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阳离子壳聚糖衍生物作为潜在的抗真菌剂:结构优化及应用综述。

Cationic chitosan derivatives as potential antifungals: A review of structural optimization and applications.

机构信息

Key Laboratory of Experimental Marine Biology, Center for Ocean Mega-Science, Institute of Oceanology, Chinese Academy of Sciences, Qingdao, China; Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology (Qingdao), No. 1 Wenhai Road, Qingdao, 266237, China.

Key Laboratory of Experimental Marine Biology, Center for Ocean Mega-Science, Institute of Oceanology, Chinese Academy of Sciences, Qingdao, China; Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology (Qingdao), No. 1 Wenhai Road, Qingdao, 266237, China.

出版信息

Carbohydr Polym. 2020 May 15;236:116002. doi: 10.1016/j.carbpol.2020.116002. Epub 2020 Feb 14.

Abstract

The increasing resistance of pathogen fungi poses a global public concern. There are several limitations in current antifungals, including few available fungicides, severe toxicity of some fungicides, and drug resistance. Therefore, there is an urgent need to develop new antifungals with novel targets. Chitosan has been recognized as a potential antifungal substance due to its good biocompatibility, biodegradability, non-toxicity, and availability in abundance, but its applications are hampered by the low charge density results in low solubility at physiological pH. It is believed that enhancing the positive charge density of chitosan may be the most effective approach to improve both its solubility and antifungal activity. Hence, this review mainly focuses on the structural optimization strategy of cationic chitosan and the potential antifungal applications. This review also assesses and comments on the challenges, shortcomings, and prospect of cationic chitosan derivatives as antifungal therapy.

摘要

病原体真菌的耐药性不断增强,引起了全球公众的关注。目前的抗真菌药物存在一些局限性,包括可用的杀真菌剂种类有限、某些杀真菌剂毒性较大以及存在耐药性等。因此,迫切需要开发具有新作用靶点的新型抗真菌药物。壳聚糖由于其良好的生物相容性、可生物降解性、无毒性以及丰富的可用性,已被认为是一种有潜力的抗真菌物质,但由于其在生理 pH 值下电荷密度低导致溶解度低,其应用受到限制。人们认为,提高壳聚糖的正电荷密度可能是提高其溶解度和抗真菌活性的最有效方法。因此,本综述主要集中于阳离子壳聚糖的结构优化策略及其在潜在抗真菌方面的应用。本综述还评估并评论了阳离子壳聚糖衍生物作为抗真菌治疗的挑战、缺点和前景。

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