Diarylheptanoid-flavanone Hybrids as Multiple-target Antidiabetic Agents from Alpinia katsumadai

doi:10.1002/cjoc.202100469

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	Diarylheptanoid-flavanone Hybrids as Multiple-target Antidiabetic Agents from Alpinia katsumadai
	He,Xiao-Feng ; Chen,Ji-Jun; Li,Tian-Ze ; Hu,Jing ; Huang,Xiao-Yan ; Zhang,Xue-Mei ; Guo,Yuan-Qiang ; Geng,Chang-An
	2021
发表期刊	CHINESE JOURNAL OF CHEMISTRY
ISSN	1001-604X
卷号	39 期号:11 页码:3051-3063
摘要	Main observation and conclusion The EtOAc fraction of Alpinia katsumadai seeds showed significant inhibition on glycogen phosphorylase a (GPa) with inhibitory ratios of 97.9% and 64.6% at concentrations of 200 and 100 mu g/mL, respectively. Bioactivity-guided isolation afforded 15 new diarylheptanoid-flavanone hybrids, katsumadainols B-1-B-15 (1-15), together with eight known ones (16-23). Compounds 4-10 and 12-21 exhibited activity against GPa with IC50 values of 10.1-95.4 mu mol/L; compounds 4, 5, 16, and 17 displayed inhibitory effects on alpha-glucosidase with IC50 values of 7.1, 12.4, 7.2, and 8.3 mu mol/L, obviously higher than acarbose (IC50, 209.1 mu mol/L); compounds 4-6, 14, 16-20, 22, and 23 were PTP1B/TCPTP selective inhibitors with IC50 values of 40.7-95.8 mu mol/L; compounds 4, 5, 16, and 17 showed DPP4 inhibitory effects with inhibitory ratios of 50.0%-54.2% (200 mu mol/L). Diarylheptanoid-flavanone hybrids (4, 5, 16, and 17) with a p-hydroxybenzyl at C-6 position represent a promising class of multiple-target antidiabetic agents inhibiting GPa, alpha-glucosidase, PTP1B, and DPP4.
关键词	Alpinia katsumadai Katsumadainols B-1-B-15 Natural products Structure elucidation Biological activity TYROSINE-PHOSPHATASE 1B GLYCOGEN-PHOSPHORYLASE ALPHA-GLUCOSIDASE ABSOLUTE-CONFIGURATION STRUCTURE ELUCIDATION DUAL INHIBITION SEEDS CONSTITUENT DERIVATIVES CHALCONE
DOI	10.1002/cjoc.202100469
WOS记录号	WOS:000692937500001
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/73675
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.Li, Tian-Ze 4.Hu, Jing 5.Huang, Xiao-Yan 6.Zhang, Xue-Mei 7.Chinese Acad Sci, Yunnan Key Lab Nat Med Chem, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China 8.Nankai Univ, Coll Pharm, Tianjin 300071, Peoples R China 9.Nankai Univ, Tianjin Key Lab Mol Drug Res, Tianjin 300071, Peoples R China 10.Univ Chinese Acad Sci, Chinang 100049, Peoples R China
推荐引用方式 GB/T 7714	He,Xiao-Feng,Chen,Ji-Jun,Li,Tian-Ze,et al. Diarylheptanoid-flavanone Hybrids as Multiple-target Antidiabetic Agents from Alpinia katsumadai[J]. CHINESE JOURNAL OF CHEMISTRY,2021,39(11):3051-3063.
APA	He,Xiao-Feng.,Chen,Ji-Jun.,Li,Tian-Ze.,Hu,Jing.,Huang,Xiao-Yan.,...&Geng,Chang-An.(2021).Diarylheptanoid-flavanone Hybrids as Multiple-target Antidiabetic Agents from Alpinia katsumadai.CHINESE JOURNAL OF CHEMISTRY,39(11),3051-3063.
MLA	He,Xiao-Feng,et al."Diarylheptanoid-flavanone Hybrids as Multiple-target Antidiabetic Agents from Alpinia katsumadai".CHINESE JOURNAL OF CHEMISTRY 39.11(2021):3051-3063.

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