OBJECTIVE: To isolate and identify lignans chemical constituents from Coptis chinensis, and to investigate their inhibitory activities to protein tyrosine phosphatase-1B (PTP1B). METHODS: The acetic ether part of 95% ethanol extract from C. chinensis was isolated by HPLC and gel column chromatography, and the structure of chemical constituents were identified by UV, IR, MS and NMR. Using RK-682 as positive drug, the inhibitory activity to PTP1B was investigated (the concentrations of positive drug and isolated chemical constituents were 0, 15, 30, 50, 65, 80, 100, 120, 140, 170 and 200 μmol/L, respectively). Inhibitory rate and IC50 of them were calculated. RESULTS: 5 lignans were isolated, including 9-acetyl lanicepside B, Lanicepside A, Woorenogenin, (+)-isolariciresinol and (+)-lariciresinol gluciside (compound 1-5), and compound 1 and 2 were isolated from C. chinensis for the first time. Compound 1-5 inhibited PTP1B to certain extent in concentration-dependent manner. IC50 of them were 57, 49, 71, 58 and 51 μmol/L, but their effects were not as good as RK-682 (IC50=32 μmol/L). CONCLUSIONS: 5 lignans have been isolated from C. chinensis and can inhibit PTP1B to certain extent.