1. In vitro inhibition of rat monoamine oxidase by liquiritigenin and isoliquiritigenin isolated from Sinofranchetia chinensis
- Author
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X, Pan, L D, Kong, Y, Zhang, C H, Cheng, and R X, Tan
- Subjects
Flavonoids ,Chalcone ,Chalcones ,Monoamine Oxidase Inhibitors ,Plants, Medicinal ,Flavanones ,Animals ,Brain ,Monoamine Oxidase ,Drugs, Chinese Herbal ,Mitochondria ,Rats - Abstract
To study the inhibition of liquiritigenin (1) and isoliquiritigenin (2) isolated from Sinofranchetia chinensis on rat monoamine oxidase A and B (MAO A and B).Rat brain mitochondrial fraction, prepared by differential centrifugation, was utilized as a source of MAO activity. MAO activity was determined radiochemically with [14C]5-hydroxytryptamine (5-HT) and [14C]beta-phenylethylamine (beta-PEA) used as MAO A or B specific radiolabled substrates, respectively. The Ki and KI values were obtained from Lineweaver-Burk plot using linear regression analysis.Liquiritigenin and isoliquiritigenin were found to be inhibitory against both MAO A and B in a dose-dependent manner. IC50 (95% of confidence limits) of liquiritigenin and isoliquiritigenin were 32 (26-36) and 13.9 (12.8-15.6) mumol/L for the inhibition of MAO A, and 104.6 (89.0-118.9) and 47.2 (39.5-54.5) mumol/L for that of MAO B, respectively. Lineweaver-Burk transformation of the MAO A inhibition data indicated that the inhibition was non-competitive for both liquiritigenin and isoliquiritigenin whereas their inhibition of MAO B was of mixed type. Regarding MAO A inhibition, the Ki values of liquiritigenin and isoliquiritigenin were 31.5 mumol/L and 14.3 mumol/L, respectively. As to the inhibition of MAO B, the Ki and KI data for liquiritigenin were 164.7 and 15.2 mumol/L, and those for isoliquiritigenin were 62.2 and 9.3 mumol/L, respectively.Liquiritigenin and isoliquiritigen inhibited the activity of MAO A and B in rat brain mitochondria, and the latter was more active than the former.
- Published
- 2001