Yang Jun Li, Ha Thi Kim Quy, Lee Ba Wool, Kim Jinwoong, Oh Won Keun
Korea Bioactive Natural Material Bank, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
Korea Bioactive Natural Material Bank, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
Bioorg Med Chem Lett. 2017 Nov 15;27(22):5076-5081. doi: 10.1016/j.bmcl.2017.09.031. Epub 2017 Sep 14.
To find PTP1B inhibitors from natural products, two new compounds (1 and 2), along with nine known compounds (3-11), were isolated from a methanol-soluble extract of Iris sanguinea seeds. The structures of compounds 1 and 2 were determined based on extensive spectroscopic data analysis including UV, IR, NMR, and MS. The IC value of compound 5 on protein tyrosine phosphatase 1B (PTP1B) inhibitory activity is 7.30±0.88µM with a little activity compared to the IC values of the tested positive compound. Compound 5 significantly enhanced glucose uptake and activation of pACC, pAMPK and partially Erk1/2 signaling. These results suggest that compound 5 from Iris sanguinea seeds are utilized as both PTP1B inhibitors and regulators of glucose uptake. These beneficial effects could be applied to treat metabolic diseases such as diabetes and obesity.
为了从天然产物中寻找蛋白酪氨酸磷酸酶1B（PTP1B）抑制剂，从鸢尾种子的甲醇可溶提取物中分离出两种新化合物（1和2）以及九种已知化合物（3 - 11）。基于包括紫外、红外、核磁共振和质谱在内的广泛光谱数据分析确定了化合物1和2的结构。化合物5对蛋白酪氨酸磷酸酶1B（PTP1B）的抑制活性IC值为7.30±0.88µM，与测试的阳性化合物的IC值相比活性较低。化合物5显著增强了葡萄糖摄取以及pACC、pAMPK和部分Erk1/2信号的激活。这些结果表明，鸢尾种子中的化合物5可作为PTP1B抑制剂和葡萄糖摄取调节剂。这些有益作用可应用于治疗糖尿病和肥胖症等代谢疾病。
