Patel Miraj, Kikani Twara, Thakore Sonal
Department of Chemistry, Faculty of Science, The Maharaja Sayajirao University of Baroda, Vadodara 390 002, India.
Department of Chemistry, Faculty of Science, The Maharaja Sayajirao University of Baroda, Vadodara 390 002, India.
Int J Biol Macromol. 2025 Jul;318(Pt 4):145242. doi: 10.1016/j.ijbiomac.2025.145242. Epub 2025 Jun 13.
Polymers are being greatly researched to design biocompatible, cost effective and efficient antibacterial agents. This work explores the impact of derivatization of dextran with the heterocyclic moiety via imine linkages. Introducing a heterocyclic moiety is expected to improve bioactivity of dextran and expand its scope of application. Four imine derivatives of dextran were synthesized to examine the effect of heterocyclic structure on the antibacterial and antioxidant activity. Antibacterial activity was investigated against gram-positive bacteria (Staphylococcus aureus) and gram-negative bacteria (Escherichia coli). Compound 2a, containing a furan ring, exhibited the most potent antibacterial activity, with inhibition zones of 36 mm against E. coli and 24 mm against S. aureus. This was comparable to the standard antibiotic rifampicin which produced inhibition zones of 34 mm and 22 mm against E. coli and S. aureus, respectively. Among the derivatives, compound 2c, featuring an indole ring, exhibited the highest antioxidant activity, with IC values of 29.86 ± 2.28, 34.10 ± 0.39, and 31.60 ± 0.20 μg/mL for DPPH, hydroxyl, and nitric oxide radicals, respectively. The findings showed that heterocyclic moiety and imine linkage enhanced the antibacterial and antioxidant activities of dextran.
人们正在大力研究聚合物，以设计出生物相容性好、成本效益高且高效的抗菌剂。这项工作探讨了通过亚胺键将杂环部分衍生化对葡聚糖的影响。引入杂环部分有望提高葡聚糖的生物活性并扩大其应用范围。合成了四种葡聚糖亚胺衍生物，以研究杂环结构对抗菌和抗氧化活性的影响。针对革兰氏阳性菌（金黄色葡萄球菌）和革兰氏阴性菌（大肠杆菌）研究了抗菌活性。含有呋喃环的化合物2a表现出最强的抗菌活性，对大肠杆菌的抑菌圈为36毫米，对金黄色葡萄球菌的抑菌圈为24毫米。这与标准抗生素利福平相当，利福平对大肠杆菌和金黄色葡萄球菌的抑菌圈分别为34毫米和22毫米。在这些衍生物中，具有吲哚环的化合物2c表现出最高的抗氧化活性，对DPPH、羟基和一氧化氮自由基的IC值分别为29.86±2.28、34.10±0.39和31.60±0.20μg/mL。研究结果表明，杂环部分和亚胺键增强了葡聚糖的抗菌和抗氧化活性。
