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水飞蓟素-硒纳米颗粒共轭物的合成及其体外生物活性研究。

Synthesis of silymarin-selenium nanoparticle conjugate and examination of its biological activity in vitro.

作者信息

Staroverov Sergey A, Kozlov Sergey V, Fomin Alexander S, Gabalov Konstantin P, Khanadeev Vitaliy A, Soldatov Dmitry A, Domnitsky Ivan Yu, Dykman Lev A, Akchurin Sergey V, Guliy Olga I

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

ADMET DMPK. 2021 Nov 14;9(4):255-266. doi: 10.5599/admet.1023. eCollection 2021.

Abstract

Silymarin (Sil) was conjugated to selenium nanoparticles (SeNPs) to increase Sil bioavailability. The conjugates were monodisperse; the average diameter of the native SeNPs was ~ 20-50 ± 1.5 nm, whereas that of the conjugates was 30-50 ± 0.5 nm. The use of SeNPs to increase the bioavailability of Sil was examined with the MH-22a, EPNT-5, HeLa, Hep-2, and SPEV-2 cell lines. The EPNT-5 (glioblastoma) cells were the most sensitive to the conjugates compared to the conjugate-free control. The conjugates increased the activity of cellular dehydrogenases and promoted the penetration of Sil into the intracellular space. Possibly, SeNPs play the main part in Sil penetration of cells and Sil penetration is not associated with phagocytosis. Thus, SeNPs are promising for use as a Sil carrier and as protective antigens.

摘要

水飞蓟素(Sil)与硒纳米颗粒(SeNPs)结合以提高水飞蓟素的生物利用度。这些结合物是单分散的;天然SeNPs的平均直径约为20 - 50 ± 1.5纳米,而结合物的平均直径为30 - 50 ± 0.5纳米。使用MH - 22a、EPNT - 5、HeLa、Hep - 2和SPEV - 2细胞系研究了SeNPs提高水飞蓟素生物利用度的情况。与无结合物的对照相比,EPNT - 5(胶质母细胞瘤)细胞对结合物最为敏感。这些结合物增加了细胞脱氢酶的活性,并促进水飞蓟素渗透到细胞内空间。可能,SeNPs在水飞蓟素进入细胞过程中起主要作用,且水飞蓟素的渗透与吞噬作用无关。因此,SeNPs有望用作水飞蓟素载体和保护性抗原。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d6f7/8920099/164e3b0aec06/admet-9-1023-g001.jpg

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