Bioassay-Guided Isolation of Triterpenoids as <i>α</i>-Glucosidase Inhibitors from <i>Cirsium setosum</i>
Xiuting Li,
Xiangjian Zhong,
Xin Wang,
Jinjie Li,
Jiachen Liu,
Kaiqi Wang,
Jianyu Yue,
Ximiao Yang,
Xiaoya Shang,
Sheng Lin
Affiliations
Xiuting Li
Beijing Advanced Innovation Center for Food Nutrition and Human Health, Beijing Technology and Business University, Beijing 100048, China
Xiangjian Zhong
Beijing Key Laboratory of Bioactive Substances and Functional Foods, Beijing Union University, Beijing 100023, China
Xin Wang
Beijing Key Laboratory of Bioactive Substances and Functional Foods, Beijing Union University, Beijing 100023, China
Jinjie Li
Beijing Key Laboratory of Bioactive Substances and Functional Foods, Beijing Union University, Beijing 100023, China
Jiachen Liu
Beijing Key Laboratory of Bioactive Substances and Functional Foods, Beijing Union University, Beijing 100023, China
Kaiqi Wang
Beijing Key Laboratory of Bioactive Substances and Functional Foods, Beijing Union University, Beijing 100023, China
Jianyu Yue
Beijing Key Laboratory of Bioactive Substances and Functional Foods, Beijing Union University, Beijing 100023, China
Ximiao Yang
Beijing Key Laboratory of Bioactive Substances and Functional Foods, Beijing Union University, Beijing 100023, China
Xiaoya Shang
Beijing Key Laboratory of Bioactive Substances and Functional Foods, Beijing Union University, Beijing 100023, China
Sheng Lin
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Cirsium setosum (C. setosum) has a potential antihyperglycemic effect, but it is unclear what bioactive components play a key role. According to the α-glucosidase inhibition activity, three new taraxastane-type triterpenoids of 3β-hydroxy-30-hydroperoxy-20-taraxastene (1), 3β-hydroxy-22α-methoxy-20-taraxastene (2), and 30-nor-3β,22α-dihydroxy-20-taraxastene (3), as well as five known taraxastane triterpenoids of 3β,22-dihydroxy-20-taraxastene (4), 20-taraxastene-3,22-dione (5), 3β-acetoxy-20-taraxasten-22-one (6), 3β-hydroxy-20-taraxasten-22-one (7), and 30-nor-3β-hydroxy-20-taraxastene (8) were obtained from the petroleum ether-soluble portion of the ethanol extract from C. setosum. All chemical structures of the compounds were elucidated by spectroscopic data analysis and compared with literature data. Compounds 4–8 were identified for the first time from this plant, and compounds 1, 2, 4, and 7 exhibited more potent α-glucosidase inhibitory activity—with IC50 values of 18.34 ± 1.27, 26.98 ± 0.89, 17.49 ± 1.42, and 22.67 ± 0.25 μM, respectively—than acarbose did (positive control, IC50 42.52 ± 0.32 μM).
