Tan Wenqiang, Li Qing, Wang Huali, Liu Yan, Zhang Jingjing, Dong Fang, Guo Zhanyong
Key Laboratory of Coastal Biology and Bioresource Utilization, Yantai Institute of Coastal Zone Research, Chinese Academy of Sciences, Yantai 264003, China; University of Chinese Academy of Sciences, Beijing 100049, China.
Key Laboratory of Coastal Biology and Bioresource Utilization, Yantai Institute of Coastal Zone Research, Chinese Academy of Sciences, Yantai 264003, China.
Carbohydr Polym. 2016 May 20;142:1-7. doi: 10.1016/j.carbpol.2016.01.007. Epub 2016 Jan 7.
Four novel starch-linked-1,2,3-triazole derivatives were synthesized including 6-hydroxymethyltriazole-6-deoxy starch (HMTST), 6-bromomethyltriazole-6-deoxy starch (BMTST), 6-chloromethyltriazole-6-deoxy starch (CMTST), and 6-carboxyltriazole-6-deoxy starch (CBTST). Their antibacterial properties against Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) were evaluated in vitro, respectively. The inhibitory property of the obtained amphiprotic starch derivatives exhibited a remarkable improvement over starch. And the antibacterial indices of most of the products were higher than 60% and 40% at 1.0 mg/mL when the culture time was 8 h and 16 h, respectively. Moreover, the inhibitory index of CBTST attained 97% above at 1.0 mg/mL. Generally, the inhibitory activity decreased in the order: CBTST>CMTST>BMTST>HMTST>starch. Furthermore, the order of their antibacterial activity was consistent with the electron-withdrawing property of different substituted groups of the 1,2,3-triazole groups. The substituted groups with stronger electron withdrawing ability relatively possessed greater antibacterial activity.
合成了四种新型的淀粉连接的1,2,3-三唑衍生物，包括6-羟甲基三唑-6-脱氧淀粉（HMTST）、6-溴甲基三唑-6-脱氧淀粉（BMTST）、6-氯甲基三唑-6-脱氧淀粉（CMTST）和6-羧基三唑-6-脱氧淀粉（CBTST）。分别对它们针对大肠杆菌（E. coli）和金黄色葡萄球菌（S. aureus）的抗菌性能进行了体外评估。所获得的两性淀粉衍生物的抑制性能相对于淀粉有显著提高。当培养时间分别为8小时和16小时时，大多数产品在1.0 mg/mL时的抗菌指数分别高于60%和40%。此外，CBTST在1.0 mg/mL时的抑制指数达到97%以上。一般来说，抑制活性顺序为：CBTST>CMTST>BMTST>HMTST>淀粉。此外，它们的抗菌活性顺序与1,2,3-三唑基团不同取代基的吸电子性能一致。吸电子能力较强的取代基相对具有更大的抗菌活性。
