New thiadiazole modified chitosan derivative to control the growth of human pathogenic microbes and cancer cell lines

Scientific reports(2022)

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摘要
The emergence of multidrug-resistant microbes and the propagation of cancer cells are global health issues. The unique properties of chitosan and its derivatives make it an important candidate for therapeutic applications. Herein, a new thiadiazole derivative, 4-((5-(butylthio)-1,3,4-thiadiazol-2-yl) amino)-4-oxo butanoic acid (BuTD-COOH) was synthesized and used to modify the chitosan through amide linkages, forming a new thiadiazole chitosan derivative (BuTD-CH). The formation of thiadiazole and the chitosan derivative was confirmed by FT-IR, 1 H/ 13 C-NMR, GC–MS, TGA, Elemental analysis, and XPS. The BuTD-CH showed a high antimicrobial effect against human pathogens Escherichia coli , Pseudomonas aeruginosa , Bacillus subtilis , Staphylococcus aureus , and Candida albicans with low MIC values of 25–50 μg ml −1 compared to unmodified chitosan. The in-vitro cytotoxicity of BuTD-CH was evaluated against two cancer cell lines (MCF-7 and HepG2) and one normal cell (HFB4) using the MTT method. The newly synthesized derivatives showed high efficacy against cancerous cells and targeted them at low concentrations (IC 50 was 178.9 ± 9.1 and 147.8 ± 10.5 μg ml −1 for MCF-7 and HepG2, respectively) compared with normal HFB4 cells (IC 50 was 335.7 ± 11.4 μg ml −1 ). Thus, low concentrations of newly synthesized BuTD-CH could be safely used as an antimicrobial and pharmacological agent for inhibiting the growth of human pathogenic microbes and hepatocellular and adenocarcinoma therapy.
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Biotechnology,Cancer,Chemistry,Drug discovery,Engineering,Materials science,Microbiology,Science,Humanities and Social Sciences,multidisciplinary
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