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In vitro cytotoxic, antioxidant, hemolytic and cytoprotective potential of promising ethacrynic acid derivatives


 
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1. Title Title of document In vitro cytotoxic, antioxidant, hemolytic and cytoprotective potential of promising ethacrynic acid derivatives
 
2. Creator Author's name, affiliation, country A. Idir; Team of Experimental Oncology and Natural Substances, Cellular and Molecular Immuno-pharmacology, Faculty of Science and Technology, Sultan Moulay Slimane University, Beni-Mellal, Morocco; Morocco
 
2. Creator Author's name, affiliation, country N. Bouchmaa; Institute of Biological Sciences (ISSB-P), Mohammed VI Polytechnic University of Ben-Guerir; Morocco
 
2. Creator Author's name, affiliation, country A. El Abbouchi; Euromed Research Center, Euromed Institute of Technology, Euromed University of Fes (UEMF)–Route de Meknès, 30000 Fes, Morocco; Morocco
 
2. Creator Author's name, affiliation, country N. El Brahmi; Euromed Research Center, Euromed Institute of Technology, Euromed University of Fes (UEMF)–Route de Meknès, 30000 Fes, Morocco; Morocco
 
2. Creator Author's name, affiliation, country R. Ben Mrid; Institute of Biological Sciences (ISSB-P), Mohammed VI Polytechnic University of Ben-Guerir
 
2. Creator Author's name, affiliation, country Y. Bouargalne; Laboratory of Biochemistry and Molecular Genetics, Faculty of Sciences and Technologies of Tangier, BP 416, 90,000 Tangier, Morocco; Morocco
 
2. Creator Author's name, affiliation, country H. Ait Mouse; Team of Experimental Oncology and Natural Substances, Cellular and Molecular Immuno-pharmacology, Faculty of Science and Technology, Sultan Moulay Slimane University, Beni-Mellal, Morocco
 
2. Creator Author's name, affiliation, country M. Nhiri; Laboratory of Biochemistry and Molecular Genetics, Faculty of Sciences and Technologies of Tangier, BP 416, 90,000 Tangier, Morocco; Morocco
 
2. Creator Author's name, affiliation, country M. Bousmina; Euromed Research Center, Euromed Institute of Technology, Euromed University of Fes (UEMF)–Route de Meknès, 30000 Fes, Morocco; Morocco
 
2. Creator Author's name, affiliation, country S. El Kazzouli; Euromed Research Center, Euromed Institute of Technology, Euromed University of Fes (UEMF)–Route de Meknès, 30000 Fes, Morocco; Morocco
 
2. Creator Author's name, affiliation, country A. Zyad; Team of Experimental Oncology and Natural Substances, Cellular and Molecular Immuno-pharmacology, Faculty of Science and Technology, Sultan Moulay Slimane University, Beni-Mellal, Morocco; Morocco
 
3. Subject Discipline(s)
 
3. Subject Keyword(s) Ethacrynic acid; breast cancer; antioxidant activity; antioxidant enzymes; reactive oxygen species
 
4. Description Abstract

The present study aims to screen some pharmacological activities of three promising ethacrynic acid (EA) derivatives (P3, P4, and P5) containing a piperazine moiety. The EA derivatives were tested against MDA-MB-468 cancer cell line as a model for the triple-negative breast cancer and MCF7 cancer cell line as a model subtype of luminal breast cancer using the methyl tetrazolium test (MTT). Additionally, the modulation of the glutathione and thioredoxin enzymatic systems, as well as the antioxidant and cytoprotective potential of each compound, were investigated. Moreover, initial in vitro safety screening was conducted using human blood cells. As a result, EA derivatives showed clear dose-dependent antiproliferative activity in the micromolar range (between 1.13 and 2.51 uM), with high selectivity to cancer cells by orchestrating oxidative stress. Derivative P3 has the most promising potential for further preclinical investigation, owing to its safety profile and significant cytoprotective and antitumor properties.

 
5. Publisher Organizing agency, location
 
6. Contributor Sponsor(s)
 
7. Date (YYYY-MM-DD) 24-05-2023
 
8. Type Status & genre Peer-reviewed Article
 
8. Type Type
 
9. Format File format PDF
 
10. Identifier Uniform Resource Identifier https://revues.imist.ma/index.php/morjchem/article/view/34818
 
10. Identifier Digital Object Identifier (DOI) https://doi.org/10.48317/IMIST.PRSM/morjchem-v11i3.34818
 
11. Source Title; vol., no. (year) Moroccan Journal of Chemistry; Vol 11, No 3 (2023): pp. 579-896
 
12. Language English=en en
 
13. Relation Supp. Files
 
14. Coverage Geo-spatial location, chronological period, research sample (gender, age, etc.)
 
15. Rights Copyright and permissions Copyright (c) 2023 Moroccan Journal of Chemistry