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Design of Peptide-Based Probes for the Microscale Detection of Reactive Oxygen Species

机译:基于肽的反应性氧物质检测探头的设计

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摘要

Reactive oxygen species (ROS) can induce oxidative stress and are associated with cell death and chronic diseases in organisms. In the treatment of disease, drugs that induce ROS are associated with many side effects and unpleasant symptoms. Therefore, during the assessment of new drugs and candidate compounds, ROS generation is an issue of concern; because ROS can modify proteins, lipids, and nucleic acids within organisms and alter their biological functions. In this work, we designed a peptide-based probe for the rapid (<10 mm) high-throughput survey of oxidative stress induced by clinical drugs at the microliter level. Using menadione and H2O2 as positive controls, just 100 mu g/mL of the test compound and 100 mu g/mL of the probe were sufficient effectively monitor the generation of ROS, which is important as many active compounds are rare and difficult to isolate or purify. This in vitro evaluation could be used to effectively generate preliminary data before pharmacologically active candidate compounds are processed in cell-line or animal tests. Furthermore, we demonstrated that this peptide probe successfully detects ROS in biological samples.
机译:活性氧物质(ROS)可以诱导氧化应激,与生物体中的细胞死亡和慢性病有关。在治疗疾病中,诱导ROS的药物与许多副作用和令人不快的症状有关。因此,在评估新药和候选化合物期间,ROS生成是一个关注的问题;因为ROS可以在生物体内修饰蛋白质,脂质和核酸并改变它们的生物学功能。在这项工作中,我们设计了一种基于肽的探针,用于快速(<10 mm)高通量调查的临床药物在微透镜水平上诱导的氧化应激。使用Menadione和H 2 O 2作为阳性对照,只有100μg/ ml的试验化合物和100μg/ ml探针的探针是充分的有效监测RO的产生,这是重要的,因为许多活性化合物很少且难以分离或难以分离净化。在体外评估中可用于在药理学活性候选化合物在细胞系或动物试验中加工之前有效地产生初步数据。此外,我们证明了该肽探针在生物样品中成功地检测ROS。

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  • 来源
    《Analytical chemistry》 |2017年第20期|共6页
  • 作者单位

    Kaohsiung Med Univ Res Ctr Environm Med Kaohsiung 80708 Taiwan;

    Kaohsiung Med Univ Sch Pharm Coll Pharm Kaohsiung 80708 Taiwan;

    Natl Sun Yat Sen Univ Dept Chem Coll Sci Kaohsiung 80424 Taiwan;

    Kaohsiung Med Univ Res Ctr Environm Med Kaohsiung 80708 Taiwan;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 分析化学;
  • 关键词

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