Synthesis of Cefixime–Gelatin Chemical Conjugated Microparticles and Their Antibacterial Activity Against Escherichia coli

IF 3.2 4区工程技术 Q2 CHEMISTRY, MULTIDISCIPLINARY

Korean Journal of Chemical Engineering Pub Date : 2025-05-25 DOI:10.1007/s11814-025-00469-2

Sathianarayanan Sankaran, Avinash Shivdas, Jose Asha, Mahendra Gowdru Srinivasa, Rekha Thiruvengadam, Shine Kadaikunnan, Naiyf S. Alharbi, Rekha Arcot, Muthu Thiruvengadam

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引用次数: 0

Abstract

Escherichia coli (E. coli) is a Gram-negative bacillus found in the intestine, which can also cause intestinal and extraintestinal illnesses in humans. Several hundred E. coli strains have been identified to cause diseases ranging from mild, self-limiting gastroenteritis to renal failure and septic shock. Its virulence allows E. coli to evade host defenses and develop resistance to common antibiotics. The aim of our study was to develop an aqueous-soluble cefixime conjugate for the treatment of E. coli infections. Cefixime shows excellent activity against E. coli strains. However, it has poor aqueous solubility. Thus, it was conjugated with gelatin using 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC) to produce a Cefixime–gelatin chemical conjugate (CGcc) with a significantly higher solubility than that of the pure drug, which may produce a better therapeutic effect. The conjugate was characterized using spectral data. The conjugate was determined to be non-hemolytic and non-toxic to L929 cells. The antibacterial activity of CGcc against E. coli was evaluated in vitro using the disc-diffusion method. The results showed that CGcc was slightly soluble in methanol, but very soluble in water and PBS, and its melting point was found to be 224–230 °C. The SEM images revealed that the CGcc exhibited a spherical morphology. All spectral data support the chemical conjugation of gelatin. The conjugation efficiency of CGcc was 74.54 ± 3.358%. In addition to its hemocompatibility and biocompatibility, CGcc exhibited enhanced solubility. The antibacterial effects revealed that CGcc exhibited good antibacterial activity against E. coli. CGcc showed a clear zone of inhibition and it was found to be 11.74 mm for 0.5 µg and 15.13 mm for 1 µg, respectively. Overall, the cefixime–gelatin chemical conjugate was effective in treating E. coli infections. This preliminary study may provide valuable insights into therapeutic effects during both preclinical and clinical trials. Detailed innovative methods are needed for the future alteration of gelatin and cefixime and integration of polymers into proper therapeutic applications.

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头孢昔肟-明胶化学偶联微球的合成及其对大肠杆菌的抑菌活性

大肠杆菌（E. coli）是一种在肠道中发现的革兰氏阴性杆菌，它也能引起人类肠道和肠外疾病。数百种大肠杆菌菌株已被确定可引起从轻度自限性胃肠炎到肾衰竭和感染性休克等疾病。它的毒力使大肠杆菌能够逃避宿主的防御，并对普通抗生素产生耐药性。本研究的目的是研制一种用于治疗大肠杆菌感染的水溶性头孢克肟偶联物。头孢克肟对大肠杆菌具有良好的抑菌活性。然而，它的水溶性很差。因此，用1-乙基-3-（3-二甲氨基丙基）碳二酰亚胺（EDC）与明胶偶联得到头孢昔肟-明胶化学偶联物（ccgc），其溶解度明显高于纯药物，可能会产生更好的治疗效果。利用光谱数据对共轭物进行了表征。该偶联物对L929细胞无溶血作用和毒性。采用圆盘扩散法测定了cgc对大肠杆菌的抑菌活性。结果表明，CGcc在甲醇中微溶，在水和PBS中极溶，熔点为224 ~ 230℃。SEM图像显示，cgc呈球形。所有光谱数据都支持明胶的化学偶联。CGcc的结合效率为74.54±3.358%。除了血液相容性和生物相容性外，CGcc还表现出增强的溶解度。结果表明，cgc对大肠杆菌具有良好的抑菌活性。ccgcc有明显的抑制区，0.5µg和1µg分别为11.74 mm和15.13 mm。总的来说，头孢昔肟-明胶化学偶联物治疗大肠杆菌感染是有效的。这项初步研究可能为临床前和临床试验的治疗效果提供有价值的见解。未来需要详细的创新方法来改变明胶和头孢克肟，并将聚合物整合到适当的治疗应用中。

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来源期刊

Korean Journal of Chemical Engineering 工程技术-工程：化工

CiteScore

4.60

自引率

11.10%

发文量

310

审稿时长

4.7 months

期刊介绍： The Korean Journal of Chemical Engineering provides a global forum for the dissemination of research in chemical engineering. The Journal publishes significant research results obtained in the Asia-Pacific region, and simultaneously introduces recent technical progress made in other areas of the world to this region. Submitted research papers must be of potential industrial significance and specifically concerned with chemical engineering. The editors will give preference to papers having a clearly stated practical scope and applicability in the areas of chemical engineering, and to those where new theoretical concepts are supported by new experimental details. The Journal also regularly publishes featured reviews on emerging and industrially important subjects of chemical engineering as well as selected papers presented at international conferences on the subjects.