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水飞蓟宾-金纳米粒子缀合物的合成及其护肝活性分析。

Synthesis of Silymarin-Gold Nanoparticle Conjugate and Analysis of its Liver-Protecting Activity.

机构信息

Saratov State Agrarian University, Saratov, Russian Federation.

Institute of Biochemistry and Physiology of Plants and Microorganisms, Russian Academy of Sciences, Saratov, Russian Federation.

出版信息

Curr Pharm Biotechnol. 2021;22(15):2001-2007. doi: 10.2174/1389201022666210101163734.

Abstract

BACKGROUND

The liver disease problem prompts investigators to search for new methods of liver treatment.

INTRODUCTION

Silymarin (Sil) protects the liver by reducing the concentration of free radicals and the extent of damage to the cell membranes. A particularly interesting method to increase the bioavailability of Sil is to use synthesized gold nanoparticles (AuNPs) as reagents. The study considered whether it was possible to use the silymarin-AuNP conjugate as a potential liver-protecting drug.

METHODS

AuNPs were conjugated to Sil and the liver-protecting activity of the conjugate was examined. Experimental hepatitis and hepatocyte cytolysis after carbon tetrachloride action were used as a model system, and the experiments were conducted with laboratory animals.

RESULTS

For the first time, silymarin was conjugated to colloidal gold nanoparticles (AuNPs). Electron microscopy showed that the resultant preparations were monodisperse and that the mean conjugate diameter was 18-30 nm ± 0.5 nm (mean diameter of the native nanoparticles, 15 ± 0.5 nm). In experimental hepatitis in mice, conjugate administration interfered with glutathione depletion in hepatocytes in response to carbon tetrachloride. It also was conducive to an increase in energy metabolism and stimulated the monocyte-macrophage function of the liver. The results were confirmed by the high respiratory activity of the hepatocytes in cell culture.

CONCLUSION

We conclude that the silymarin-AuNP conjugate holds promise as a liver-protecting agent in acute liver disease caused by carbon tetrachloride poisoning.

摘要

背景

肝脏疾病问题促使研究人员寻找新的肝脏治疗方法。

介绍

水飞蓟素(Sil)通过降低自由基浓度和细胞膜损伤程度来保护肝脏。增加 Sil 生物利用度的一种特别有趣的方法是使用合成的金纳米粒子(AuNPs)作为试剂。本研究考虑是否可以将水飞蓟素-AuNP 缀合物用作潜在的肝脏保护药物。

方法

AuNPs 与 Sil 缀合,并检查缀合物的肝脏保护活性。使用实验性肝炎和四氯化碳作用后的肝细胞溶解作为模型系统,在实验室动物中进行实验。

结果

首次将水飞蓟素与胶体金纳米粒子(AuNPs)缀合。电子显微镜显示,所得制剂为单分散的,平均缀合直径为 18-30nm±0.5nm(原生纳米粒子的平均直径为 15±0.5nm)。在小鼠实验性肝炎中,缀合物的给药干扰了四氯化碳引起的肝细胞中谷胱甘肽的耗竭。它还有利于增加能量代谢并刺激肝脏的单核细胞-巨噬细胞功能。细胞培养中肝细胞的高呼吸活性证实了这一结果。

结论

我们得出结论,水飞蓟素-AuNP 缀合物有望成为四氯化碳中毒引起的急性肝疾病的肝脏保护剂。

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