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首页> 外文期刊>Chemical and Pharmaceutical Bulletin >Chemical Constituents from Sambucus adnata and Their Protein–Tyrosine Phosphatase 1B Inhibitory Activities
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Chemical Constituents from Sambucus adnata and Their Protein–Tyrosine Phosphatase 1B Inhibitory Activities

机译:接骨木的化学成分及其蛋白酪氨酸磷酸酶1B的抑制活性

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The MeOH extract from the whole plants of Sambucus adnata has shown significant protein–tyrosine phosphatase 1B (PTP1B) inhibitory activity. Chemical study on the extract resulted in the isolation of thirteen compounds, including a novel triterpene ( 1 ). The structure of 1 was determined to be 1α,3β-dihydroxy-urs-12-en-11-one-3-yl palmitate on the basis of extensive spectroscopic analyses. Among the isolated compounds, ursolic acid, oleanolic acid and (±)-boehmenan showed the most potent PTP1B inhibitory activity in vitro with the IC50 values of 4.1, 14.4 and 43.5 μm, respectively. The kinetic analysis indicated that (±)-boehmenan inhibits PTP1B activity in a competitive manner.
机译:从接骨木的整个植物中提取的MeOH表现出显着的蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性。对提取物的化学研究导致分离出13种化合物,包括新型三萜(1)。根据广泛的光谱分析,确定1的结构为1α,3β-二羟基-urs-12-en-11-one-3-基棕榈酸酯。在分离出的化合物中,熊果酸,齐墩果酸和(±)-波美南酮在体外显示出最有效的PTP1B抑制活性,IC 50 分别为4.1、14.4和43.5μm。动力学分析表明,(±)-波美南以竞争性方式抑制PTP1B活性。

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