Diarylheptanoid-chalcone hybrids with PTP1B and alpha-glucosidase dual inhibition from Alpinia katsumadai

doi:10.1016/j.bioorg.2021.104683

KIB OpenIR

	Diarylheptanoid-chalcone hybrids with PTP1B and alpha-glucosidase dual inhibition from Alpinia katsumadai
	He,Xiao-Feng ; Chen,Ji-Jun; Li,Tian-Ze ; Hu,Jing ; Zhang,Xue-Mei ; Geng,Chang-An
	2021
Source Publication	BIOORGANIC CHEMISTRY
ISSN	0045-2068
Volume	108 Pages:104683
Abstract	The EtOH extracts of the dried seeds of Alpinia katsumadai were revealed with hypoglycemic effects on db/db mice at the concentration of 200 mg/kg. In order to clarify the antidiabetic constituents, 16 new diarylheptanoidchalcone hybrids, katsumadainols A(1)-A(16) (1-16), together with 13 known analogues (17-29), were isolated from A. katsumadai under the guidance of bioassay. Most of the compounds showed alpha-glucosidase and PTP1B dual inhibition, among which compounds 1-3, 5-7, 11-14, 21-25, and 27 showed PTP1B/TCPTP selective inhibition with IC50 values ranging from 22.0 to 96.7 mu M, which were 2-10 times more active than sodium orthovanadate (IC50, 215.7 mu M). All compounds exhibited obvious inhibition against alpha- glucosidase with IC50 values of 2.9-29.5 mu M, indicating 6-59 times more active than acarbose (IC50, 170.9 mu M). Study of enzyme kinetics indicated compounds 1, 3, and 12 were PTP1B and alpha-glucosidase mixed-type inhibitors with K-i values of 13.1, 12.9, 21.6 mu M, and 4.9, 7.4, 3.4 mu M, respectively.
Keyword	Alpinia katsumadai Katsumadainols A(1)-A(16) PTP1B/TCPTP selective inhibitors alpha-glucosidase inhibitors Antidiabetic effects THEORETICAL CALCULATION ABSOLUTE-CONFIGURATION SEEDS BLEPHAROCALYXINS ADDUCT MOIETY
DOI	10.1016/j.bioorg.2021.104683
WOS ID	WOS:000624555700005
Citation statistics
Document Type	期刊论文
Identifier	http://ir.kib.ac.cn/handle/151853/73678
Collection	中国科学院昆明植物研究所
Affiliation	1.[He, Xiao-Feng 2.Chen, Ji-Jun 3.Li, Tian-Ze 4.Hu, Jing 5.Zhang, Xue-Mei 6.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Yunnan Key Lab Nat Med Chem, Kunming 650201, Yunnan, Peoples R China 7.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
Recommended Citation GB/T 7714	He,Xiao-Feng,Chen,Ji-Jun,Li,Tian-Ze,et al. Diarylheptanoid-chalcone hybrids with PTP1B and alpha-glucosidase dual inhibition from Alpinia katsumadai[J]. BIOORGANIC CHEMISTRY,2021,108:104683.
APA	He,Xiao-Feng,Chen,Ji-Jun,Li,Tian-Ze,Hu,Jing,Zhang,Xue-Mei,&Geng,Chang-An.(2021).Diarylheptanoid-chalcone hybrids with PTP1B and alpha-glucosidase dual inhibition from Alpinia katsumadai.BIOORGANIC CHEMISTRY,108,104683.
MLA	He,Xiao-Feng,et al."Diarylheptanoid-chalcone hybrids with PTP1B and alpha-glucosidase dual inhibition from Alpinia katsumadai".BIOORGANIC CHEMISTRY 108(2021):104683.

Files in This Item:
There are no files associated with this item.

If you have any objections to this item, please fill out the form below and the administrator will contact you as soon as possible.
Content:
Email：	*
Institution:
Verification Code:	Refresh

Any comments and suggestions are welcomed.
Title:	*
Content:
Email：	*
Verification Code:	Refresh

中国科学院昆明植物研究所知识管理系统