（1,2,3-三唑-4-基）甲基烟酰基壳聚糖的合成及抑菌活性评价。

Synthesis and antifungal evaluation of (1,2,3-triazol-4-yl)methyl nicotinate chitosan.

机构信息

Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China.

出版信息

Int J Biol Macromol. 2013 Oct;61:58-62. doi: 10.1016/j.ijbiomac.2013.05.023. Epub 2013 May 31.

DOI:10.1016/j.ijbiomac.2013.05.023

Abstract

With an aim to discover novel chitosan derivatives with significant activities against crop-threatening fungi, (1,2,3-triazol-4-yl)methyl nicotinate chitosan (TAMNCS) was prepared via azide-alkyne click reaction. Its structure was characterized by FT-IR, (1)H NMR, elemental analysis, DSC, and SEM. In vitro antifungal properties of TAMNCS against Rhizoctonia solani Kühn (R. solani), Stemphylium solani weber (S. solani), and Alternaria porri (A. porri) were studied at the concentrations ranged from 0.25 mg/mL to 1.0 mg/mL. Experiments conducted displayed the derivative had obviously enhanced antifungal activity after chemical modification compared with original chitosan. Moreover, it was shown that TAMNCS can 94.2% inhibit growth of A. porri at 1.0 mg/mL, while dose at which the fungicide triadimefon had lower inhibitory index (62.2%). The primary antifungal results described here indicate this derivative may be a promising candidate as an antifungal agent.

摘要

为了发现具有显著防治作物病害真菌活性的新型壳聚糖衍生物，通过叠氮-炔点击反应制备了（1,2,3-三唑-4-基）甲基烟酸壳聚糖（TAMNCS）。通过傅里叶变换红外光谱（FT-IR）、（1）H 核磁共振、元素分析、差示扫描量热法和扫描电子显微镜对 TAMNCS 的结构进行了表征。在浓度为 0.25 mg/mL 至 1.0 mg/mL 的范围内，研究了 TAMNCS 对茄腐镰孢菌（R. solani）、茄丝核菌（S. solani）和葱腐葡萄孢（A. porri）的体外抗真菌特性。实验结果表明，与原始壳聚糖相比，化学修饰后的衍生物具有明显增强的抗真菌活性。此外，TAMNCS 在 1.0 mg/mL 时可以抑制 94.2%的葱腐葡萄孢生长，而杀菌剂三唑酮的抑菌指数（62.2%）较低。这里描述的初步抗真菌结果表明，该衍生物可能是一种有前途的抗真菌剂候选物。