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Enhanced antitumor activity of carbendazim on HeLa cervical cancer cells by aptamer mediated controlled release

机译:Aptamer介导的控制释放,增强了Carbendazim对HeLa宫颈癌细胞的抗肿瘤活性

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摘要

Carbendazim, is a broad-spectrum fungicide and also a promising experimental antitumor drug as reproduction and developmental toxicant, which is currently under phase II preclinical trials. In this study, an approach based on controlled and targeted release with aptamers and mesoporous silica nanoparticles was investigated to improve the antitumor activity of carbendazim. To this end, we synthesized aptamer conjugated silica nanoparticles for testing cytotoxicity properties in vitro with human cervical adenocarcinoma (HeLa) cultured cells. Nucleolin (AS1411) binding aptamers were used to entrap carbendazim molecules inside nanopores of MCM-41 type silica nanoparticles to obtain a stimuli-dependent release system. The effect of carbendazim loaded aptamer silica complex was tested and compared to free carbendazim treatment on HeLa cells, demonstrating 3.3 fold increase of toxicity on targeted cells with our delivery system. In addition, cytotoxicity of the complex was determined to be mostly due to increased apoptosis and to a less extend necrosis related pathways.
机译:Carbendazim是一种广谱杀菌剂,也是有前途的实验抗肿瘤药作为繁殖和发育毒性,目前在II期临床前试验。在本研究中,研究了一种基于受适体和中孔二氧化硅纳米粒子的受控和靶向释放的方法,以改善碳氮基菊酯的抗肿瘤活性。为此,我们合成适体缀合的二氧化硅纳米型纳米粒子,用于在体外用人宫颈腺癌(HELA)培养细胞进行细胞毒性特性。核仁(AS1411)结合适体用于捕获MCM-41型二氧化硅纳米粒子的纳米孔内的碳氮胶蛋草分子,得到刺激依赖性释放系统。测试了Carbendazim负载的适体二氧化硅复合物的效果,并与HeLa细胞的游离碳氮化治疗进行了比较,展示了靶向细胞的3.3倍的毒性与我们的递送系统。此外,该复合物的细胞毒性决定主要是由于凋亡增加和较少的延伸性坏死相关途径。

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    《RSC Advances》 |2019年第62期|共6页
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  • 正文语种 eng
  • 中图分类 化学;
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