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蛋白酪氨酸磷酸酶1B(PTP1B)是胰岛素信号转导过程中的重要负调控因子,PTP1B是治疗2型糖尿病的有效靶点.来源于海洋红藻松节藻Rhodomela confervoides的4个溴酚类化合物,2,2′,3,3′-四溴-4,4′,5,5′-四羟基二苯甲烷(1),3-溴-4,5-双-(2,3-二溴-4,5-二羟基苄基)-邻苯二酚(2),双-(2,3-二溴-4,5-二羟基苄基)-醚(3)和2,2′,3-三溴-3′,4,4′,5-四羟基-6′-乙氧甲基二苯甲烷(4),表现出强烈的PTP1B抑制活性(IC50分别为2.4,1.7,1.5和0.84μmol/L),可能成为一类新型的2型糖尿病治疗药物.采用高脂饮食、链脲佐菌素诱导的2型糖尿病大鼠模型对松节藻的乙醇提取物进行了体内降血糖实验,结果表明,与糖尿病模型组相比,海藻醇提取物的中、高剂量组表现出显著的降血糖疗效.该研究表明,松节藻醇提取物体内良好的降血糖功效可能部分通过溴酚化合物对PTP1B酶活性抑制途径起作用,这对于2型糖尿病的治疗具有重要指导作用.
Protein tyrosine phosphatase 1B (PTP1B) is an important negative regulator in the process of insulin signal transduction. PTP1B is an effective target for the treatment of type 2 diabetes. Four bromophenols derived from Rhodomela conferringes Compounds, 2,2’,3,3’-tetrabromo-4,4’,5,5’-tetrahydroxydiphenylmethane (1), 3-bromo-4,5-bis-(2,3-bis Bromo-4,5-dihydroxybenzyl)-catechol (2), bis-(2,3-dibromo-4,5-dihydroxybenzyl)-ether (3) and 2,2’, 3-tribromo-3’,4,4’,5-tetrahydroxy-6’-ethoxymethyldiphenylmethane (4), exhibiting potent PTP1B inhibitory activity (IC50 of 2.4, 1.7, 1.5 and 0.84, respectively) Μmol/L) may become a novel type 2 diabetes mellitus therapeutic drug. In vivo hypoglycemic experiments were conducted on ethanol extracts of pine needles in a rat model of type 2 diabetes induced by high-fat diet and streptozotocin. The results showed that compared with the diabetic model group, the high dose group of alginate extract showed a significant hypoglycemic effect. This study showed that the good hypoglycemic effect in the rosarylin extract may partially pass the bromophenol compound Acts on PTP1B enzyme activity inhibition pathway, which treats type 2 diabetes There are important guiding role.