School of Pharmacy, Walailak University, Nakhon Si Thammarat 80161, Thailand.
Drug and Cosmetics Excellence Center, Walailak University, Nakhon Si Thammarat 80161, Thailand.
Molecules. 2022 Sep 7;27(18):5780. doi: 10.3390/molecules27185780.
Colistin is a potent peptide antibiotic that is effective against Gram-negative bacteria. However, nephrotoxicity limited its clinical use. Silver nanoparticles (AgNPs) have gained attention as a potential antimicrobial agent and nanodrug carrier. The conjugation of antibiotics and AgNPs has been found to increase the activity and decrease drug toxicity. In this study, colistin was conjugated with AgNPs (Col-AgNPs), which was confirmed by Fourier-transform infrared (FT-IR) and energy-dispersive X-ray (EDX) spectra. The optimized Col-AgNPs had the proper characteristics, including spherical shape, monodispersity, nanosized particle, high surface charge, and good stability. The powder X-ray diffraction (PXRD) pattern supported the crystallinity of Col-AgNPs and AgNPs. The drug loading of Col-AgNPs was 11.55 ± 0.93%. Col-AgNPs had higher activity against Gram-negative bacteria (, , and ) than AgNPs and colistin. The mechanism of actions of Col-AgNPs involved membrane disruption and genomic DNA damage. The Col-AgNPs and AgNPs were biocompatible with human red blood cells and renal cells at concentrations up to 16 µg/mL. Interestingly, Col-AgNPs exhibited higher cell survival than AgNPs and colistin at 32 µg/mL. Our results revealed that the Col-AgNPs could enhance the antimicrobial activity and cell biocompatibility more than colistin and AgNPs.
黏菌素是一种有效的针对革兰氏阴性菌的强效多肽抗生素。然而，其肾毒性限制了其临床应用。纳米银颗粒（AgNPs）作为一种潜在的抗菌剂和纳米药物载体受到了广泛关注。将抗生素与 AgNPs 结合已被发现可以提高其活性并降低药物毒性。在这项研究中，黏菌素与 AgNPs （Col-AgNPs）结合，这一点通过傅里叶变换红外（FT-IR）和能谱（EDX）光谱得到了证实。优化后的 Col-AgNPs 具有适当的特性，包括球形、单分散性、纳米尺寸、高表面电荷和良好的稳定性。粉末 X 射线衍射（PXRD）图谱支持了 Col-AgNPs 和 AgNPs 的结晶度。Col-AgNPs 的载药量为 11.55±0.93%。Col-AgNPs 对革兰氏阴性菌（,, 和 ）的活性高于 AgNPs 和黏菌素。Col-AgNPs 的作用机制涉及到细胞膜的破坏和基因组 DNA 的损伤。Col-AgNPs 和 AgNPs 在浓度高达 16μg/mL 时对人红细胞和肾细胞均具有生物相容性。有趣的是，在 32μg/mL 时，Col-AgNPs 的细胞存活率高于 AgNPs 和黏菌素。我们的研究结果表明，与黏菌素和 AgNPs 相比，Col-AgNPs 可以增强抗菌活性和细胞生物相容性。
