瑞香狼毒根中的瑞塔尼酚 III 是一种 PTP1B 抑制剂。
Ratanhiaphenol III from Ratanhiae radix is a PTP1B inhibitor.
机构信息
Department of Pharmacognosy, University of Vienna, Vienna, Austria.
出版信息
Planta Med. 2012 May;78(7):678-81. doi: 10.1055/s-0031-1298242. Epub 2012 Feb 3.
Abstract
The inhibition of protein tyrosine phosphatase 1B (PTP1B) is considered a valid strategy to combat insulin resistance and type II diabetes. We show here that a dichloromethane extract of Ratanhiae radix ( RR_EX) dose-dependently inhibits human recombinant PTP1B in vitro and enhances insulin-stimulated glucose uptake in murine myocytes. By determination of the PTP1B inhibiting potential of 11 recently isolated lignan derivatives from RR_EX, the observed activity of the extract could be partly assigned to ratanhiaphenol III. This compound inhibited PTP1B in vitro with an IC (50) of 20.2 µM and dose-dependently increased insulin receptor phosphorylation as well as insulin-stimulated glucose uptake in cultured myotubes. This is the first report to reveal an antidiabetic potential for a constituent of rhatany root, traditionally used against inflammatory disorders, by showing its capability of inhibiting PTP1B.
摘要
蛋白酪氨酸磷酸酶 1B（PTP1B）的抑制被认为是对抗胰岛素抵抗和 2 型糖尿病的有效策略。我们在这里表明，瑞香科根（RR_EX）的二氯甲烷提取物在体外剂量依赖性地抑制人重组 PTP1B，并增强小鼠肌细胞中胰岛素刺激的葡萄糖摄取。通过测定 RR_EX 中最近分离的 11 种木脂素衍生物的 PTP1B 抑制潜力，提取物的观察到的活性部分归因于瑞香酚 III。该化合物在体外抑制 PTP1B 的 IC50 为 20.2 µM，并剂量依赖性地增加培养的肌管中的胰岛素受体磷酸化以及胰岛素刺激的葡萄糖摄取。这是第一个通过显示其抑制 PTP1B 的能力来揭示传统上用于治疗炎症性疾病的瑞香根成分的抗糖尿病潜力的报告。
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