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| 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
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| 2021 | |
| Source Publication | BIOORGANIC CHEMISTRY
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| ISSN | 0045-2068 |
| Volume | 108Pages: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. |
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| 082-F04-016-2021-何小凤（2223KB） | 期刊论文 | 出版稿 | 开放获取 | CC BY-NC-SA | View Download | |
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