Caffeic acid phenethyl ester (CAPE), an active component of propolis, inhibits Helicobacter pylori peptide deformylase activity
文献类型：期刊论文
| 作者 | Cui, Kunqiang2; Lu, Weiqiang2; Zhu, Lili2; Shen, Xu1,2 ; Huang, Jin2
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| 刊名 | BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
 |
| 出版日期 | 2013-05-31 |
| 卷号 | 435期号:2页码:289-294 |
| 关键词 | Helicobacter pylori Peptide deformylase Propolis Phenolic compounds Caffeic acid phenethyl ester |
| ISSN号 | 0006-291X |
| DOI | 10.1016/j.bbrc.2013.04.026 |
| 文献子类 | Article |
| 英文摘要 | Helicobacter pylori (H. pylori) is a major causative factor for gastrointestinal illnesses, H. pylori peptide deformylase (HpPDF) catalyzes the removal of formyl group from the N-terminus of nascent polypeptide chains, which is essential for H. pylori survival and is considered as a promising drug target for anti-H. pylori therapy. Propolis, a natural antibiotic from honeybees, is reported to have an inhibitory effect on the growth of H. pylori in vitro. In addition, previous studies suggest that the main active constituents in the propolis are phenolic compounds. Therefore, we evaluated a collection of phenolic compounds derived from propolis for enzyme inhibition against HpPDF. Our study results show that Caffeic acid phenethyl ester (CAPE), one of the main medicinal components of propolis, is a competitive inhibitor against HpPDF, with an IC50 value of 4.02 mu M. Furthermore, absorption spectra and crystal structural characterization revealed that different from most well known PDF inhibitors, CAPE block the substrate entrance, preventing substrate from approaching the active site, but CAPE does not have chelate interaction with HpPDF and does not disrupt the metal-dependent catalysis. Our study provides valuable information for understanding the potential anti-H. pylori mechanism of propolis, and CAPE could be served as a lead compound for further anti-H. pylori drug discovery. Crown Copyright (C) 2013 Published by Elsevier Inc. All rights reserved. |
| WOS关键词 | OCCURRING ANTIBACTERIAL AGENT ; GASTRIC PRECANCEROUS LESIONS ; BRAZILIAN PROPOLIS ; PROTEIN ; CANCER ; ANTIBIOTICS ; EXPRESSION ; FLAVONOIDS ; ACTINONIN ; DISCOVERY |
| 资助项目 | National Natural Science Foundation of China[81102420] ; Innovation Program of Shanghai Municipal Education Commission[10ZZ41] ; Specialized Research Fund for the Doctoral Program of Higher Education of China[20090074120012] ; Shanghai Committee of Science and Technology[11DZ2260600] ; Fundamental Research Funds for the Central Universities[00000000] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Biophysics |
| 语种 | 英语 |
| WOS记录号 | WOS:000320828300021 |
| 出版者 | ACADEMIC PRESS INC ELSEVIER SCIENCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277609]  |
| 专题 | 药理学第三研究室 |
| 通讯作者 | Huang, Jin |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Cui, Kunqiang,Lu, Weiqiang,Zhu, Lili,et al. Caffeic acid phenethyl ester (CAPE), an active component of propolis, inhibits Helicobacter pylori peptide deformylase activity[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2013,435(2):289-294. |
| APA | Cui, Kunqiang,Lu, Weiqiang,Zhu, Lili,Shen, Xu,&Huang, Jin.(2013).Caffeic acid phenethyl ester (CAPE), an active component of propolis, inhibits Helicobacter pylori peptide deformylase activity.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,435(2),289-294. |
| MLA | Cui, Kunqiang,et al."Caffeic acid phenethyl ester (CAPE), an active component of propolis, inhibits Helicobacter pylori peptide deformylase activity".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 435.2(2013):289-294. |
入库方式： OAI收割
来源：上海药物研究所
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