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两种新型壳聚糖衍生物制剂对致病性微生物具有显著抗菌活性且对成纤维细胞具有安全性,其治疗潜力研究。

Therapeutic potential of two formulated novel chitosan derivatives with prominent antimicrobial activities against virulent microorganisms and safe profiles toward fibroblast cells.

作者信息

Hassan Mohamed A, Tamer Tamer M, Omer Ahmed M, Baset Walid M A, Abbas Eman, Mohy-Eldin Mohamed S

机构信息

Protein Research Department, Genetic Engineering and Biotechnology Research Institute (GEBRI), City of Scientific Research and Technological Applications (SRTA-City), New Borg El-Arab City, P.O. Box: 21934 Alexandria, Egypt.

Polymer Materials Research Department, Advanced Technologies and New Materials Research Institute (ATNMRI), City of Scientific Research and Technological Applications (SRTA-City), New Borg El-Arab City, P.O. Box: 21934 Alexandria, Egypt.

出版信息

Int J Pharm. 2023 Mar 5;634:122649. doi: 10.1016/j.ijpharm.2023.122649. Epub 2023 Jan 26.

Abstract

The development of new antimicrobial agents has been drawing considerable attention due to the extreme escalation of multi-drug resistant microorganisms. We thus sought to ameliorate the antimicrobial activities of the chitosan (Cs) biopolymer by coupling chitosan with cyclohexanone and 2-N-methyl pyrrolidone, synthesizing two novel Schiff bases (CsSB1 and CsSB2), respectively. FT-IR, TGA, DSC, SEM, and potentiometric titration were employed to characterize the formulated chitosan derivatives. The findings exposed that the degrees of deacetylation were 88.12% and 89.98% for CsSB1 and CsSB2, respectively. The antimicrobial capacities of CsSB1 and CsSB2 were substantially enhanced compared with prime chitosan. Furthermore, the CsSB1 and CsSB2 demonstrated minimum inhibitory concentrations (MIC) of 50 µg/ml in relation to all studied microorganisms, whereas chitosan revealed MIC value of 50 µg/ml only for E. coli. Furthermore, CsSB1 with a concentration of 250 µg/ml manifested the highest antibacterial activity against Gram-positive bacteria. Correspondingly, CsSB2 revealed a comparable trend of microbial hindrance with lower activities. Besides, the two derivatives could thwart the growth of Candida albicans (C. albicans). The cytotoxicity assay of the biomaterials accentuated their biocompatibility with fibroblasts. Collectively, the two formulated chitosan derivatives could competently rival the native chitosan, particularly for future applications in wound healing.

摘要

由于多重耐药微生物的急剧增加,新型抗菌剂的开发一直备受关注。因此,我们试图通过将壳聚糖与环己酮和2-N-甲基吡咯烷酮偶联,分别合成两种新型席夫碱(CsSB1和CsSB2),以改善壳聚糖(Cs)生物聚合物的抗菌活性。采用傅里叶变换红外光谱(FT-IR)、热重分析(TGA)、差示扫描量热法(DSC)、扫描电子显微镜(SEM)和电位滴定法对所制备的壳聚糖衍生物进行表征。结果表明,CsSB1和CsSB2的脱乙酰度分别为88.12%和89.98%。与原始壳聚糖相比,CsSB1和CsSB2的抗菌能力显著增强。此外,CsSB1和CsSB2对所有研究的微生物的最低抑菌浓度(MIC)均为50µg/ml,而壳聚糖仅对大肠杆菌的MIC值为50µg/ml。此外,浓度为250µg/ml的CsSB1对革兰氏阳性菌表现出最高的抗菌活性。相应地,CsSB2显示出类似的微生物抑制趋势,但活性较低。此外,这两种衍生物可以抑制白色念珠菌(C. albicans)的生长。生物材料的细胞毒性试验强调了它们与成纤维细胞的生物相容性。总的来说,这两种制备的壳聚糖衍生物可以有效地与天然壳聚糖竞争,特别是在伤口愈合的未来应用中。

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