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Biological activity of new bioactive steroids deriving from biotransformation of cortisone

Cortisone is a metabolite belonging to the corticosteroid class that is used pharmaceutically directly as a drug or prodrug. In addition to its large consumption, its use is linked to several side effects, so pharmaceutical research aims to develop effective drugs with low or no side effects, altern...

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Autores principales: Costa, Stefania, Tedeschi, Paola, Ferraro, Luca, Beggiato, Sarah, Grandini, Alessandro, Manfredini, Stefano, Buzzi, Raissa, Sacchetti, Gianni, Valacchi, Giuseppe
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9685055/
https://www.ncbi.nlm.nih.gov/pubmed/36419154
http://dx.doi.org/10.1186/s12934-022-01967-2
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author Costa, Stefania
Tedeschi, Paola
Ferraro, Luca
Beggiato, Sarah
Grandini, Alessandro
Manfredini, Stefano
Buzzi, Raissa
Sacchetti, Gianni
Valacchi, Giuseppe
author_facet Costa, Stefania
Tedeschi, Paola
Ferraro, Luca
Beggiato, Sarah
Grandini, Alessandro
Manfredini, Stefano
Buzzi, Raissa
Sacchetti, Gianni
Valacchi, Giuseppe
author_sort Costa, Stefania
collection PubMed
description Cortisone is a metabolite belonging to the corticosteroid class that is used pharmaceutically directly as a drug or prodrug. In addition to its large consumption, its use is linked to several side effects, so pharmaceutical research aims to develop effective drugs with low or no side effects, alternative compounds to cortisone are part of an active investment in ongoing research on drug discovery. Since biotransformation can be considered a source of new molecules with potential therapeutic use, the present work focuses on a preliminary in vitro study aimed at evaluating the mutagenic, anti-inflammatory, antioxidant and neuroprotective activity of SCA and SCB molecules obtained from the biotransformation of cortisone using Rh. Rhodnii strain DSM 43960. The results obtained are very encouraging due to the safety of biotransformed compounds with reference to genotoxicity checked by Ames test, to the very high antioxidant capacity and to the anti-inflammatory activity. In fact, thecompounds inhibited both the TNFα-stimulated expression and secretion of NFkB target cytokines, and COX activity, and can activate the glucocorticoid receptor. Finally SCA and SCB exhibited neuroprotective properties.
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spelling pubmed-96850552022-11-25 Biological activity of new bioactive steroids deriving from biotransformation of cortisone Costa, Stefania Tedeschi, Paola Ferraro, Luca Beggiato, Sarah Grandini, Alessandro Manfredini, Stefano Buzzi, Raissa Sacchetti, Gianni Valacchi, Giuseppe Microb Cell Fact Research Cortisone is a metabolite belonging to the corticosteroid class that is used pharmaceutically directly as a drug or prodrug. In addition to its large consumption, its use is linked to several side effects, so pharmaceutical research aims to develop effective drugs with low or no side effects, alternative compounds to cortisone are part of an active investment in ongoing research on drug discovery. Since biotransformation can be considered a source of new molecules with potential therapeutic use, the present work focuses on a preliminary in vitro study aimed at evaluating the mutagenic, anti-inflammatory, antioxidant and neuroprotective activity of SCA and SCB molecules obtained from the biotransformation of cortisone using Rh. Rhodnii strain DSM 43960. The results obtained are very encouraging due to the safety of biotransformed compounds with reference to genotoxicity checked by Ames test, to the very high antioxidant capacity and to the anti-inflammatory activity. In fact, thecompounds inhibited both the TNFα-stimulated expression and secretion of NFkB target cytokines, and COX activity, and can activate the glucocorticoid receptor. Finally SCA and SCB exhibited neuroprotective properties. BioMed Central 2022-11-24 /pmc/articles/PMC9685055/ /pubmed/36419154 http://dx.doi.org/10.1186/s12934-022-01967-2 Text en © The Author(s) 2022 https://creativecommons.org/licenses/by/4.0/Open AccessThis 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/) . The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/ (https://creativecommons.org/publicdomain/zero/1.0/) ) applies to the data made available in this article, unless otherwise stated in a credit line to the data.
spellingShingle Research
Costa, Stefania
Tedeschi, Paola
Ferraro, Luca
Beggiato, Sarah
Grandini, Alessandro
Manfredini, Stefano
Buzzi, Raissa
Sacchetti, Gianni
Valacchi, Giuseppe
Biological activity of new bioactive steroids deriving from biotransformation of cortisone
title Biological activity of new bioactive steroids deriving from biotransformation of cortisone
title_full Biological activity of new bioactive steroids deriving from biotransformation of cortisone
title_fullStr Biological activity of new bioactive steroids deriving from biotransformation of cortisone
title_full_unstemmed Biological activity of new bioactive steroids deriving from biotransformation of cortisone
title_short Biological activity of new bioactive steroids deriving from biotransformation of cortisone
title_sort biological activity of new bioactive steroids deriving from biotransformation of cortisone
topic Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9685055/
https://www.ncbi.nlm.nih.gov/pubmed/36419154
http://dx.doi.org/10.1186/s12934-022-01967-2
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