Microbial Biotechnology Laboratory, CSIR-Institute of Genomics and Integrative Biology, Sukhdev Vihar, New Delhi, 110025, India; Department of Biomedical Sciences, Acharya Narendra Dev College, University of Delhi, Kalkaji, New Delhi, 110019, India.
Nucleic Acids Research Laboratory, CSIR-Institute of Genomics and Integrative Biology, Mall Road, Delhi, 110007, India.
Mater Sci Eng C Mater Biol Appl. 2020 Feb;107:110284. doi: 10.1016/j.msec.2019.110284. Epub 2019 Oct 15.
Development of nanoparticle- and self-assembled nanomaterial-based therapeutics has become a rapidly growing area in the field of nanotechnology. One of the natural compounds, dopamine, presents as a neurotransmitter in the human brain serving as a messenger and deals with the behavioural responses, has provided an ideal platform through self-polymerization under aerobic conditions leading to the formation of a beneficial organic biopolymer, polydopamine (PDA). This polymer provides sufficient reactive functionalities, which can further be use to attach amine- or thiol-containing ligands to obtain conjugates. In the present study, self-polymerized polydopamine nanoparticles have been synthesized and tethered to aminoglycosides (AGs: Gentamicin, Kanamycin and Neomycin) through amino moieties to obtain PDA-AG nanoconjugates. These nanoconjugates are characterized by physicochemical techniques and evaluated for their antimicrobial potency against various bacterial strains including resistant ones. Simultaneously, cytocompatibility was also assessed for PDA-AG nanoconjugates. Of these three nanoconjugates (PDA-Gentamicin, PDA-Kanamycin and PDA-Neomycin), PDA-Kanamycin (PDA-K) nanoconjugate exhibited the highest activity against potent pathogens, least toxicity in human embryonic kidney (HEK 293) cells and intense toxic effects on human glioblastoma (U87) cells. Together, these results advocate the promising potential of these nanoconjugates to be used as potent antimicrobials in future applications.
基于纳米粒子和自组装纳米材料的治疗方法的发展已经成为纳米技术领域的一个快速增长的领域。多巴胺是一种天然化合物，作为人类大脑中的神经递质，作为信使，处理行为反应，它提供了一个理想的平台，通过有氧条件下的自聚合形成有益的有机生物聚合物，聚多巴胺（PDA）。这种聚合物提供了足够的反应性功能，可以进一步用于连接含有胺基或巯基的配体以获得缀合物。在本研究中，通过氨基部分将自聚合的聚多巴胺纳米颗粒与氨基糖苷（AG：庆大霉素、卡那霉素和新霉素）键合，得到 PDA-AG 纳米缀合物。这些纳米缀合物通过物理化学技术进行表征，并评估它们对各种细菌菌株（包括耐药菌株）的抗菌效力。同时，还评估了 PDA-AG 纳米缀合物的细胞相容性。在这三种纳米缀合物（PDA-庆大霉素、PDA-卡那霉素和 PDA-新霉素）中，PDA-卡那霉素（PDA-K）纳米缀合物对有效病原体表现出最高的活性，对人胚肾（HEK 293）细胞的毒性最小，对人神经胶质瘤（U87）细胞的毒性最强。总之，这些结果表明这些纳米缀合物具有作为未来应用中潜在的强效抗菌剂的潜力。
