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
AbstractThe 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.
KeywordAlpinia katsumadai Katsumadainols A(1)-A(16) PTP1B/TCPTP selective inhibitors alpha-glucosidase inhibitors Antidiabetic effects THEORETICAL CALCULATION ABSOLUTE-CONFIGURATION SEEDS BLEPHAROCALYXINS ADDUCT MOIETY
WOS IDWOS:000624555700005
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Document Type期刊论文
Affiliation1.[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
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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.
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