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

Autor: Qashou E; School of Pharmacy, University of Jordan, Amman 11942, Queen Rania Street, Jordan., Al-Hiari Y; School of Pharmacy, University of Jordan, Amman 11942, Queen Rania Street, Jordan.; School of Pharmacy, Al-Zaytoonah University of Jordan, Amman, Jordan., Kasabri V; School of Pharmacy, University of Jordan, Amman 11942, Queen Rania Street, Jordan., AlBashiti R; School of Pharmacy, University of Jordan, Amman 11942, Queen Rania Street, Jordan., AlAlawi S; School of Pharmacy, University of Jordan, Amman 11942, Queen Rania Street, Jordan., Telfah A; Leibniz Institut für analytische Wissenschaften - ISAS e.V. Bunsen-Kirchhoff-Str.1144139 Dortmund, Germany.; Hamdi Mango Center for Academic Research, University of Jordan, Amman 11942, Queen Rania Street, Jordan., AlHadid A; School of Pharmacy, Al-Zaytoonah University of Jordan, Amman, Jordan.
Jazyk: angličtina
Zdroj: Asian Pacific journal of cancer prevention : APJCP [Asian Pac J Cancer Prev] 2022 May 01; Vol. 23 (5), pp. 1529-1537. Date of Electronic Publication: 2022 May 01.
DOI: 10.31557/APJCP.2022.23.5.1529
Abstrakt: 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 IC50 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 IC50 values (<50µM) of HCT116 0.84< HT29 1.6Conclusion: 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.
Databáze: MEDLINE
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