Furan-based Chalcone Annihilates the Multi-Drug-Resistant Pseudomonas aeruginosa and Protects Zebra Fish Against its Infection.

The emergence of carbapenem-resistant Pseudomonas aeruginosa, a multi-drug-resistant bacteria, is becoming a serious public health concern. This bacterium infects immunocompromised patients and has a high fatality rate. Both naturally and synthetically produced chalcones are known to have a wide array of biological activities. The antibacterial properties of synthetically produced chalcone were studied against P. aeruginosa. In vitro, study of the compound (chalcone derivative named DKO1), also known as (2E)-1-(5-methylfuran-2-yl)-3-(4-nitrophenyl) prop-2-en-1-one, had substantial antibacterial and biofilm disruptive action. DKO1 effectively shielded against P. aeruginosa-induced inflammation, oxidative stress, lipid peroxidation, and apoptosis in zebrafish larvae. In adult zebrafish, the treatment enhanced the chances of survivability and reduced the sickness-like behaviors. Gene expression, biochemical analysis, and histopathology studies found that proinflammatory cytokines (TNF-α, IL-1ß, IL-6, iNOS) were down regulated; antioxidant enzymes such as superoxide dismutase (SOD) and catalase (CAT) levels increased, and histoarchitecture was restored in zebrafish. The data indicate that DKO1 is an effective antibacterial agent against P. aeruginosa demonstrated both in vitro and in vivo.

Synthesis of novel furan-based chalcone derivatives as anti-tuberculosis agents: in vitro, cytotoxicity assessment and in silico.

Background: The aim of the study is to identify a novel furan-based chalcone derivative as potent inhibitor against the H37Rv strain. Materials & methods: The in silico pharmacokinetic characteristics, toxicity tests, molecular modeling, chemical synthesis and minimum inhibitory concentration (MIC; IC50) were carried out to evaluate the antitubercular potential of the synthesized furan-based chalcone analogues against H37Rv. Results & conclusion: Among the ten target compounds synthesized, DF02, DF05 and DF07 had MIC values of 1.6 µg/ml equivalent to isoniazid and DF10 showed MIC values of 3.25 µg/ml which is equipotent to pyrazinamide. All the other compounds had optimal concentrations 6.25-100 µg/ml against the H37Rv strain. Compounds DF02 and DF10 were further evaluated for cytotoxicity assay performed using HeLa cell lines.