Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University (SJTU), 800 Dongchuan Road, Shanghai 200240, China.
Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University (SJTU), 800 Dongchuan Road, Shanghai 200240, China.
Bioorg Chem. 2019 Jun;87:12-15. doi: 10.1016/j.bioorg.2019.02.046. Epub 2019 Feb 22.
Type 2 diabetes mellitus is a fast-growing epidemic affecting people globally. We initiated the project by searching the possible target of the Pueraria lobata root extract (P. lobata). We conducted the IC assays of P. lobata on the four diabetes-related proteins: PTP1B, TCPTP, SHP-2 and DPP-4. Results indicated that P. lobata exhibited high PTP1B inhibitory activity with IC of 0.043 mg/ml. Treated insulin-resistant HepG2 cells with 0.0115 mg/ml of P. lobata increased the glucose uptake by two times compared with the negative control. Further, we performed OGTT test on the diabetic C57BL/6 male mice. 20% decreased blood glucose (AUC) was obtained with a dose of 1 g/kg P. lobata compared with the negative control. Herein, we were able to demonstrate the antidiabetic effects of P. lobata might be related to the inhibition of PTP1B and therefore, bettering the insulin signaling pathway.
2 型糖尿病是一种在全球范围内迅速流行的疾病。我们从寻找葛根提取物（葛根）的可能作用靶点开始启动了这个项目。我们对葛根进行了与四种糖尿病相关蛋白的 IC 测定实验：PTP1B、TCPTP、SHP-2 和 DPP-4。结果表明，葛根对 PTP1B 表现出高抑制活性，IC 为 0.043mg/ml。用 0.0115mg/ml 的葛根处理胰岛素抵抗 HepG2 细胞，与阴性对照相比，葡萄糖摄取增加了两倍。此外，我们在糖尿病 C57BL/6 雄性小鼠上进行了 OGTT 测试。与阴性对照相比，葛根 1g/kg 的剂量可使血糖（AUC）降低 20%。在此，我们能够证明葛根的抗糖尿病作用可能与抑制 PTP1B 有关，从而改善胰岛素信号通路。
