Isolation and Identification of Lignans Chemical Constituents from Coptis chinensis and Their Inhibitory Activity to Protein Tyrosine Phosphatase-1B / 中国药房

ABSTRACT

OBJECTIVE:To isolate and identify lignans chemical constituents from Coptis chinensis,and to investigate their in-hibitory 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 posi-tive drug and isolated chemical constituents were 0,15,30,50,65,80,100,120,140,170 and 200 μmol/L,respectively). In-hibitory 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 lig-nans have been isolated from C. chinensis and can inhibit PTP1B to certain extent.