Protein Tyrosine Phosphatase 1B Inhibitory Activity of Lavandulyl Flavonoids from Roots of Sophora flavescens
Protein Tyrosine Phosphatase 1B Inhibitory Activity of Lavandulyl Flavonoids from Roots of Sophora flavescens
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DOI：
10.1055/s-0034-1368400
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发表时间：
2014-05-01
期刊：
影响因子：
2.7
通讯作者：
Koike, Kazuo
中科院分区：
文献类型：
--
作者：
Sasaki, Tatsunori;Li, Wei;Koike, Kazuo
蛋白酪氨酸磷酸酶1B（Protein tyrosine phosphatase 1B，PTP 1B）是一种非跨膜蛋白酪氨酸磷酸酶，是胰岛素信号转导通路中的主要负调控因子，因此PTP 1B抑制剂作为糖尿病的潜在治疗药物受到广泛关注。通过对天然化合物库的筛选，从苦参根中分离得到5个新的PTP 1B抑制剂化合物：kuraridin（1）、norkurarinone（2）、kurarinone（3）、2 '-methoxykurarinone（4）和kushenol T（5）。三种最有效的化合物1、2和4（IC 50
Protein tyrosine phosphatase 1B is a non-transmembrane protein tyrosine phosphatase and major negative regulator in insulin signaling cascades, and much attention has been paid to protein tyrosine phosphatase 1B inhibitors as potential therapies for diabetes. The screening of a natural compound library led to the discovery of five lavandulyl flavonoids, which were isolated from the roots of Sophora flavescens, as novel PTP1B inhibitors: kuraridin (1), norkurarinone (2), kurarinone (3), 2'-methoxykurarinone (4), and kushenol T (5). The three most potent compounds, 1, 2, and 4 (IC50