黄连中木脂素类化合物的分离鉴定及其对蛋白酪氨酸磷酸酶1B的抑制活性Δ

摘要

目的：对黄连中木脂素类化合物进行分离鉴定，并考察其对蛋白酪氨酸磷酸酶1B（PTP1B）的抑制活性。方法：利用高效液相色谱及凝胶柱色谱等技术对黄连95％乙醇提取物的乙酸乙酯部位进行分离，将得到的化合物采用紫外（UV）、红外（IR）、质谱（MS）、核磁共振（NMR）等方法鉴定其化学结构；以RK-682为阳性药物，考察分离的各化合物对PTP1B的抑制活性（阳性药物和分离化合物的浓度均为0、15、30、50、65、80、100、120、140、170、200μmol/L），并计算其抑制率和半数抑制浓度（IC50）。结果：共分离得到5个木脂素类化合物，分别鉴定为9-acetyl lanicepside B、Lanicepside A、Woorenogenin、（+）-isolariciresinol和（+）-lariciresin-ol gluciside（即化合物1～5），其中化合物1、2首次从黄连中分离得到。化合物1～5对PTP1B均有一定抑制作用，且与浓度呈正相关，其IC50分别为57、49、71、58、51μmol/L，但其作用均不及RK-682（IC50为32μmol/L）。结论：从黄连中共分离鉴定出了5个木质素类化合物，且均具有一定的PTP1B抑制活性。%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.