, Rawan
Younes, Nadeen
Shanaa, Amani
Nuseirat, Mariam
Mousa, Ahmed
author_facet Hawash, Mohammed
Jaradat, Nidal
Abualhasan, Murad
Thaher, Manar
Sawalhi, Rawan
Younes, Nadeen
Shanaa, Amani
Nuseirat, Mariam
Mousa, Ahmed
author_sort Hawash, Mohammed
collection PubMed
description Previously developed fluorophenyl-isoxazole-carboxamides derivatives were re-synthesized and their scavenging activity against DPPH free radical and inhibitory activity against lipase and α-amylase enzymes were evaluated. The inhibition of the tested enzymes was weak while the most potent activities were observed in the DPPH assay. In particular, compounds 2a and 2c demonstrated high antioxidant potency with IC(50) values of 0.45 ± 0.21 and 0.47 ± 0.33 µg/ml, respectively, when compared to Trolox, the positive control compound, which has an IC(50) value of 3.10 ± 0.92 µg/ml. Based on the in vitro results, the most potent compound 2a was chosen for in vivo evaluation of antioxidant properties using 20 male mice injected intra-peritoneally and divided into four groups. The in vivo results revealed that total antioxidant capacity (TAC) obtained for mice treated with 2a was two folds greater than that of mice treated with the positive control Quercetin. Although further biological and preclinical investigations need to be performed to assess the therapeutic potential of 2a, the results of this study show promising antioxidant activities both in vitro and in vivo.
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spelling pubmed-96178522022-10-31 In vitro and in vivo assessment of the antioxidant potential of isoxazole derivatives Hawash, Mohammed Jaradat, Nidal Abualhasan, Murad Thaher, Manar Sawalhi, Rawan Younes, Nadeen Shanaa, Amani Nuseirat, Mariam Mousa, Ahmed Sci Rep Article Previously developed fluorophenyl-isoxazole-carboxamides derivatives were re-synthesized and their scavenging activity against DPPH free radical and inhibitory activity against lipase and α-amylase enzymes were evaluated. The inhibition of the tested enzymes was weak while the most potent activities were observed in the DPPH assay. In particular, compounds 2a and 2c demonstrated high antioxidant potency with IC(50) values of 0.45 ± 0.21 and 0.47 ± 0.33 µg/ml, respectively, when compared to Trolox, the positive control compound, which has an IC(50) value of 3.10 ± 0.92 µg/ml. Based on the in vitro results, the most potent compound 2a was chosen for in vivo evaluation of antioxidant properties using 20 male mice injected intra-peritoneally and divided into four groups. The in vivo results revealed that total antioxidant capacity (TAC) obtained for mice treated with 2a was two folds greater than that of mice treated with the positive control Quercetin. Although further biological and preclinical investigations need to be performed to assess the therapeutic potential of 2a, the results of this study show promising antioxidant activities both in vitro and in vivo. Nature Publishing Group UK 2022-10-29 /pmc/articles/PMC9617852/ /pubmed/36309576 http://dx.doi.org/10.1038/s41598-022-23050-x Text en © The Author(s) 2022 https://creativecommons.org/licenses/by/4.0/Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) .
spellingShingle Article
Hawash, Mohammed
Jaradat, Nidal
Abualhasan, Murad
Thaher, Manar
Sawalhi, Rawan
Younes, Nadeen
Shanaa, Amani
Nuseirat, Mariam
Mousa, Ahmed
In vitro and in vivo assessment of the antioxidant potential of isoxazole derivatives
title In vitro and in vivo assessment of the antioxidant potential of isoxazole derivatives
title_full In vitro and in vivo assessment of the antioxidant potential of isoxazole derivatives
title_fullStr In vitro and in vivo assessment of the antioxidant potential of isoxazole derivatives
title_full_unstemmed In vitro and in vivo assessment of the antioxidant potential of isoxazole derivatives
title_short In vitro and in vivo assessment of the antioxidant potential of isoxazole derivatives
title_sort in vitro and in vivo assessment of the antioxidant potential of isoxazole derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9617852/
https://www.ncbi.nlm.nih.gov/pubmed/36309576
http://dx.doi.org/10.1038/s41598-022-23050-x
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