Antilipolytic-Antiproliferative Activity of Novel Antidiabesity Triazolo/Fluoroquinolones

Shereen Arabiyat, Violet Kasabri, Yusuf Al-Hiari


Background & Aim: The new Fluoroquinolones (FQs) and triazolofluoroquinolones (TFQs) were synthesized and evaluated for antiproliferative – antilipolytic activity and anti-diabesity activity via DPP IV enzyme and glycation-inflammation bioassays.
Methods: new synthetic approaches to 3 fluoroquinolones (FQs) have been developed. Enzymatic bioassays with colorimetric inhibition kinetics were undertaken. Cell lines’ cultures with colorimetric endpoint bioassays were utilised. Appropriate reference agents were procured.
Results: Incomparably to Diprotin A; TFQs lacked for DPPIV inhibition. The superior antiglycation activity of derivative 5 with IC50 (µM) value of 1.61±0.14 exceeded aminoguanidine’s (AG). Compounds 3 and 4 impressively exerted a comparable protection to AG against methylglyoxal-induced carbonyl toxicity (respective IC50 values of 7.9 and 6.35 µM). All 3 TFQs had a moderate safety profile. All 3 TFQs incomparably exceeded the antiinflammatory indomethacin (IC50 value= 212 µM) efficacy against LPS-induced nitric oxide production in RAW 264.7 macrophages with minimal cytotoxicity. In their respective PL-IC50 values; appreciable antilipolytic activity was recognized, though less potent than orlistat. Noticeably 3 and 4 (but not 5) could be identified for their comparable or outstanding antiprolifertaive capacities vs. cisplatin in the colorectal cancer cell lines (HT29, HCT116, SW620 CACO2 and SW480) with unselective cytotoxity.
Conclusion: FQ and TFQ derivatives may unveil new antidiabesity and anticancer agents.


Fluoroquinolones & triazolofluoroquinolones, glycation- inflammation & DPP IV-Pancreatic Lipase, obesity-colorectal cancer

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