| Kinase Assay: |
| Biol. Pharm. Bull., 2006, 29(2):302-5. | | Glycosidase inhibitory flavonoids from Sophora flavescens.[Pubmed: 16462036] | The methanol extract of Sophora flavescens showed a potent glycosidase inhibitory activity.
METHODS AND RESULTS:
Active components were identified as well-known flavonoid antioxidants: Kushenol A (1), (-)-kurarinone (2), sophoraflavanone G (3), 2'-methoxykurarinone (4), kurarinol (5), 8-prenylkaempferol (6), isoxanthohumol (7), kuraridin (8) and maackian (9). All flavonoids were effective inhibitors of alpha-glucosidase and beta-amylase. Interestingly, lavandulylated flavanones 1-5 had strong alpha-glucosidase inhibitory activities, with IC(50) values of 45 microM, 68 microM, 37 microM, 155 microM and 179 microM, respectively. Kushenol A (1) which does not bear a 4'-hydroxy group showed selective alpha-glucosidase inhibitory activity. Lavandulylated chalcone, kuraridine (8), exhibited IC(50) value of 57 microM against beta-glucosidase, which is the first report of a chalcone displaying glycosidase inhibition.
CONCLUSIONS:
Results showed that 8-lavandulyl group in B-ring was a key factor of the glycosidase inhibitory activities. The inhibition pattern was noncompetitive for alpha-glucosidase, whereas mixed inhibition was observed for beta-amylase. | | Chem. Pharm. Bull., 1986, 34(5):2094-9. | | Inhibition of adenosine 3',5'-cyclic monophosphate phosphodiesterase by components of Sophora flavescens Aiton.[Pubmed: 3017587] | Adenosine 3', 5'-cyclic monophosphate (cAMP) phosphodiesterase inhibitiors contained in the roots of Sophora flavescens AITON were identified as flavonoids, Kushenol A (9), kurarinone (5), and kuraridin (22).
METHODS AND RESULTS:
The structure-inhibitory activity relationships were studied in 30 flavonoids. O-Methylation of a hydroxyl group on an aromatic ring decreased the activity. The prenyl group is important for high inhibitory activity.
CONCLUSIONS:
A kinetic study revealed that nor-kurarinone, kurarinol and kurafidin non-competitively inhibit cAMP phosphodiesterase. |
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