Department of Nephrology, China-Japan Union Hospital of Jilin University, Changchun, China.
Department of Radiotherapy, The Second Hospital of Jilin University, Changchun, China.
J Biomol Struct Dyn. 2021 Apr;39(6):2014-2020. doi: 10.1080/07391102.2020.1749131. Epub 2020 Apr 9.
The unavoidable glycation reaction is the major cause of diabetes and metabolic disorders. The glycation reaction is enhanced in case when the glycating agent is reactive carbonyl species (RCS) like, methylglyoxal (MG). The impact of RCS may result into the diabetes mellitus and its secondary complications along-with its role in cancers too. This reaction can be discontinued by using natural product inhibitors or by chemically synthesized drugs, like aminoguanidine (AG). However, AG is reported to be nephrotoxic (toxic to kidneys) at a concentration of 10 mM or more and has therefore serious health concerns. In the present study, bioconjugation of AG was done with the gold nanoparticles (Gnps) to mitigate its toxic effect and upsurge the efficacy of AG on RCS induced glycation. The AG-Gnps formed waas characterized by UV-Vis. spectroscopy and it reveals a peak at 529 nm corresponding to AG-gold nanoparticles. The particle size of the AG-Gnp was found to be 12 nm in TEM while in DLS it was found to be 54.07 nm. The fluorescence studies in combination with GK-peptide and δ-Glu assay support the inhibition of AGEs by AG-Gnps. Based on the idea of gold nano-particle synthesis, it is anticipated, the toxicity of numerous drugs used at high doses can be diminished with additional efficiency.Communicated by Ramaswamy H. Sarma.
不可避免的糖化反应是糖尿病和代谢紊乱的主要原因。当糖化剂是反应性羰基物质（RCS）时，糖化反应会增强，如甲基乙二醛（MG）。RCS 的影响可能导致糖尿病及其继发性并发症，以及其在癌症中的作用。这种反应可以通过使用天然产物抑制剂或通过化学合成药物来中断，如氨基胍（AG）。然而，AG 被报道在 10mM 或更高浓度时具有肾毒性（对肾脏有毒），因此存在严重的健康问题。在本研究中，通过将 AG 与金纳米粒子（Gnps）进行生物缀合，来减轻其毒性作用，并提高 AG 对 RCS 诱导的糖化的疗效。AG-Gnps 通过紫外可见光谱进行了表征，在 529nm 处有一个峰，对应于 AG-金纳米粒子。TEM 中 AG-Gnp 的粒径为 12nm，而在 DLS 中为 54.07nm。荧光研究与 GK-肽和δ-Glu 测定相结合，支持 AG-Gnps 抑制 AGEs。基于金纳米粒子合成的想法，可以预期，许多高剂量使用的药物的毒性可以通过额外的效率来降低。由 Ramaswamy H. Sarma 传达。
