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首页> 外文期刊>RSC Advances >Simultaneous inhibition of EGFR and MET receptors with phytochemical conjugated magnetic nanocarriers: in silico and in vitro study
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Simultaneous inhibition of EGFR and MET receptors with phytochemical conjugated magnetic nanocarriers: in silico and in vitro study

机译：用植物化学缀合磁纳米载体同时抑制EGFR和MET受体：在硅和体外研究中

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摘要

Cross talk between Epidermal Growth Factor Receptor (EGFR) and hepatocyte growth factor or MET receptor has turned out to be a major challenge in cancer treatment. Inhibitors targeting both receptors, when expressed at elevated levels, can significantly reduce cancer cell progression. In the present work, methanolic extract (of Mentha piperita) coated super-paramagnetic iron oxide nanoparticles (SPIONs) were prepared and tested for effective inhibition of EGFR and MET receptors. Extract encapsulated SPIONs (20 +/- 5 nm) showed high stability (zeta potential -62.9 mV), antioxidant activity (96% at 1 mg ml(-1)) and non-haemolytic activity (upto 2.5 mg ml(-1)). Dose dependent inhibition of EGF and MET receptors by encapsulated SPIONs (IC50 = 67 mu g ml(-1)) was three-fold higher when compared to Mentha piperita extract. Molecular docking analysis with identified bioactive compounds revealed lowest binding energies for 1,3,8-P-menthatriene (-7.89 and -6.59 kcal mol(-1)), DL-alpha-tocopherol (-7.32 and -5.98 kcal mol(-1)) and beta-sitosterol (-9.22 and -6.27 kcal mol(-1)) towards EGFR and MET receptors, respectively. Hydrophobic interactions were found to be crucial for the best docked ligands' (beta-sitosterol, 1,3,8-P-menthatriene and DL-alpha-tocopherol) mediated EGFR/MET inhibition, irrespective of their hydrogen bonding.
机译：表皮生长因子受体（EGFR）和肝细胞生长因子或满足受体之间的交叉谈话证明是癌症治疗的主要挑战。靶向两个受体的抑制剂，当在升高的水平表达时，可以显着降低癌细胞进展。在本作工作中，制备并测试甲醇提取物（Mentha Piperita）涂覆的超级顺磁性氧化铁纳米颗粒（栓塞），以有效抑制EGFR并满足受体。提取物封装的酱（20 +/- 5nm）显示出高稳定性（Zeta电位-62.9mV），抗氧化活性（96％在1mg ml（-1））和非溶血活性（高达2.5mg ml（-1） ）。与Mentha Piperita提取物相比，封装酱（IC50 =67μg（-1））的剂量依赖性抑制和满足受体（IC50 =67μgml（-1））。具有鉴定的生物活性化合物的分子对接分析显示出1,3,8-p-inhathaterne（-7.89和-6.59kcal（-1）），dl-α-生育酚（-7.32和-5.98kcal摩尔（ - 1））和β-谷甾醇（-9.22和-6.27 kcal摩尔（-1））分别朝向EGFR和满足受体。发现疏水相互作用对于最佳停顿配体（β-谷甾醇，1,3,8-p-inhathatriene和D1-α-生育酚）是至关重要的，介导的EGFR / MET抑制，而不管它们的氢键如何。

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  • 来源
    《RSC Advances》 |2016年第83期|共12页
  • 作者

    Ilangovan Shanmuga Sundari; Sen Shampa;

  • 作者单位

    VIT Univ Sch Biosci &

    Technol Vellore Tamil Nadu India;

    VIT Univ Sch Biosci &

    Technol Vellore Tamil Nadu India;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
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