四唑是由一个碳原子和四个氮原子组成的五元环芳香杂环分子。几种基于四唑的药物已显示出对抗细菌、真菌、哮喘、癌症、高血压等的良好活性。本研究的总体目的是确定四唑和四唑缀合银纳米颗粒的抗棘阿米巴特性。合成了四唑共轭银纳米粒子，并使用紫外可见光谱、动态光散射和傅里叶变换红外光谱进行了确认。通过杀阿米巴、包囊和排胞试验，研究结果表明，四唑具有抗阿米巴特性，并且当与银纳米颗粒缀合时，这些效果会增强。当进行寄生虫杀灭测试时，最小抑制浓度从单独使用四唑的约 20μM 降低到使用四唑缀合银纳米颗粒的 10μM。重要的是，与银纳米颗粒的结合增加了体外寄生虫介导的人类细胞死亡（通过乳酸脱氢酶释放来测量），但它减少了单独药物对人类细胞的毒性作用。在细胞致病性测定中，最小抑制浓度从单独四唑的~15μM降低到四唑缀合银纳米颗粒的小于50μM。总体而言，这些结果清楚地表明，四唑具有有效的抗阿米巴特性，可以通过与银纳米颗粒结合来增强这种特性，并且在合理开发针对寄生虫感染（如致病性棘阿米巴引起的角膜炎和肉芽肿性阿米巴脑炎）的治疗干预措施方面具有潜在作用。版权所有 © 2024爱思唯尔公司出版。

Tetrazoles are five-membered ring aromatic heterocyclic molecules that consist of one carbon and four nitrogen atoms. Several tetrazole-based drugs have shown promising activities against bacteria, fungi, asthma, cancer, hypertension etc. The overall aim of this study was to determine anti-Acanthamoebic properties of tetrazoles and tetrazole-conjugated silver nanoparticles. Tetrazole-conjugated silver nanoparticles were synthesized and confirmed using ultraviolet-visible spectrometry, Dynamic light scattering, and Fourier-transform infrared spectroscopy. Using amoebicidal, encystment, and excystment assays, the findings revealed that tetrazoles exhibited antiamoebic properties and these effects were enhanced when conjugated with silver nanoparticles. When tested for parasite killing, the minimum inhibitory concentration was reduced from ∼20μM with tetrazole alone to 10μM with tetrazole-conjugated silver nanoparticles. Importantly, conjugation with silver nanoparticles increased parasite-mediated human cell death in vitro, as measured by lactate dehydrogenase release, but it reduced toxic effects of drugs alone on human cells. In cytopathogenicity assays, the minimum inhibitory concentration was reduced from ∼15μM with tetrazole alone to less than 50μM with tetrazole-conjugated silver nanoparticles. Overall, these results showed clearly that tetrazoles exhibit potent antiamoebic properties which can be enhanced by conjugation with silver nanoparticles and have potential role in the rational development of therapeutic interventions against parasitic infections such as keratitis and granulomatous amoebic encephalitis due to pathogenic Acanthamoeba.Copyright © 2024. Published by Elsevier Inc.