Department of Chemistry, Pondicherry University, Kalapet, Puducherry, 605 014, India.
Department of Microbial Biotechnology, Bharathiar University, Coimbatore, India.
J Mater Chem B. 2022 Jun 1;10(21):4048-4058. doi: 10.1039/d2tb00240j.
Conventional antimicrobial agents are losing the war against drug resistance day-by-day. Chitosan biopolymer is one of the alternative materials that lends itself well to this application by fine-tuning its bioactivity using different pendant groups. Herein, we report the synthesis of novel chitosan with pendant ()-5-((4-acetylphenyl)diazenyl)-6-aminouracil (APAU) groups by forming Schiff base linkages between chitosan and the pendant groups. These chitosan biopolymers with pendant APAU groups form films superior in thermal stability compared to the neat chitosan. Interestingly, APAU alone was inactive against , , , and . However, novel chitosan samples were active against with an MIC of 390 μg mL, half that of plain chitosan at 780 μg mL. APAU modified chitosan samples, CA80 and CA100 showed an MIC (against and ) of 23.4 μg mL, superior to plain chitosan's MIC of 187.5 μg mL and is close to commercial Fluconazole's MIC of 11.7 μg mL. The activity of chitosan changes with APAU content and at higher concentrations shows a strong synergetic antimicrobial effect.
传统的抗菌剂在与耐药性的斗争中日益败退。壳聚糖生物聚合物是一种替代材料，通过使用不同的侧基来微调其生物活性，非常适合这种应用。在此，我们报告了通过壳聚糖和侧基之间形成席夫碱键，合成了带有侧基（）-5-((4-乙酰基苯基)偶氮基)-6-氨基尿嘧啶 (APAU) 的新型壳聚糖。与纯壳聚糖相比，带有 APAU 侧基的这些壳聚糖生物聚合物形成的薄膜具有更好的热稳定性。有趣的是，APAU 本身对 、 、 、 和 没有活性。然而，新型壳聚糖样品对 具有活性，MIC 为 390 μg mL，是纯壳聚糖 MIC（780 μg mL）的一半。APAU 修饰的壳聚糖样品 CA80 和 CA100 对 和 的 MIC 为 23.4 μg mL，优于纯壳聚糖的 MIC（187.5 μg mL），接近商业氟康唑的 MIC（11.7 μg mL）。壳聚糖的活性随 APAU 含量而变化，在较高浓度下显示出很强的协同抗菌作用。
