天然蛋白酪氨酸磷酸酶-1B抑制剂的研究进展  

Research Progress on Inhibitors of Natural Protein Tyrosine Phosphatase-1B

作　　者：郭忠秋 王欣[1] 韩佳婧 刘宇[1] 

机构地区：[1]辽宁大学药学院,辽宁沈阳

出　　处：《药物资讯》2018年第6期129-140,共12页Pharmacy Information

摘　　要：蛋白酪氨酸磷酸酶-1B (PTP1B)是胰岛素信号转导途径中重要的负调控因子。PTP1B通过使胰岛素受体及其底物的酪氨酸残基去磷酸化从而破坏胰岛素信号转导。近年来,作为治疗2型糖尿病的新靶点,有关PTP1B抑制剂的研究引起了广泛关注。中国有丰富的植物资源,通过对天然产物进行提取,可以获得一些有活性的PTP1B抑制剂。高效PTP1B抑制剂的发现可以为2型糖尿病的治疗提供新的途径。本文根据PTP1B抑制剂的结构类型,综述了一些具有代表性的天然PTP1B抑制剂的研究进展,包括溴酚类化合物,黄铜化合物,萜类化合物,香豆素类化合物等。表明深入研究PTP1B及其有效的抑制剂对于治疗2型糖尿病具有很好的发展前景。Protein tyrosine phosphatase-1B (PTP1B) is a major negative regulator in insulin signal transduction pathways. In recent years, as a new target for the treatment of type 2 diabetes, the study of PTP1B inhibitors has attracted extensive attention. PTP1B disrupts the insulin signal transduction by dephosphorylating phosphotyrosine residues of insulin receptor and its substrates. China has plenty of plant resources, through the extraction of natural products, some active PTP1B inhibitors can be obtained. The discovery of highly effective inhibitors of PTP1B can provide a new way to treat type 2 diabetes. In this paper, according to the structural types of PTP1B inhibitors, the research progress of some representative natural PTP1B inhibitors is reviewed, including bromophenol compounds, brass compounds, terpenoid compounds, coumarin compounds and others, which shows that further study of PTP1B and its potent inhibitors have good prospects for the treatment of type 2 diabetes.

关 键 词：蛋白酪氨酸磷酸酶-1B 2型糖尿病 抑制剂 天然化合物 

分 类 号：R28[医药卫生—中药学]