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首页> 外文期刊>Future medicinal chemistry >Ephedrine as a lead compound for the development of new DPP-IV inhibitors
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Ephedrine as a lead compound for the development of new DPP-IV inhibitors

机译：Ephedrine作为开发新的DPP-IV抑制剂的铅化合物

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Aim: Extracts from Ephedra species have been reported to be effective as antidiabetics. A previous in silico study predicted that ephedrine and five ephedrine derivatives could contribute to the described antidiabetic effect of Ephedra extracts by inhibiting dipeptidyl peptidase IV (DPP-IV). Finding selective DPP-IV inhibitors is a current therapeutic strategy for Type 2 diabetes mellitus management. Therefore, the main aim of this work is to experimentally determine whether these alkaloids are DPP-IV inhibitors. Materials & methods: The DPP-IV inhibition of Ephedra's alkaloids was determined via a competitive-binding assay. Then, computational analyses were used in order to find out the protein-ligand interactions and to perform a lead optimization. Results: Our results show that all six molecules are DPP-IV inhibitors, with IC50 ranging from 124 mu M for ephedrine to 28 mM for N-methylpseudoephedrine. Conclusion: Further computational analysis shows how Ephedra's alkaloids could be used as promising lead molecules for designing more potent and selective DPP-IV inhibitors.
机译：目的：据报道，来自Ephedra物种的提取物作为抗透氧剂是有效的。在三硅研究中预测，通过抑制二肽基肽酶IV（DPP-IV），麻黄碱和五种麻黄碱衍生物可以有助于Ephedra提取物的描述抗糖尿病效应。寻找选择性DPP-IV抑制剂是2型糖尿病管理的当前治疗策略。因此，这项工作的主要目的是通过实验确定这些生物碱是否是DPP-IV抑制剂。材料和方法：通过竞争性结合测定测定EpheDra的生物碱的DPP-IV抑制。然后，使用计算分析以找出蛋白质 - 配体相互作用并进行铅优化。结果：我们的研究结果表明，所有六种分子都是DPP-IV抑制剂，IC50从124 mu m范围内，对于N-甲基施霉素的Ephedrine为28mm。结论：进一步的计算分析表明，EpheDra的生物碱如何用作具有更有效和选择性DPP-IV抑制剂的有前途的铅分子。

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