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首页> 外文期刊>RSC Advances >Cochinchinenin C, a potential nonpolypeptide anti-diabetic drug, targets a glucagon-like peptide-1 receptor
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Cochinchinenin C, a potential nonpolypeptide anti-diabetic drug, targets a glucagon-like peptide-1 receptor

机译：Cochinchinenin C，潜在的非β-抗糖尿病药物，靶向胰高血糖素肽-1受体

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摘要

The glucagon-like peptide-1 (GLP-1) receptor is currently being explored as a therapeutic target for antidiabetic drugs. GLP-1 analogs possess therapeutic effects similar to those of other anti-diabetic drugs such as guanidine and sulfonylureas but do not cause hypoglycemia and gastrointestinal discomfort. GLP-1 has the ability to reduce blood glucose in a glucose-dependent manner. Several GLP-1 analog agonists have been developed. However, polypeptide drugs are easily degraded by DPP4 in vivo. Therefore, the focus is now on the development of nonpolypeptide anti-diabetic drugs targeting the GLP-1 receptor. In this study, computer-aided drug design was applied to search for potential molecules of this type. Cochinchinenin C, extracted from sangusis draconi, interacted well with GLP-1 receptor via hydrophobic interaction, which was confirmed by fluorescence spectroscopy and molecular simulation. In cell experiments, it was demonstrated that pancreatic beta cells promoted insulin secretion upon treatment with cochinchinenin C, and increases of intracellular cAMP and ATP levels also occurred, indicating GLP-1 receptor activation and glucose metabolism. These results showed that cochinchinenin C has potential for the development of drugs for treating diabetes.
机译：目前正在探索胰高血糖素样肽-1（GLP-1）受体作为抗糖尿病药物的治疗靶标。 GLP-1类似物具有与其他抗糖尿病药物如胍和磺酰脲类等其他类似的治疗效果，但不会引起低血糖和胃肠道不适。 GLP-1能够以血糖依赖性方式降低血糖。已经开发了几种GLP-1类似物激动剂。然而，多肽药物在体内轻易降解DPP4。因此，重点现在正在靶向GLP-1受体的非聚合物抗糖尿病药物的发展。在本研究中，应用计算机辅助药物设计来搜索这种类型的潜在分子。从Sangusis Draconi中提取的CochinchinenIN C，通过疏水相互作用与GLP-1受体相互作用，通过荧光光谱和分子模拟证实。在细胞实验中，证明胰腺β细胞在用Cochinchinenin C处理后促进了胰岛素分泌，并且还发生了细胞内阵营和ATP水平的增加，表明GLP-1受体活化和葡萄糖代谢。这些结果表明，科钦宁蛋白C具有促进治疗糖尿病药物的发育。

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  • 来源
    《RSC Advances》 |2017年第77期|共9页
  • 作者

    Sha Yijie; Shi Yunfeng; Niu Bing; Chen Qin;

  • 作者单位

    Shanghai Univ Sch Life Sci Shanghai Key Lab Bioenergy Crops Shanghai Peoples R China;

    Shanghai Univ Sch Life Sci Shanghai Key Lab Bioenergy Crops Shanghai Peoples R China;

    Shanghai Univ Sch Life Sci Shanghai Key Lab Bioenergy Crops Shanghai Peoples R China;

    Shanghai Univ Sch Life Sci Shanghai Key Lab Bioenergy Crops Shanghai Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
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