Ten active principles (compounds 1-10) have been isolated following protein tyrosine phosphatase 1B (PTP1B) assay-guided fractionation of the methanol extract of the root of Polygonum cuspidatum. The chemical structures of the compounds were characterized mainly by nuclear magnetic resonance (NMR) spectroscopic and physicochemical data. This is the first time that 9,10-anthraquinones (compounds 5-6) have been isolated from P. cuspidatum, and this is the first record of compound 9 from the genus Polygonum. Except for compound 4, all the isolates showed potential inhibitory activity against PTP1B with half-maximal inhibitory concentration IC₅₀ values ranging from 6.3 to 28.9 µM. Furthermore, a kinetic study indicated mixed-competitive inhibition with PTP1B for compounds 2 and 9 and noncompetitive inhibition for compounds 3 and 6. In addition, compounds 2, 3, 6, and 9 also induced the 2-deoxy-2-[(7-nitro-2,1,3-benzoxadiazol-4-yl) amino]-d-glucose uptake stimulation in 3T3-L1 adipocytes at concentrations of 10 and 5 µM. Taken together, the results reveal that P. cuspidatum could be a new source of natural compounds for further research and development of antidiabetic agents.

十活性成分（化合物1 - 10）已被分离下列蛋白质酪氨酸磷酸酶1B（PTP1B）测定引导的根的甲醇提取物的分馏虎杖。化合物的化学结构主要由核磁共振（NMR）光谱和理化数据表征。这是第一次，9,10-蒽醌（化合物5-6）已经从分离虎杖，这就是化合物的第一个记录9从该属蓼。化合物4除外，所有分离物均显示出对PTP1B的潜在抑制活性，其最大半数抑制浓度IC ₅₀值为6.3至28.9 µM。此外，动力学研究表明，化合物2和9与PTP1B混合竞争性抑制，而化合物3和6与非竞争性抑制。另外，化合物2，3，6，和9也诱导的2-脱氧-2 - [（7-硝基-2,1,3-苯并恶二唑-4-基）氨基] - d -葡萄糖摄取刺激3T3- L1脂肪细胞的浓度为10和5 µM。两者合计，结果表明虎杖 可能是进一步研发抗糖尿病药物的天然化合物的新来源。