Drug Discovery Lab, Life Science Division, Institute of Advanced Study in Science and Technology (IASST), Paschim Boragaon, Garchuk, Guwahati 781035, Assam, India.
Dr. B. Borooah Cancer Institute, Guwahati, Assam, India; Department of Applied Sciences, Gopinath Bordoloi Nagar, Jalukbari, Gauhati University, Guwahati 781014, Assam, India.
Mater Sci Eng C Mater Biol Appl. 2016 Apr 1;61:720-7. doi: 10.1016/j.msec.2015.12.078. Epub 2015 Dec 30.
In this study, we have described the biosynthesis of biocompatible gold nanoparticles (GNPs) from aqueous extract of the aerial parts of a pteridophyte, "Adiantum philippense" by microwave irradiation and its surface functionalization with broad spectrum beta lactam antibiotic, amoxicillin (Amox). The functionalization of amoxicillin on GNPs (GNP-Amox) was carried out via electrostatic interaction of protonated amino group and thioether moiety mediated attractive forces. The synthesized GNPs and GNP-Amox were physicochemically characterized. UV-Vis spectroscopy, Zeta potential, XRD, FTIR and SERS (surface enhanced raman spectra) results confirmed the loading of Amox into GNPs. Loading of Amox to GNPs reduce amoxicillin cytotoxicity, whereas GNPs were found to be nontoxic to mouse fibroblast cell line (L929) as evident from MTT and acridine orange/ethidium bromide (AO/EtBr) live/dead cell assays. The GNP-Amox conjugates demonstrated enhanced broad-spectrum bactericidal activity against both Gram-positive and Gram-negative bacteria. Furthermore, in-vitro and in-vivo assays of GNP-Amox revealed potent anti-MRSA activity and improved the survival rate. This indicates the subversion of antibiotic resistance mechanism by overcoming the effect of high levels of β-lactamase produced by methicillin resistant Staphylococcus aureus (MRSA). Taken together, this study demonstrates the positive attributes from GNP-Amox conjugates as a promising antibacterial therapeutic agent against MRSA as well as other pathogens.
在这项研究中，我们描述了通过微波辐射从蕨类植物“凤尾蕨”的气生部分的水提物中生物合成生物相容性的金纳米颗粒（GNPs）及其与广谱β-内酰胺抗生素阿莫西林（Amox）的表面功能化。Amox 在 GNPs（GNP-Amox）上的功能化是通过质子化氨基和硫醚部分介导的吸引力之间的静电相互作用进行的。合成的 GNPs 和 GNP-Amox 进行了物理化学表征。紫外-可见光谱、Zeta 电位、XRD、FTIR 和 SERS（表面增强拉曼光谱）结果证实了 Amox 加载到 GNPs 上。Amox 加载到 GNPs 上降低了阿莫西林的细胞毒性，而 MTT 和吖啶橙/溴化乙锭（AO/EtBr）活/死细胞测定显示 GNPs 对小鼠成纤维细胞系（L929）无毒性。GNP-Amox 缀合物表现出对革兰氏阳性和革兰氏阴性细菌的增强的广谱杀菌活性。此外，GNP-Amox 的体内和体内试验显示出强大的抗 MRSA 活性并提高了存活率。这表明通过克服耐甲氧西林金黄色葡萄球菌（MRSA）产生的高水平β-内酰胺酶的影响来颠覆抗生素耐药机制。总之，这项研究表明，GNP-Amox 缀合物具有作为抗 MRSA 以及其他病原体的有前途的抗菌治疗剂的积极属性。
