URSOLIC ACID DERIVATIVES BEARING 1,2,3-TRIAZOLE MOIETIES AS POTENTIAL PTP1B INHIBITORS
文献类型:期刊论文
作者 | Liu, Zhe1; Bai, Xueqian1; Sheng, Li2; Sun, Liangpeng3; Li, Jia2![]() |
刊名 | CHEMISTRY OF NATURAL COMPOUNDS
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出版日期 | 2023-05-01 |
卷号 | 59期号:3页码:508-511 |
关键词 | ursolic acid PTP1B inhibitors dose-dependently molecular docking |
ISSN号 | 0009-3130 |
DOI | 10.1007/s10600-023-04037-0 |
通讯作者 | Li, Jia(jli@simm.ac.cn) ; Zhang, Tianyi(tianyizhang@126.com) |
英文摘要 | Here, a series of ursolic acid (UA) derivatives were identified as potential PTP1B enzyme inhibitors. All of the tested compounds showed potent PTP1B inhibitory activity (87.79-96.80%) at a concentration of 20 mu g/mL and dose-dependently inhibited PTP1B enzyme with IC50 values ranging from 4.15 +/- 0.01 to 14.10 +/- 0.45 mu M. Compound 11e showed the best PTP1B inhibitory potency, with IC50 values of 4.15 +/- 0.01 mu M, which was slightly lower than that of the positive control. Molecular docking simulation and analysis suggested that compound 11e has a good binding interaction with the active pocket. |
WOS关键词 | TYROSINE-PHOSPHATASE 1B ; INSULIN-RECEPTOR ; OBESITY |
资助项目 | Natural Science Foundation of Jilin Province[YDZJ202201ZYTS277] ; Department of Education of Jilin Province[JJKH20210495KJ] ; Health Department of Jilin Province[2020Z005] |
WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
语种 | 英语 |
WOS记录号 | WOS:001004110600003 |
出版者 | SPRINGER |
源URL | [http://119.78.100.183/handle/2S10ELR8/306403] ![]() |
专题 | 中国科学院上海药物研究所 |
通讯作者 | Li, Jia; Zhang, Tianyi |
作者单位 | 1.Jilin Med Univ, Jilin 132013, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 3.Yanbian Univ, Yanji 133000, Peoples R China |
推荐引用方式 GB/T 7714 | Liu, Zhe,Bai, Xueqian,Sheng, Li,et al. URSOLIC ACID DERIVATIVES BEARING 1,2,3-TRIAZOLE MOIETIES AS POTENTIAL PTP1B INHIBITORS[J]. CHEMISTRY OF NATURAL COMPOUNDS,2023,59(3):508-511. |
APA | Liu, Zhe,Bai, Xueqian,Sheng, Li,Sun, Liangpeng,Li, Jia,&Zhang, Tianyi.(2023).URSOLIC ACID DERIVATIVES BEARING 1,2,3-TRIAZOLE MOIETIES AS POTENTIAL PTP1B INHIBITORS.CHEMISTRY OF NATURAL COMPOUNDS,59(3),508-511. |
MLA | Liu, Zhe,et al."URSOLIC ACID DERIVATIVES BEARING 1,2,3-TRIAZOLE MOIETIES AS POTENTIAL PTP1B INHIBITORS".CHEMISTRY OF NATURAL COMPOUNDS 59.3(2023):508-511. |
入库方式: OAI收割
来源:上海药物研究所
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