| In vitro: |
| Planta Med., 2014, 80(7):557-60. | | Protein tyrosine phosphatase 1B inhibitory activity of lavandulyl flavonoids from roots of Sophora flavescens.[Pubmed: 24782228] | Protein tyrosine phosphatase 1B is a non-transmembrane protein tyrosine phosphatase and major negative regulator in insulin signaling cascades, and much attention has been paid to protein tyrosine phosphatase 1B inhibitors as potential therapies for diabetes.
METHODS AND RESULTS:
The screening of a natural compound library led to the discovery of five lavandulyl flavonoids, which were isolated from the roots of Sophora flavescens, as novel PTP1B inhibitors: kuraridin (1), norkurarinone (2), kurarinone (3), 2'-Methoxykurarinone (4), and kushenol T (5). The three most potent compounds, 1, 2, and 4 (IC50 < 30 μM), were demonstrated to be noncompetitive inhibitors of protein tyrosine phosphatase 1B based on a kinetic analysis, and they exhibited different inhibitory selectivities against four homologous protein tyrosine phosphatases (T cell protein tyrosine phosphatase, vaccinia H1-related phosphatase, and Src homology domain 2-containing protein tyrosine phosphatases 1 and 2). | | Natural Medicines, 2003, 57:253-5. | | Trypanocidal Flavonoids from Sophora flavescens[Reference: WebLink] | The acetone extract of Sophora flavescens Aiton (Leguminosae) exhibited lethal activity against Trypanosoma cruzi.
METHODS AND RESULTS:
Column chromatographic separation of the extract guided by trypanocidal activity afforded a new prenylated flavanone (4), together with nine known flavonoids: sophoraflavanone G (1), (-) -kurarinone (2), kushenol L (3), 2'-Methoxykurarinone, (5), 7,4′-dihydroxy-5-methoxy-8-(γ,γ-dimethylallyl)-flavanone (6), leachianone A (7), 8-prenylnaringenin (8), noranhydroicaritin (9) and alopecurone G (10). The structure of the new flavanone 4 was determined on the basis of spectroscopic analyses.
CONCLUSIONS:
The minimum lethal concentrations of these compounds against epimastigotes of T. cruzi were 3.7 μM (1), 14 μM (2), 7.1 μM (3), 7.2 μM (4), 6.9 μM (5), 71 μM (6), 5.5 μM (7), 18 μM (8), 4.4 μM (9) and 3.6 μM (10). |
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