首页> 外文期刊>RSC Advances >In vitro antileishmanial activity of aza-scorpiand macrocycles. Inhibition of the antioxidant enzyme iron superoxide dismutase
【24h】

In vitro antileishmanial activity of aza-scorpiand macrocycles. Inhibition of the antioxidant enzyme iron superoxide dismutase

机译:AZA-SCORPIAND宏γ的体外抗体活动。 抑制抗氧化酶铁超氧化物歧化酶

获取原文
获取原文并翻译 | 示例
           

摘要

The in vitro leishmanicidal activity of a series of nine aza-scorpiand-like macrocycles, recently synthesized, was tested on Leishmania infantum, Leishmania braziliensis and Leishmania donovani parasites, using promastigotes and intracellular amastigotes forms. The cytotoxicity of the tested compounds on J774.2 macrophage cells was also measured. Four of the tested compounds (1, 2, 8 and 9) showed selectivity indexes higher than those of the reference drug Glucantime for the three Leishmania species. Moreover, the data on infection rates and on amastigotes showed that compounds 1, 2, 8 and 9 are the most active against the three Leishmania species. The changes in the excretion product profile of parasites treated with the four compounds (1, 2, 8 and 9) were also consistent with substantial cytoplasmic alterations. On the other hand, the most active compounds were potent inhibitors of Fe-SOD in the three parasite species considered, whereas their impact on human CuZn-SOD was low. The high activity, low toxicity, stability, low cost of the starting materials and straightforward synthesis make these compounds appropriate molecules for the development of affordable anti-leishmanicidal agents.
机译:最近合成的一系列九种Aza-scorpiand的宏杂种的体外Leishmanicatoral活性在Leishmania Infantum,Leishmania Braziliensis和Leishmania Donovani寄生虫上进行了测试,使用Promastigotes和细胞内Amastigotes形式。还测量了在J774.2巨噬细胞上的测试化合物的细胞毒性。四种测试化合物(1,2,8和9)显示了比三个LeishMania物种的参考药物葡萄糖的选择性指标高。此外,关于感染率和Amastigot的数据显示,化合物1,2,8和9对三种LeishMania物种最活跃。用四种化合物(1,2,8和9)处理的寄生虫的排泄产物谱的变化也与大量细胞质改变一致。另一方面,最活跃的化合物是在考虑的三种寄生虫物种中的Fe-SOD有效抑制剂,而它们对人Cuzn-Sod的影响很低。起始材料的高活性,低毒性,稳定性,低成本和直接合成使得这些化合物适当的分子用于显着的抗Leishmanicatoger的发育。

著录项

  • 来源
    《RSC Advances》 |2016年第21期|共10页
  • 作者单位

    Univ Granada Hosp Univ Granada Inst Invest Biosanitaria Ibs GRANADA Dept Parasitol Granada Spain;

    Univ Valencia Inst Ciencia Mol Dept Quim Inorgan E-46980 Paterna Valencia Spain;

    Univ Granada Hosp Univ Granada Inst Invest Biosanitaria Ibs GRANADA Dept Parasitol Granada Spain;

    Hosp Univ &

    Politecn La Fe GIBI 230 Valencia Spain;

    Univ Granada Hosp Univ Granada Inst Invest Biosanitaria Ibs GRANADA Dept Parasitol Granada Spain;

    Univ Valencia Inst Ciencia Mol Dept Quim Inorgan E-46980 Paterna Valencia Spain;

    Univ Valencia Inst Ciencia Mol Dept Quim Inorgan E-46980 Paterna Valencia Spain;

    Univ Granada Hosp Univ Granada Inst Invest Biosanitaria Ibs GRANADA Dept Parasitol Granada Spain;

    Univ Granada Hosp Univ Granada Inst Invest Biosanitaria Ibs GRANADA Dept Parasitol Granada Spain;

    Univ Valencia Inst Ciencia Mol Dept Quim Inorgan E-46980 Paterna Valencia Spain;

    Univ Granada Hosp Univ Granada Inst Invest Biosanitaria Ibs GRANADA Dept Parasitol Granada Spain;

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

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号