PTP1B inhibitors from stems of Angelica keiskei (Ashitaba)
文献类型：期刊论文
| 作者 | Li, Jin-long2; Gao, Li-xin1; Meng, Fan-wang3; Tang, Chun-lan1; Zhang, Ru-jun2; Li, Jingy-ya1; Luo, Cheng3 ; Li, Jia1; Zhao, Wei-min2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2015-05-15 |
| 卷号 | 25期号:10页码:2028-2032 |
| 关键词 | Angelica keiskei Chalcone PTP1B inhibition Molecular docking |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2015.04.003 |
| 文献子类 | Article |
| 英文摘要 | Three new chalcones, xanthoangelols K-M (1-3), together with 19 known compounds were isolated from the stems of Angelica keiskei Koidzumi, a well-known rejuvenated and anti-diabetic plant originated from Japan. The structures of compounds 1-3 were elucidated on the basis of spectroscopic data and Mosher's method. All compounds were evaluated for their inhibitory activity against protein tyrosine phosphatase 1B (PTP1B). Among them, six chalcones, xanthoangelol K (1), xanthoangelol (4), xanthoangelol F (5), 4-hydroxyderricin (6), xanthoangelol D (7), xanthoangelol E (8), and a coumarin, methoxsalen (17), showed strong PTP1B inhibitory effect with IC50 values of 0.82, 1.97, 1.67, 2.47, 3.97, 1.43, and 2.53 mu g/mL, respectively. A kinetic study revealed that compound 1 inhibited PTP1B with characteristics typical of a competitive inhibitor. Molecular docking simulations elucidated that ring B of 1 may anchor in a pocket of PTP1B and the molecule is stabilized by hydrogen bonds with Arg47, Asp48, and pi-pi interaction with Phe182 of PTP1B. (C) 2015 Elsevier Ltd. All rights reserved. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; CHEMICAL-COMPONENTS ; CHALCONES ; RATS ; 4-HYDROXYDERRICIN ; XANTHOANGELOL ; FOOD |
| 资助项目 | National Science and Technology Major Projects for Major New Drugs Innovation and Development[2013ZX09507002] ; National Natural Science Foundation of China[81125023] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000353526300002 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276526]  |
| 专题 | 药物发现与设计中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 天然药物化学研究室 国家新药筛选中心 |
| 通讯作者 | Luo, Cheng |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Nat Prod Chem, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Jin-long,Gao, Li-xin,Meng, Fan-wang,et al. PTP1B inhibitors from stems of Angelica keiskei (Ashitaba)[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2015,25(10):2028-2032. |
| APA | Li, Jin-long.,Gao, Li-xin.,Meng, Fan-wang.,Tang, Chun-lan.,Zhang, Ru-jun.,...&Zhao, Wei-min.(2015).PTP1B inhibitors from stems of Angelica keiskei (Ashitaba).BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,25(10),2028-2032. |
| MLA | Li, Jin-long,et al."PTP1B inhibitors from stems of Angelica keiskei (Ashitaba)".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 25.10(2015):2028-2032. |
入库方式： OAI收割
来源：上海药物研究所
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