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通过功能化金纳米粒子增强蛋白酶体抑制剂的效果。

Enhancing proteasome-lnhibitor effect by functionalized gold nanoparticles.

出版信息

J Biomed Nanotechnol. 2014 Apr;10(4):717-23. doi: 10.1166/jbn.2014.1743.

Abstract

Colloidal gold nanoparticles intensify the anticancer response of the drug bortezomib, a proteasome inhibitor. Polyethylene glycol-coated gold nanoparticles and the drug show a synergistic effect in reducing the cell viability of prostate cancer cell line Du145. It was observed a significant cell viability reduction with bortezomib concentrations as low as 4 nM. The proteasome inhibitor alone had to be present at concentrations in the ranger of 120 nM to induce identical cytotoxicity response. These findings demonstrate that gold nanoparticles enhancing the permeation and retention (EPR) effect in Du145 cells and open the possibility to decrease multi-drug resistance (MDR). The in vitro results of functionalized gold nanoparticles, internalized by cancer cells, pave the way for a more efficient proteasome inhibitor delivery and release in adenocarcinoma cells.

摘要

胶态金纳米粒子增强了蛋白酶体抑制剂硼替佐米的抗癌反应。聚乙二醇包覆的金纳米粒子和药物在降低前列腺癌细胞系 Du145 的细胞活力方面表现出协同作用。观察到硼替佐米浓度低至 4 nM 时就会显著降低细胞活力。单独使用蛋白酶体抑制剂时,必须在 120 nM 的范围内才能诱导相同的细胞毒性反应。这些发现表明,金纳米粒子增强了 Du145 细胞中的渗透和保留(EPR)效应,并为降低多药耐药性(MDR)提供了可能性。被癌细胞内化的功能化金纳米粒子的体外结果为更有效地将蛋白酶体抑制剂递送至并释放到腺癌细胞中铺平了道路。

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