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维替他汀偶联金纳米粒子增强了对埃尔托生物型的抗菌活性。

Virstatin-Conjugated Gold Nanoparticle with Enhanced Antimicrobial Activity against the El Tor Biotype.

机构信息

Department of Biochemistry, Bose Institute, P1/12 CIT Scheme VIIM, Kolkata 700054, India.

Division of Molecular Medicine, Bose Institute, P1/12 CIT Scheme VIIM, Kolkata 700054, India.

出版信息

ACS Appl Bio Mater. 2021 Apr 19;4(4):3089-3100. doi: 10.1021/acsabm.0c01483. Epub 2021 Mar 23.

DOI:10.1021/acsabm.0c01483
PMID:35014397
Abstract

Because of the emergence of multidrug-resistant pathogenic bacteria, there is a growing interest for the development of an efficient alternative to antibiotics. Gold nanoparticles (AuNPs) are promising candidates due to their inherent non-toxicity and can be used as effective carriers of drugs. Cholera caused by Gram-negative is still a potential threat in many developing countries. Virstatin, a small molecule, has been reported to inhibit virulence regulation in . Herein, we report an efficient synthesis of virstatin-conjugated gold nanoparticles (VL-AuNPs) and their antibacterial efficacy against the El Tor biotype of (N16961). The spherical-shaped NPs have an average diameter of ∼17 nm. The uniqueness of VL-AuNPs relies in the enhanced antibacterial efficacy compared to virstatin, as evidenced from the inhibitory concentration obtained from growth kinetics, and attributed to the inhibition of ATPase activity and DNA damage. More importantly, the expression of cholera toxin, the most important virulence factor of , is reduced to a far greater extent than by any of the component molecules. The effect of VL-AuNPs on N16961 was monitored using various assays such as confocal microscopy, FACS, fluorescence spectroscopy, and so on. Overall, VL-AuNPs could be a potential candidate for the use as an effective agent for combating diarrheal diseases caused by .

摘要

由于多药耐药性病原菌的出现,人们对开发抗生素的有效替代品越来越感兴趣。由于其固有无毒的特性,金纳米粒子(AuNPs)是很有前途的候选者,并且可以用作药物的有效载体。由革兰氏阴性引起的霍乱仍然是许多发展中国家的潜在威胁。小分子维司他汀已被报道可抑制霍乱弧菌的毒力调节。在此,我们报告了一种有效的维司他汀缀合金纳米粒子(VL-AuNPs)的合成方法及其对 El Tor 生物型霍乱弧菌(N16961)的抗菌功效。这些球形 NPs 的平均直径约为 17nm。VL-AuNPs 的独特之处在于其抗菌功效增强,这从生长动力学获得的抑制浓度中可以得到证明,这归因于其对 ATP 酶活性和 DNA 损伤的抑制作用。更重要的是,霍乱毒素的表达,这是霍乱弧菌最重要的毒力因子,被大大降低,其程度超过了任何一种成分分子。使用共聚焦显微镜、FACS、荧光光谱等各种检测方法监测 VL-AuNPs 对 N16961 的影响。总的来说,VL-AuNPs 可以成为一种有效的候选药物,用于对抗由霍乱弧菌引起的腹泻疾病。

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