Functionalised Flouroquinolones as a Potentially Novel Class of Anti-inflammatory and Anti-glycation Compounds; Synthesis and Pharmacological Appraisal. Issue 3 (3rd May 2020)

• Record Type: Journal Article
• Authors: Al-Shahrabi, Rula; Kasabri, Violet; Al-Hiari, Yusuf; Arabiyat, Shereen; Al Bashiti, Rabab; Alalawi, Sundus; Alhadid, Amani
• Is Part Of: Analytical chemistry letters. Volume 10:Issue 3(2020)
• Page Start: 280
• Page End: 297
• Publication Date: 2020-05-03
• Subjects: Fluoroquinolones -- sulphorodhamine B -- aminoguanidine -- ascorbic acid -- indomethacin -- dual glycation-inflammation modulation -- DPPH -- greiss assay -- LPS -- methylglyoxal -- RAW264.7 macrophages; Chemistry, Analytic -- Periodicals; 543.05
• DOI: 10.1080/22297928.2020.1777196
• Languages: English
• ISSNs: 2229-7928

Abstract

Abstract: New synthetic 36 fluoroquinolones (FQs) have been developed. Their anti-inflammatory and 2, 2-diphenyl-1-picrylhydrazyl (DPPH)- and nitric oxide (NO)- radicals scavenging propensities were delineated in vitro . The anti-inflammation related NO radical scavenging bioactivities of new FQs compounds against lipopolysaccharide (LPS)-prompted NO production in RAW 264.7 macrophages were examined using the Griess assay. Selectively nitro FQ compound 2-AnisCEtA exerted an exceedingly superior anti-inflammatory effects (p<0.001 vs. indomethacin IC50 value of 103.35±4.4 μM) while 7 nitro FQs, 10 reduced FQs and 9 triazolo FQs were moderately more efficacious than indomethacin. The remaining 9 Compounds could display appreciable anti-inflammatory capacity. Unequivocally their DPPH radical scavenging effects were of substantially lesser efficacy than ascorbic acid. Using 400 μM methylglyoxal as the choice glucotoxicity concentration in RAW264.7 macrophages; it was shown that 18 out of 36 FQs could exhibit an exceedingly more superior than or significantly comparable cytoprotection against methylglyoxal-induced carbonyl toxicity to antiglycation aminoguanidine. Suggestively dual modulation of glycation-inflammation can be linked with FQs lipophilicity-chelating properties. FQs can serve as scaffolds for the development and designing of new druggable deglycation and antiglycation therapeutic candidates via duality of antiglycation-antiinflammatory capacities.