Diarylheptanoid-chalcone hybrids with PTP1B and alpha-glucosidase dual inhibition from Alpinia katsumadai
文献类型：期刊论文
| 作者 | He,Xiao-Feng; Chen,Ji-Jun ; Li,Tian-Ze; Hu,Jing; Zhang,Xue-Mei; Geng,Chang-An
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| 刊名 | BIOORGANIC CHEMISTRY
 |
| 出版日期 | 2021 |
| 卷号 | 108页码:104683 |
| 关键词 | Alpinia katsumadai Katsumadainols A(1)-A(16) PTP1B/TCPTP selective inhibitors alpha-glucosidase inhibitors Antidiabetic effects THEORETICAL CALCULATION ABSOLUTE-CONFIGURATION SEEDS BLEPHAROCALYXINS ADDUCT MOIETY |
| ISSN号 | 0045-2068 |
| DOI | 10.1016/j.bioorg.2021.104683 |
| 英文摘要 | 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. |
| WOS记录号 | WOS:000624555700005 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/73678]  |
| 专题 | 中国科学院昆明植物研究所 |
| 作者单位 | 1.Li, Tian-Ze 2.Zhang, Xue-Mei 3.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 4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 5.[He, Xiao-Feng 6.Chen, Ji-Jun 7.Hu, Jing |
| 推荐引用方式 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. |
入库方式： OAI收割
来源：昆明植物研究所
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