水飞蓟素-硒纳米颗粒缀合物的合成及其体外生物活性研究

IF 3.4 Q2 CHEMISTRY, MEDICINAL ADMET and DMPK Pub Date : 2021-11-14 DOI:10.5599/admet.1023
S. Staroverov, S. Kozlov, A. Fomin, K. Gabalov, Vitaliy Khanadeev, D. Soldatov, I. Domnitsky, L. Dykman, S. Akchurin, O. Guliy
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引用次数: 6

摘要

将水飞蓟素(Sil)与硒纳米粒子(SeNPs)偶联以提高硒的生物利用度。共轭物是单分散的;天然SeNPs的平均直径为~ 20 ~ 50±1.5 nm,而共轭物的平均直径为30 ~ 50±0.5 nm。用MH-22a、EPNT-5、HeLa、Hep-2和SPEV-2细胞系研究了SeNPs提高Sil生物利用度的作用。EPNT-5(胶质母细胞瘤)细胞对偶联物最敏感,与无偶联物对照相比。这些偶联物增加了细胞脱氢酶的活性,促进了Sil渗透到细胞内空间。可能,SeNPs在Sil渗透细胞中起主要作用,而Sil渗透与吞噬作用无关。因此,SeNPs有望用作Sil载体和保护性抗原。
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Synthesis of silymarin–selenium nanoparticle conjugate and examination of its biological activity in vitro
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.
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来源期刊
ADMET and DMPK
ADMET and DMPK Multiple-
CiteScore
4.40
自引率
0.00%
发文量
22
审稿时长
4 weeks
期刊介绍: ADMET and DMPK is an open access journal devoted to the rapid dissemination of new and original scientific results in all areas of absorption, distribution, metabolism, excretion, toxicology and pharmacokinetics of drugs. ADMET and DMPK publishes the following types of contributions: - Original research papers - Feature articles - Review articles - Short communications and Notes - Letters to Editors - Book reviews The scope of the Journal involves, but is not limited to, the following areas: - physico-chemical properties of drugs and methods of their determination - drug permeabilities - drug absorption - drug-drug, drug-protein, drug-membrane and drug-DNA interactions - chemical stability and degradations of drugs - instrumental methods in ADMET - drug metablic processes - routes of administration and excretion of drug - pharmacokinetic/pharmacodynamic study - quantitative structure activity/property relationship - ADME/PK modelling - Toxicology screening - Transporter identification and study
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