Preparation Of Licorice Chalcone Derivatives And Their Anti-cervical Cancer Activity In Vitro

Objective: To study the high performance preparation technology of licochalcone A from Xinjiang Glycyrrhiza Inflata Bat; to synthesize isoliquiritigenin and its two derivatives of 3-hydroxyl- isoliquiritigenin (butein) and 3-O-methyl- isoliquiritigenin (homobutein); to study the effects of these four target compounds on the proliferation of human cervical cancer cells in vitro. Methods: The total flavonoids were extracted from the root of Glycyrrhiza inflata with chloroform under ultrasonic treatment; the extract was chromatographed on a versamide column to give a fration with the chemical features of chalcone; the fraction was rechromatographed with silica gel columns to furnish pure licochalcone A; isoliquiritigenin and its derivatives were obtained with the aldolization between 2,4-dihydroxyl acetophenone and hydroxyl benzaldehyde; the reaction conditions including ratio of materials, time, temperature and solvent were optimized; the growth inhibitive effects on cell proliferation were evaluated by MTT method. Results: We obtained four chalcone monomers, that is, licochalcone A (yield3.51mg/g), isoliquiritigenin (yield31.77%), 3-hydroxyl- isoliquiritigenin (yield16.51%) and 3-O-methyl- isoliquiritigenin (yield 12.35%) and studied their physical-chemical properties and spectrometrical characteristics; the inhibitive rate of SiHa cells exposed to licochalcone A (50μg/ml) was 90.75%; isoliquiritigenin, 3-hydroxyl- isoliquiritigenin and 3-O-methyl- isoliquiritigenin (5～250μg/ml) inhibited the proliferation of human cervical cancer cells in a concentration-depended manner, and the maximum inhibitive rate was 75.03%, 60.85% and 89.59% respectively. Conclusion: The use of column chromatography is an effective way for high performance preparation of licochalcone A in the laboratory; the use of aldolization is an feasible way for chemical synthesis of isoliquiritigenin derivatives; the prepared target compounds can significantly inhibit the proliferation of human cervical cancer cells in vitro.