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首页> 外文期刊>Journal of Pharmacy and Pharmacology >Benzyl sulforaphane is superior to sulforaphane in inhibiting the Akt/ MAPK MAPK and activating the Nrf2/ ARE ARE signalling pathways in HepG2 cells
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Benzyl sulforaphane is superior to sulforaphane in inhibiting the Akt/ MAPK MAPK and activating the Nrf2/ ARE ARE signalling pathways in HepG2 cells

机译:苄基苏尔素优异于抑制AKT / MAPK MAPK并激活NRF2 /是HepG2细胞中的信号传导途径

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摘要

Abstract Objectives Sulforaphane ( SFN ), an isothiocyanate found in cruciferous vegetables, has been reported to own anticarcinogenic, antiinflammatory and cancer chemopreventive properties. Benzyl sulforaphane ( BSFN ) was a derivative of SFN which was designed and synthesized by our laboratory. Here, the cancer prevention and anticancer effects of BSFN on human hepatoma (HepG2) cells were investigated. Methods The following effects of BSFN on components of the mitochondrial apoptotic pathway were examined: generation of reactive oxygen species and mitochondrial membrane potential (ΔΨm) changes by flow cytometry, the expression changes of Bcl‐2 family proteins and Akt/ MAPK proteins by western blot. The protein levels of Nrf2 and Keap1 were also tested via Western blot. The effects of BSFN on Nrf2 nuclear translocation and ARE ‐reporter gene activity?were examined by fluorescence microscope and multifunctional spectrophotometer. Key findings Benzyl sulforaphane could induce cell apoptosis by mitochondrion‐dependent pathway, which inhibited HepG2 cells growth in a manner of time‐ and concentration ‐dependent. Furthermore, BSFN could inhibit the Akt/ MAPK and activate the Nrf2/ ARE pathway in HepG2 cells. Conclusions Benzyl sulforaphane was superior to SFN in inhibiting Akt/ MAPK and activating Nrf2/ ARE signalling pathways in HepG2 cells, which indicated that BSFN could be a safe therapeutic strategy?for the prevention and treatment of liver cancer.
机译:摘要目标苏尔林(SFN)(SFN),据报道,在十字花植物中发现的异硫氰酸酯,据报道患有抗癌,抗炎和癌症化学预防性质。苄基苏尔林(BSFN)是SFN的衍生物,由我们的实验室设计和合成。这里,研究了BSFN对人肝癌(HepG2)细胞的癌症预防和抗癌效应。方法研究BSFN对线粒体凋亡途径组分的以下影响:通过流式细胞术,通过蛋白质印迹产生反应性氧物质和线粒体膜电位(Δεm)的产生,Bcl-2家族蛋白和Akt / Mapk蛋白的表达变化。也通过蛋白质印迹测试NRF2和Keap1的蛋白质水平。 BSFN对NRF2核转位的影响及 - 荧光显微镜和多功能分光光度计检测αsex基因活性。主要成分苄基苏尔素可以通过线粒体依赖性途径诱导细胞凋亡,其以时间和浓度的方式抑制HepG2细胞生长。此外,BSFN可以抑制AKT / MAPK并激活HepG2细胞中的NRF2 /是途径。结论苄基苏尔丙烷抑制AKT / MAPK中的SFN优于SFN,并激活NRF2 /位于HepG2细胞中的信号通路,表明BSFN可以是安全的治疗策略?用于预防和治疗肝癌。

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  • 来源
    《Journal of Pharmacy and Pharmacology》 |2018年第12期|共11页
  • 作者单位

    School of Pharmaceutical Engineering &

    Life ScienceChangzhou UniversityChangzhou Jiangsu China;

    School of Pharmaceutical Engineering &

    Life ScienceChangzhou UniversityChangzhou Jiangsu China;

    School of Pharmaceutical Engineering &

    Life ScienceChangzhou UniversityChangzhou Jiangsu China;

    School of PharmacyNantong UniversityNantong Jiangsu China;

    School of Pharmaceutical Engineering &

    Life ScienceChangzhou UniversityChangzhou Jiangsu China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药理学;
  • 关键词

    Akt/ MAPK; apoptosis; benzyl sulforaphane; mitochondria; Nrf2;

    机译:akt / mapk;细胞凋亡;苄基苏尔素;线粒体;nrf2;

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