新型壳聚糖希夫碱的药物潜力，特别针对其抗菌、抗生物膜、抗氧化、抗炎、血液相容性和细胞毒性活性。
Pharmaceutical Potential of a Novel Chitosan Derivative Schiff Base with Special Reference to Antibacterial, Anti-Biofilm, Antioxidant, Anti-Inflammatory, Hemocompatibility and Cytotoxic Activities.
机构信息
Biofuels Institute, School of the Environment and Safety Engineering, Jiangsu University, Zhenjiang, 212013, China.
Botany Department, Faculty of Science, Tanta University, Tanta, 31527, Egypt.
出版信息
Pharm Res. 2018 Nov 7;36(1):5. doi: 10.1007/s11095-018-2535-x.
PURPOSE
Chitosan and its derivatives possess several unique properties relevant in the field of pharmaceutics and medicinal chemistry. This study aimed to evaluate the pharmaceutical performance of an innovative chitosan derivative, methyl acrylate chitosan bearing p-nitrobenzaldehyde (MACSpNBA) Schiff base.
METHODS
The antibacterial activity of MACSpNBA was tested against multi-drug resistant (MDR) Gram-negative and Gram-positive bacteria using agar-well diffusion method. Anti-biofilm formation was analyzed using a microtitre plate. Antioxidant assays were performed to assess the scavenging activity of MACSpNBA using DPPH, hydrogen peroxide, superoxide together with its reducing power activity. Anti-inflammatory activity was evaluated by albumin denaturation, membrane stabilization, and proteinase inhibition methods. MACSpNBA was tested for its hemolytic efficiency on human erythrocytes. Cytotoxicity of MACSpNBA was evaluated by MTT assay.
RESULTS
MACSpNBA showed a significant performance as an antibacterial candidate against MDR bacteria, anti-biofilm, antioxidant and anti-inflammatory biomaterial, evidencing hemocompatibility and no cytotoxicity. It exhibited a significant negative correlation with biofilm formation by the MDR-PA-09 strain. Biological activities were found to be significantly concentration-dependent.
CONCLUSIONS
the newly chitosan derivative MACSpNBA showed to be promising for pharmaceutical applications, expanding the treatment ways toward skin burn infections since it allied excellent antibacterial, anti-biofilm, antioxidant, anti-inflammatory, hemocompatibility and absence of cytotoxic activities.
目的
壳聚糖及其衍生物具有在药剂学和药物化学领域相关的几个独特性质。本研究旨在评估一种创新壳聚糖衍生物——甲基丙烯酰基壳聚糖接枝对硝基苯甲醛（MACSpNBA）席夫碱的药物性能。
方法
采用琼脂孔扩散法检测 MACSpNBA 对多药耐药（MDR）革兰氏阴性和革兰氏阳性菌的抗菌活性。采用微量滴定板分析抗生物膜形成。通过 DPPH、过氧化氢、超氧自由基清除实验和还原力实验评估 MACSpNBA 的抗氧化活性。通过白蛋白变性、膜稳定性和蛋白酶抑制方法评估抗炎活性。用人红细胞检测 MACSpNBA 的溶血效率。通过 MTT 测定评估 MACSpNBA 的细胞毒性。
结果
MACSpNBA 作为一种针对 MDR 细菌的抗菌候选药物表现出显著的性能，具有抗生物膜、抗氧化和抗炎生物材料的特性，表现出良好的血液相容性和无细胞毒性。它与 MDR-PA-09 菌株的生物膜形成呈显著负相关。生物活性与浓度呈显著的相关性。
结论
新型壳聚糖衍生物 MACSpNBA 具有广阔的药物应用前景，由于其具有良好的抗菌、抗生物膜、抗氧化、抗炎、血液相容性和无细胞毒性等特性，有望为皮肤烧伤感染的治疗提供新的方法。
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