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Bioactive constituents from Salacia obovatilimba as potential in vitro hSGLT2 inhibitors
Zhi-Yong Jiang1, Lin Chen2, Hong-Xi Xie2
1School of Ethnic Medicine, Yunnan University of Chinese Medicine, Kunming, 650500, Yunnan, People's Republic of China; Key Laboratory of Modern Research on Ethnic Medicine in Colleges of Yunnan Province, Kunming, 650500, Yunnan, People's Republic of China.
Abstract:
Sixteen compounds including twelve previously undescribed sesquiterpenes were isolated from Salacia obovatilimba. Based on HRESIMS, IR, NMR and electronic circular dichroism (ECD) spectroscopic analysis, the previously undescribed compounds were characterized as twelve undescribed dihydro-β-agarofuran sesquiterpenoids (compounds 1-12). The structures of compounds 1 and 6 were confirmed by single-crystal X-ray diffraction. All compounds were assayed for their inhibitory effect on hSGLT2 in vitro, results suggested compounds 11 and 13 exhibited significant hSGLT2 inhibitory activity, with IC50 values of 11.9 and 9.45 nM, respectively. The probable binding potency were predicted through molecular docking by accurate models of protein-ligand complex.
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