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Antiproliferative Activities of Lipophililic Fluoroquinolones-Based Scaffold Against a Panel of Solid and Liquid Cancer Cell Lines

OBJECTIVES: In this work, 9 lipophilic-acid chelating FQs (fluoroquinolones) comprising chelating groups have been prepared, characterized and screened for in vitro cytotoxicity, radical scavenging and antiinflammation propensities. METHODS: Using sulforhodamine B colorimetric bioassay vs. cisplatin...

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Autores principales: Qashou, Esraa, Al-Hiari, Yusuf, Kasabri, Violet, AlBashiti, Rabab, AlAlawi, Sundus, Telfah, Ahmad, AlHadid, Amani
Formato: Online Artículo Texto
Lenguaje:English
Publicado: West Asia Organization for Cancer Prevention 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9587871/
https://www.ncbi.nlm.nih.gov/pubmed/35633535
http://dx.doi.org/10.31557/APJCP.2022.23.5.1529
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author Qashou, Esraa
Al-Hiari, Yusuf
Kasabri, Violet
AlBashiti, Rabab
AlAlawi, Sundus
Telfah, Ahmad
AlHadid, Amani
author_facet Qashou, Esraa
Al-Hiari, Yusuf
Kasabri, Violet
AlBashiti, Rabab
AlAlawi, Sundus
Telfah, Ahmad
AlHadid, Amani
author_sort Qashou, Esraa
collection PubMed
description OBJECTIVES: In this work, 9 lipophilic-acid chelating FQs (fluoroquinolones) comprising chelating groups have been prepared, characterized and screened for in vitro cytotoxicity, radical scavenging and antiinflammation propensities. METHODS: Using sulforhodamine B colorimetric bioassay vs. cisplatin; FQs-inflicted reductions’ of viability against breast T47D and MCF7, Pancreatic PANC-1, colorectal HT29, HCT116, SW620, CACO2, SW480 and Leukaemia K562 cancer cell lines were examined in quadruplicates/dose/cell line. Parameters including potency, toxicity, and selectivity (potency/toxicity) have been reported along with DPPH- and NO- radicals’ scavenging capacities -as their molecular action mechanism- in comparison to ascorbic acid and indomethacin respectively. Using Griess assay in Lipopolysaccharide (LPS) prompted RAW264.7 macrophages; mitigation of inflammation was investigated. RESULTS: nitroFQ 3b, unlike the rest of FQs in PANC1 and MCF7 cells, exhibited remarkably superior NO-radical scavenging/antiinflammation capacity to indomethacin with respective antiproliferative IC(50) values (<50µM) 49 vs. cisplatin’s 122 and 6 vs. cisplatin’s 28 (p<0.01-0.001; n=4). Reduced FQ 4b of significantly dual DPPH-NO scavenging propensities exerted exceptionally substantial micromolar antiproliferation in colorectal cancer cells with respective antiproliferative IC(50) values (<50µM) of HCT116 0.84< HT29 1.6<PANC1 5.7<SW620 9.2 vs. cisplatins’, (p<0.01-0.001; n=4). FQ 5a of superb NO radical reduction effect had antiproliferative IC(50) value (<50µM) of 37.6 in PANC1 cells. In breast cancer T47D the ascending order of pronounced nano-micromolar antiproliferative IC(50) values (<50µM) was 4d<3d<4a<4b<3b (0.009<0.59<10<15<41 vs. cisplatins’, p<0.01-0.001; n=4). Both 4d and 4b displayed both DPPH-NO radicals reduction –related cytotoxicities. NO radical scavengers 3d and 3b as well as DPPH radical scavenger 4a exerted highly appreciably relevant antineoplastic affinities. CONCLUSION: Acidic groups and C8-C7 ethylene diamine Chelation Bridge along with bulky dual halogenations can be substantially associated with molecular action mechanisms of FQs cytotoxicities, antioxidative and antiinflammation effects, collectively.
