Hie Research Of α-Glucosidase Inhibitors From The Fruits Of Terminalia Chebula Retz

α-glucosidase inhibitor was recognized as the first oral hypoglycemic extensively for IIdiabetes mellitus because it could decrease the level of postprandial blood sugar. At present,the most of clinical drugs were synthesized with less in species and difficult development,thus screening better α-glycosidase inhibitors from traditional Chinese medicine (TCM) was apopular pathway to develop natural medicines to reduce blood glucose. In recent years, thetotal crude extract of Terminalia chebula Retz. has been repeatedly proved to have inhibitionagainst α-glycosidase with high activity, and part of inhibitors have been isolated and purified.The activity constituents were isolated and purified by bioactivity-guided with the purpose offurther recognizing activity compounds in this present investigation.A novel screening method of α-glycosidase inhibitors has been established by HPLC invitro. α-glycosidase inhibitor of Terminalia chebula Retz. was isolated and purified bybioactivity-guided. Compounds were isolated and purified through extraction, silica gel,LH-20and C18column chromatography methods. In the process of separation, columnchromatography was guided by TLC and HPLC.The study found that there were many activity inhibitors, and the inhibition rate resultsof components extracted from Terminalia chebula Retz. as follows: ethyl acetate phase>aqueous phase> n-butanol phase, petroleum ether phase was not active. The acetic etherextract was isolated and purified by bioactivity-guided, eight ingredients were get after thefirst time column separation, and by the activity test, under the mass concentration of1.0mg/mL, the inhibition rate more than80%had three components: Yb, Yc, Yh. Compound1and four ingredients (Fr.b1, Fr.b2, Fr.b3, Fr.b4) were obtained after the first time columnseparation of Yb, under1mg/mL, the result of active test as follows: Fr.b1> Fr.b3> Fr.b2>Fr.b4. Fr.b1and Fr.b3were given up because of their low mass. Compound2was isolatedand purified from Fr.b2by silica gel and LH-20column. Compound4and eleven ingredientswere obtained after the first time column separation of Yc, the inhibition rate of Yc washighest under1.0mg/mL. Compound3and compound5were acquired from Yc by silica gel,LH-20and C18column. Using NMR (1H,13C), five compounds were identified respectively as5-hydroxymethylfurfrual (1), arjunic acid (2), arjunolic acid (3), arjungenin (4) and methylgallate (5), among them,5-hydroxymethylfurfrual, arjunic acid, Arjunolic acid and methylgallate had the activity, IC50of them were21.20μmol/mL,2.97μmol/mL,0.82μmol/mL,13.76μmol/mL, separately. The IC50of compounds (2) and (3) were lower than that ofAcarbose (IC50=3.87μmol/mL),5-hydroxymethylfurfrual was isolated for the frist timefrom the seeds of Terminalia chebula Retz..