常见壳聚糖衍生物的抗菌结构-活性关系。
The antibacterial structure-activity relationship for common chitosan derivatives.
机构信息
Faculty of Pharmaceutical Sciences, School of Health Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavík, Iceland.
Department of Biomedical Science, Faculty of Medicine, School of Health Sciences, University of Iceland, Hringbraut 31, IS-101 Reykjavík, Iceland.
出版信息
Int J Biol Macromol. 2020 Dec 15;165(Pt B):1686-1693. doi: 10.1016/j.ijbiomac.2020.09.200. Epub 2020 Oct 9.
The relationship between the degree of substitution and antibacterial activity was studied for six common chitosan derivatives N, N,N-trimethyl chitosan (TMC and TMC) N-(2-(N,N,N-trimethylammoniumyl)acetyl)-chitin (TACin), N-(2-hydroxyl) propyl-3-trimethyl ammonium chitosan (HTC), hydroxypropyl chitosan (HPC), thioglycolic chitosan (TGC) and carboxymethyl chitosan (CMC). The degree of substitution (DS) in the 36 studied samples ranged from 0.02 to 1.1 as determined by H NMR. The activity was determined as the minimum inhibitory concentration (MIC) against S. aureus and E. coli at pH 7.2 and 5.5. The antibacterial effect of TMC and TACin increased with DS. Samples of these derivatives with high DS were more active than chitosan at pH 7.2. HTC was more active than chitosan against S. aureus, but this activity was not affected by DS. In other cases, the activity of HTC decreased with an increase in DS. The DS for the TGC was very low and the activity was similar to unmodified chitosan. The activity of HPC decreased with DS. CMC was not active in this study.
研究了六种常见壳聚糖衍生物 N，N，N-三甲基壳聚糖（TMC 和 TMC）N-（2-（N，N，N-三甲基铵基）乙酰基）壳聚糖（TACin），N-（2-羟基）丙基-3-三甲基铵壳聚糖（HTC），羟丙基壳聚糖（HPC），巯基乙酸壳聚糖（TGC）和羧甲基壳聚糖（CMC）的取代度（DS）与抗菌活性之间的关系。通过 1H NMR 确定了 36 个研究样品的 DS 范围为 0.02 至 1.1。活性是在 pH 7.2 和 5.5 下测定的对金黄色葡萄球菌和大肠杆菌的最小抑菌浓度（MIC）。TMC 和 TACin 的抗菌效果随 DS 增加而增加。高 DS 的这些衍生物的样品在 pH 7.2 下比壳聚糖更活跃。HTC 对金黄色葡萄球菌的活性比壳聚糖强，但这种活性不受 DS 的影响。在其他情况下，HTC 的活性随 DS 的增加而降低。TGC 的 DS 非常低，活性与未修饰的壳聚糖相似。HPC 的活性随 DS 降低而降低。CMC 在本研究中不活跃。
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