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Developing a Novel Gold(III) Agent to Treat Glioma Based on the Unique Properties of Apoferritin Nanoparticles: Inducing Lethal Autophagy and Apoptosis
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2020-11-13 , DOI: 10.1021/acs.jmedchem.0c01257
Juzheng Zhang 1 , Zhenlei Zhang 1 , Ming Jiang 1 , Shanhe Li 1 , Haoliang Yuan 2 , Hongbin Sun 2 , Feng Yang 1 , Hong Liang 1
Affiliation  

Effective delivery of anticancer agents across the blood–brain barrier (BBB) required innovative strategies to achieve glioma regression. To resolve this problem, we proposed to develop a metal agent that target and treat glioma based on the unique property of apoferritin (AFt) nanoparticles (NPs). Thus, we synthesized a series of Au(III) 3-(4-metyl piperidine)thiosemicarbazides compounds and analyzed their structure–activity relationships, obtaining a Au agent (C6) with remarkable cytotoxicity in glioma. Moreover, we confirmed that C6 kills glioma cells by inducing lethal autophagy and apoptosis. Importantly, our results revealed that the successfully constructed apoferritin-C6 NPs (AFt-C6 NPs) can effectively cross the BBB, inhibit glioma growth, and selectively accumulate in tumors.

中文翻译:

基于载铁蛋白纳米颗粒的独特性质,开发一种新型的金(III)药物治疗神经胶质瘤:诱导致命的自噬和细胞凋亡。

有效跨越血脑屏障(BBB)输送抗癌药物需要创新的策略来实现胶质瘤消退。为了解决这个问题,我们提议根据脱铁铁蛋白(AFt)纳米颗粒(NPs)的独特性质开发一种靶向和治疗神经胶质瘤的金属试剂。因此,我们合成了一系列Au(III)3-(4-甲基哌啶)硫代氨基脲化合物,并分析了它们的结构-活性关系,从而获得了对神经胶质瘤具有明显细胞毒性的Au试剂(C6)。此外,我们证实了C6通过诱导致命的自噬和凋亡来杀死神经胶质瘤细胞。重要的是,我们的结果表明,成功构建的脱铁铁蛋白-C6 NP(AFt-C6 NP)可以有效穿过血脑屏障,抑制神经胶质瘤生长,并选择性地在肿瘤中蓄积。
更新日期:2020-11-25
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