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首页> 外文期刊>Future medicinal chemistry >Anticancer properties of the abietane diterpene 6,7-dehydroroyleanone obtained by optimized extraction
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Anticancer properties of the abietane diterpene 6,7-dehydroroyleanone obtained by optimized extraction

机译:通过优化提取获得的上一亚硝基苯6,7-脱氢素的抗癌性能

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摘要

Aim: 6,7-dehydroroyleanone (DHR) is a cytotoxic abietane present in the essential oil of Plectranthus madagascariensis. Methods/results: Different extraction parameters were tested, and its extraction optimization was accomplished with a Clevenger apparatus-based hydrodistillation. After isolation, its effect on microtubules, P-glycoprotein and caspases was assessed on several cell lines and the compound was coupled with hybrid nanoparticles. The results show that DHR does not interfere with microtubule formation, but evades the resistance mechanisms of P-glycoprotein. Strong activation of caspases-3 and -9 indicates that DHR is able to induce apoptosis by triggering the intrinsic cell death pathway. Moreover, the assembly of DHR with hybrid nanoparticles was able to potentiate the effect of DHR in cancer cells. Conclusion: DHR seems to be a promising starting material with anticancer properties to further be explored.
机译:目的:6,7-脱氢罗西酮(DHR)是一种存在于Plectranthus Madagascariensis的精油中的细胞毒性海丹。 方法/结果:测试了不同的提取参数,其提取优化是用基于夹夹的含量的氢化物完成的。 在分离后,在几种细胞系上评估其对微管,P-糖蛋白和胱天膜酶的影响,并将化合物与杂交纳米颗粒偶联。 结果表明,DHR不会干扰微管形成,但避免了p-糖蛋白的抗性机制。 Caspases-3和-9的强烈活化表明DHR能够通过引发内在细胞死亡途径来诱导细胞凋亡。 此外,DHR与杂化纳米粒子的组装能够提高DHR在癌细胞中的作用。 结论:DHR似乎是具有抗癌特性的有前途的起始材料,以进一步探索。

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  • 来源
    《Future medicinal chemistry》 |2018年第10期|共13页
  • 作者单位

    Univ Lusofona Humanidades &

    Tecnol Res Ctr Biosci &

    Hlth Technol CBIOS P-1749024 Lisbon Portugal;

    Univ Alcala De Henares Fac Pharm Dept Biomed Sci Ctra A2 Km 33-600 Campus Univ Alcala De;

    Univ Lisbon Fac Farm Inst Invest Med iMed ULisboa P-1649003 Lisbon Portugal;

    Univ Lusofona Humanidades &

    Tecnol Res Ctr Biosci &

    Hlth Technol CBIOS P-1749024 Lisbon Portugal;

    Univ Lisbon Fac Ciencias CQB P-1749016 Lisbon Portugal;

    Univ Lusofona Humanidades &

    Tecnol Res Ctr Biosci &

    Hlth Technol CBIOS P-1749024 Lisbon Portugal;

    CSIC Ctr Invest Biol Ramiro Maeztu 9 Madrid 28040 Spain;

    Univ Belgrade Inst Biol Res Sinisa Stankovic Despota Stefana 142 Belgrade 11060 Serbia;

    Univ Las Palmas Gran Canaria Inst Univ Invest Biomed &

    Sanitarias Dept Biochem &

    Mol Biol Paseo;

    Univ Las Palmas Gran Canaria Inst Univ Invest Biomed &

    Sanitarias Dept Biochem &

    Mol Biol Paseo;

    Univ Las Palmas Gran Canaria Inst Univ Invest Biomed &

    Sanitarias Dept Biochem &

    Mol Biol Paseo;

    Univ Las Palmas Gran Canaria Inst Univ Invest Biomed &

    Sanitarias Dept Biochem &

    Mol Biol Paseo;

    Univ Alcala De Henares Fac Pharm Dept Biomed Sci Ctra A2 Km 33-600 Campus Univ Alcala De;

    Univ Lisbon Fac Farm Inst Invest Med iMed ULisboa P-1649003 Lisbon Portugal;

    Univ Lisbon Fac Farm Inst Invest Med iMed ULisboa P-1649003 Lisbon Portugal;

    Univ Belgrade Inst Biol Res Sinisa Stankovic Despota Stefana 142 Belgrade 11060 Serbia;

    Univ Lusofona Humanidades &

    Tecnol Res Ctr Biosci &

    Hlth Technol CBIOS P-1749024 Lisbon Portugal;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

    6; 7-dehydroroyleanone; cytotoxicity; extraction; isolation; multidrug resistance; nanotechnology; Plectranthus;

    机译:6;7-脱氢;细胞毒性;提取;隔离;多药抗性;纳米技术;尺寸;

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