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一种新型细胞膜亲和样品预处理技术,用于识别和预浓缩中药中的活性成分。

A novel cell membrane affinity sample pretreatment technique for recognition and preconcentration of active components from traditional Chinese medicine.

机构信息

School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, 710061, China.

Shaanxi Engineering Research Center of Cardiovascular Drugs Screening & Analysis, Xi'an, 710061, China.

出版信息

Sci Rep. 2017 Jun 15;7(1):3569. doi: 10.1038/s41598-017-03709-6.

Abstract

We describe a novel biomembrane affinity sample pretreatment technique to quickly screen and preconcentrate active components from traditional Chinese medicine (TCM), which adopts cell membrane coated silica particles (CMCSPs) as affinity ligands which benefit the biomembrane's ability to maximize simulation of drug-receptor interactions in vivo. In this study, the prepared CMCSPs formed by irreversible adsorption of fibroblast growth factor receptor 4 (FGFR4) cell membrane on the surface of silica were characterized using different spectroscopic and imaging instruments. Drug binding experiments showed the excellent adsorption rate and adsorption capacity of FGFR4/CMCSPs compared with non-coated silica particles. The FGFR4/CMCSPs were used as solid-phase extraction sorbents to pretreat the TCM Aconitum szechenyianum Gay. The resultant FGFR4/CMCSPs exhibited good performance. In addition, high selectivity and recognition ability of the FGFR4/CMCSPs were determined by selectivity experiments. Four alkaloid were screened and identified, one of these alkaloid, napellonine, showed favorable anti-tumor activity in preliminary pharmacological verification trials including cell proliferation and molecular docking assays. The proposed cell membrane affinity sample pretreatment method is a reliable, effective and time-saving method for fast screening and enriching active compounds and can be extended to pretreat other TCMs as leading compounds resources.

摘要

我们描述了一种新型的生物膜亲和样品预处理技术,用于快速筛选和预浓缩中药(TCM)中的活性成分,该技术采用细胞膜包覆的硅粒子(CMCSPs)作为亲和配体,有利于模拟生物体内药物-受体相互作用的生物膜能力。在这项研究中,通过将成纤维细胞生长因子受体 4(FGFR4)细胞膜不可逆吸附在硅表面上,制备了 CMCSPs,并使用不同的光谱和成像仪器对其进行了表征。药物结合实验表明,FGFR4/CMCSPs 与非包覆硅粒子相比,具有优异的吸附率和吸附容量。FGFR4/CMCSPs 被用作固相萃取吸附剂,预处理中药乌头。所得的 FGFR4/CMCSPs 表现出良好的性能。此外,通过选择性实验确定了 FGFR4/CMCSPs 的高选择性和识别能力。筛选并鉴定了四种生物碱,其中一种生物碱,napellonine,在包括细胞增殖和分子对接实验在内的初步药理学验证试验中表现出良好的抗肿瘤活性。所提出的细胞膜亲和样品预处理方法是一种可靠、有效和省时的快速筛选和富集活性化合物的方法,可扩展用于预处理其他 TCM 作为先导化合物资源。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/01c2/5472601/501a25ad7c68/41598_2017_3709_Fig1_HTML.jpg

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