The antidiabetic potency of Amomum tsao-ko and its active flavanols, as PTP1B selective and alpha-glucosidase dual inhibitors

doi:10.1016/j.indcrop.2020.112908

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	The antidiabetic potency of Amomum tsao-ko and its active flavanols, as PTP1B selective and alpha-glucosidase dual inhibitors
	He,Xiao-Feng ; Chen,Ji-Jun; Huang,Xiao-Yan ; Hu,Jing ; Zhang,Xu-Ke ; Guo,Yuan-Qiang ; Zhang,Xue-Mei ; Geng,Chang-An
	2021
发表期刊	INDUSTRIAL CROPS AND PRODUCTS
ISSN	0926-6690
卷号	160 页码:112908
摘要	Amomum tsao-ko is an important crop widely cultivated in China, whose dried fruits are popularly consumed as foods and medicines. In this study, the EtOH extract of the fruits of A. tsao-ko was first revealed with PTP1B selective inhibition. Under the guidance of bioassay, eight rare flavanol-menthane conjugates, amomutsaokins A-H (1-8), together with ten known phenolics (9-18), were isolated from A. tsao-ko. Their structures including absolute configurations were elucidated by extensive spectroscopic data (1D and 2D NMR, HRESIMS, IR and UV) and ECD calculations. Their antidiabetic potency against three diabetes-related proteins (PTP1B, TCPTP, and alpha-glucosidase) was evaluated, of which compounds 2, 3, 6, 14, and 16 exhibited PTP1B selective inhibition with IC50 values of 201.45-317.51 mu M, and compounds 1-3, 5-8, 10, and 16-18 displayed alpha-glucosidase inhibitory activity with IC50 values ranging from 3.73 to 76.23 mu M. Compounds 1 and 6 were demonstrated to be alpha-glucosidase mixed-type inhibitors with Ki values of 36.2 and 24.4 mu M, respectively. Molecular docking suggested that compounds 1 and 6 were well located into the active site of alpha-glucosidase by interacting with W1355, W1369, K1460, F1559, H1584, and D1279 residues. This study enlightens the therapeutic potential of A. tsao-ko for the treatment of diabetes, as well as searching for new antidiabetic candidates from natural sources.
关键词	Amomum tsao-ko Amomutsaokins A-H Flavanol-menthane conjugates PTP1B selective inhibitors alpha-Glucosidase inhibitors ANTIOXIDANT ACTIVITY ESSENTIAL OIL CONSTITUENTS TANNINS CREVOST ACID
DOI	10.1016/j.indcrop.2020.112908
WOS记录号	WOS:000613173400006
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/73679
专题	中国科学院昆明植物研究所
作者单位	1.[He, Xiao-Feng 2.Chen, Ji-Jun 3.Huang, Xiao-Yan 4.Hu, Jing 5.Zhang, Xue-Mei 6.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, 132 Lanhei Rd, Kunming 650201, Yunnan, Peoples R China 7.Chinese Acad Sci, Kunming Inst Bot, Yunnan Key Lab Nat Med Chem, Kunming 650201, Yunnan, Peoples R China 8.[Zhang, Xu-Ke 9.Nankai Univ, Coll Pharm, Tianjin 300071, Peoples R China 10.Nankai Univ, Tianjin Key Lab Mol Drug Res, Tianjin 300071, Peoples R China 11.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	He,Xiao-Feng,Chen,Ji-Jun,Huang,Xiao-Yan,et al. The antidiabetic potency of Amomum tsao-ko and its active flavanols, as PTP1B selective and alpha-glucosidase dual inhibitors[J]. INDUSTRIAL CROPS AND PRODUCTS,2021,160:112908.
APA	He,Xiao-Feng.,Chen,Ji-Jun.,Huang,Xiao-Yan.,Hu,Jing.,Zhang,Xu-Ke.,...&Geng,Chang-An.(2021).The antidiabetic potency of Amomum tsao-ko and its active flavanols, as PTP1B selective and alpha-glucosidase dual inhibitors.INDUSTRIAL CROPS AND PRODUCTS,160,112908.
MLA	He,Xiao-Feng,et al."The antidiabetic potency of Amomum tsao-ko and its active flavanols, as PTP1B selective and alpha-glucosidase dual inhibitors".INDUSTRIAL CROPS AND PRODUCTS 160(2021):112908.

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