Abstract
During the screening of a prefractionated natural product extract library (400 biota) against sodium-glucose-linked transporter 2 (SGLT2), a methanol fraction of the traditional Chinese medicine, Sophora flavescens, displayed promising inhibitory activity against SGLT2. Based on the medium-pressure column chromatograph and preparative HPLC, bioassay-guided purification on the large-scale organic extract resulted in the isolation of a new isoflavonoid glycoside, 3-(Benzo[d][1,3]dioxol-5-yl)-7-(((2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)-4H-chromen-4-one (1), together with eight known isoflavonoid glycosides 2–9. Except compound 5, other compounds were isolated from this plant for the first time. All nine compounds exhibited inhibitory activity against SGLT2. Among them, compound 9 showed the strongest SGLT2 inhibitory activity with the IC50 value of 2.6 μM, and compound 1 showed the medium SGLT2 inhibitory activity with the IC50 value of 15.3 μM.
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Acknowledgments
The work was financially supported by Wuhan Youth Chenguang Program of Science and Technology (No. 2013070104010028), National Natural Science Foundation of China Grants (No. 81102798 and No. 31070744), and Technology Foundation for Selected Overseas Chinese Scholar, Ministry of Personnel of China (No. BZY12006).
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Yang, J., Yang, X., Wang, C. et al. Sodium-glucose-linked transporter 2 inhibitors from Sophora flavescens . Med Chem Res 24, 1265–1271 (2015). https://doi.org/10.1007/s00044-014-1200-0
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DOI: https://doi.org/10.1007/s00044-014-1200-0