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首页> 外文期刊>Chinese science bulletin >Inhibition of bromophenols against PTP1B and anti-hyperglycemic effect of Rhodomela confervoides extract in diabetic rats
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Inhibition of bromophenols against PTP1B and anti-hyperglycemic effect of Rhodomela confervoides extract in diabetic rats

机译：溴酚对PTP1B的抑制作用和红景天提取物对糖尿病大鼠的降血糖作用

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摘要

Protein tyrosine phosphatase 1B (PTP1B) plays an important role as a negative regulator in insulin signaling pathways. PTP1B is an effective target for the treatment of type 2 diabetes mellitus. Four bromophenol derivatives from red algae Rhodomela confervoides, 2,2',3,3'-tetrabromo-4,4',5,5'-tetra-hydroxydiphenyl methane (1), 3-bormo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl) pyrocatechol (2), bis(2,3-dibromo-4,5-dihydroxybenzyl) ether (3) and 2,2',3-tribromo-3',4,4',5-tetrahydroxy-6'-ethyloxy-methyldiphenylmethane (4) showed significant inhibitory activity against PTP1B (IC50 were 2.4, 1.7, 1.5 and 0.84 mu mol/L, respectively) as potential therapeutical agents for the treatment of type 2 diabetes mellitus. The anti-hyperglycemic effects of the ethanol extracts from R. confervoides on streptozotocin-induced diabetes (STZ-diabetes) in male Wistar rats fed with high fat diet were investigated. The STZ-diabetic rats treated with medium-dose and high-dose alga extracts showed remarkable reductions in fasting blood glucose (FBG) as compared with the STZ-diabetic control. The results indicate that the in vivo anti-hyperglycemic activity of the R. confervoides extracts can be partially attributed to the inhibitory actions against PTP1B of the bromophenol derivatives and that may be of clinical importance in improving the management of type 2 diabetes mellitus.
机译：蛋白酪氨酸磷酸酶1B（PTP1B）在胰岛素信号通路中作为负调节剂发挥重要作用。 PTP1B是治疗2型糖尿病的有效靶标。红藻Rhodomela中的四种溴酚衍生物赋予2,2'，3,3'-tetrabromo-4,4'，5,5'-四羟基二苯甲烷（1），3-bormo-4,5-bis（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'-乙氧基-甲基二苯甲烷（4）对PTP1B具有显着的抑制作用（IC50分别为2.4、1.7、1.5和0.84μmol/ L），可作为治疗2型糖尿病的潜在治疗剂。研究了红花乙醇提取物对高脂饮食喂养的雄性Wistar大鼠链脲佐菌素诱发的糖尿病（STZ-糖尿病）的抗降血糖作用。与STZ糖尿病对照组相比，用中剂量和高剂量藻类提取物治疗的STZ糖尿病大鼠的空腹血糖（FBG）明显降低。结果表明，红景天提取物的体内抗高血糖活性可以部分归因于对溴酚衍生物的PTP1B的抑制作用，并且在改善2型糖尿病的治疗中可能具有重要的临床意义。

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