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spelling pubmed-95878712022-10-28 Antiproliferative Activities of Lipophililic Fluoroquinolones-Based Scaffold Against a Panel of Solid and Liquid Cancer Cell Lines Qashou, Esraa Al-Hiari, Yusuf Kasabri, Violet AlBashiti, Rabab AlAlawi, Sundus Telfah, Ahmad AlHadid, Amani Asian Pac J Cancer Prev Research Article OBJECTIVES: In this work, 9 lipophilic-acid chelating FQs (fluoroquinolones) comprising chelating groups have been prepared, characterized and screened for in vitro cytotoxicity, radical scavenging and antiinflammation propensities. METHODS: Using sulforhodamine B colorimetric bioassay vs. cisplatin; FQs-inflicted reductions’ of viability against breast T47D and MCF7, Pancreatic PANC-1, colorectal HT29, HCT116, SW620, CACO2, SW480 and Leukaemia K562 cancer cell lines were examined in quadruplicates/dose/cell line. Parameters including potency, toxicity, and selectivity (potency/toxicity) have been reported along with DPPH- and NO- radicals’ scavenging capacities -as their molecular action mechanism- in comparison to ascorbic acid and indomethacin respectively. Using Griess assay in Lipopolysaccharide (LPS) prompted RAW264.7 macrophages; mitigation of inflammation was investigated. RESULTS: nitroFQ 3b, unlike the rest of FQs in PANC1 and MCF7 cells, exhibited remarkably superior NO-radical scavenging/antiinflammation capacity to indomethacin with respective antiproliferative IC(50) values (<50µM) 49 vs. cisplatin’s 122 and 6 vs. cisplatin’s 28 (p<0.01-0.001; n=4). Reduced FQ 4b of significantly dual DPPH-NO scavenging propensities exerted exceptionally substantial micromolar antiproliferation in colorectal cancer cells with respective antiproliferative IC(50) values (<50µM) of HCT116 0.84< HT29 1.6<PANC1 5.7<SW620 9.2 vs. cisplatins’, (p<0.01-0.001; n=4). FQ 5a of superb NO radical reduction effect had antiproliferative IC(50) value (<50µM) of 37.6 in PANC1 cells. In breast cancer T47D the ascending order of pronounced nano-micromolar antiproliferative IC(50) values (<50µM) was 4d<3d<4a<4b<3b (0.009<0.59<10<15<41 vs. cisplatins’, p<0.01-0.001; n=4). Both 4d and 4b displayed both DPPH-NO radicals reduction –related cytotoxicities. NO radical scavengers 3d and 3b as well as DPPH radical scavenger 4a exerted highly appreciably relevant antineoplastic affinities. CONCLUSION: Acidic groups and C8-C7 ethylene diamine Chelation Bridge along with bulky dual halogenations can be substantially associated with molecular action mechanisms of FQs cytotoxicities, antioxidative and antiinflammation effects, collectively. West Asia Organization for Cancer Prevention 2022-05 /pmc/articles/PMC9587871/ /pubmed/35633535 http://dx.doi.org/10.31557/APJCP.2022.23.5.1529 Text en https://creativecommons.org/licenses/by-nc/4.0/This work is licensed under a Creative Commons Attribution-Non Commercial 4.0 International License. https://creativecommons.org/licenses/by-nc/4.0/
spellingShingle Research Article
Qashou, Esraa
Al-Hiari, Yusuf
Kasabri, Violet
AlBashiti, Rabab
AlAlawi, Sundus
Telfah, Ahmad
AlHadid, Amani
Antiproliferative Activities of Lipophililic Fluoroquinolones-Based Scaffold Against a Panel of Solid and Liquid Cancer Cell Lines
title Antiproliferative Activities of Lipophililic Fluoroquinolones-Based Scaffold Against a Panel of Solid and Liquid Cancer Cell Lines
title_full Antiproliferative Activities of Lipophililic Fluoroquinolones-Based Scaffold Against a Panel of Solid and Liquid Cancer Cell Lines
title_fullStr Antiproliferative Activities of Lipophililic Fluoroquinolones-Based Scaffold Against a Panel of Solid and Liquid Cancer Cell Lines
title_full_unstemmed Antiproliferative Activities of Lipophililic Fluoroquinolones-Based Scaffold Against a Panel of Solid and Liquid Cancer Cell Lines
title_short Antiproliferative Activities of Lipophililic Fluoroquinolones-Based Scaffold Against a Panel of Solid and Liquid Cancer Cell Lines
title_sort antiproliferative activities of lipophililic fluoroquinolones-based scaffold against a panel of solid and liquid cancer cell lines
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9587871/
https://www.ncbi.nlm.nih.gov/pubmed/35633535
http://dx.doi.org/10.31557/APJCP.2022.23.5.1529
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