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桦木醇共轭金纳米颗粒作为稳定制剂在正常细胞和黑色素瘤细胞中的细胞毒性作用

The Cytotoxic Effects of Betulin-Conjugated Gold Nanoparticles as Stable Formulations in Normal and Melanoma Cells.

作者信息

Mioc Marius, Pavel Ioana Zinuca, Ghiulai Roxana, Coricovac Dorina E, Farcaş Claudia, Mihali Ciprian-Valentin, Oprean Camelia, Serafim Vlad, Popovici Ramona A, Dehelean Cristina A, Shtilman Michael I, Tsatsakis Aristidis M, Şoica Codruţa

机构信息

Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, Timişoara, Romania.

"George Emil Palade" Electron Microscopy Center, Institute of Life Sciences, "Vasile Goldiş" Western University of Arad, Arad, Romania.

出版信息

Front Pharmacol. 2018 May 3;9:429. doi: 10.3389/fphar.2018.00429. eCollection 2018.

Abstract

Gold nanoparticles are currently investigated as theranostics tools in cancer therapy due to their proper biocompatibility and increased efficacy related to the ease to customize the surface properties and to conjugate other molecules. Betulin, [lup-20(29)-ene-3β, 28-diol], is a pentacyclic triterpene that has raised scientific interest due to its antiproliferative effect on several cancer types. Herein we described the synthesis of surface modified betulin-conjugated gold nanoparticles using a slightly modified Turkevich method. Transmission electron microscopy (TEM) imaging, dynamic light scattering (DLS), scanning electron microscopy (SEM) and energy-dispersive X-ray spectroscopy (EDX) were used for the characterization of obtained gold nanoparticles. Cytotoxic activity and apoptosis assessment were carried out using the MTT and Annexin V/PI apoptosis assays. The results showed that betulin coated gold nanoparticles presented a dose-dependent cytotoxic effect and induced apoptosis in all tested cell lines.

摘要

由于金纳米颗粒具有良好的生物相容性,并且因其易于定制表面性质和偶联其他分子而提高了疗效,目前它们正作为癌症治疗中的诊疗工具进行研究。桦木醇,[羽扇 - 20(29)-烯 - 3β, 28 - 二醇],是一种五环三萜,因其对多种癌症类型具有抗增殖作用而引起了科学界的关注。在此,我们描述了使用略微改进的Turkevich方法合成表面修饰的桦木醇偶联金纳米颗粒。透射电子显微镜(TEM)成像、动态光散射(DLS)、扫描电子显微镜(SEM)和能量色散X射线光谱(EDX)用于表征所获得的金纳米颗粒。使用MTT和Annexin V/PI凋亡测定法进行细胞毒性活性和凋亡评估。结果表明,桦木醇包被的金纳米颗粒呈现出剂量依赖性细胞毒性作用,并在所有测试细胞系中诱导凋亡。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b20/5943567/9599dacfbc25/fphar-09-00429-g001.jpg

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