Embelin Restores Carbapenem Efficacy against NDM-1-Positive Pathogens
文献类型：期刊论文
| 作者 | Ning, Nian-Zhi2; Liu, Xiong2; Chen, Fanghong2; Zhou, Peng1,3; Hu, Lihong4; Huang, Jian1,3; Li, Zhan2; Huang, Jie2; Li, Tao2; Wang, Hui2 |
| 刊名 | FRONTIERS IN MICROBIOLOGY
 |
| 出版日期 | 2018-01-25 |
| 卷号 | 9 |
| 关键词 | embelin carbapenem NDM-1 carbapenemase inhibitor |
| ISSN号 | 1664-302X |
| DOI | 10.3389/fmicb.2018.00071 |
| 文献子类 | Article |
| 英文摘要 | The emergence and spread of carbapenemase in Gram-negative pathogens poses an enormous threat to global public health. New Delhi metallo-beta-lactamase-1 (NDM-1) inactivates nearly every class of beta-lactam antibiotics, including carbapenem; however, there is no clinically useful NDM-1 inhibitor. Embelin, an important ingredient in traditional herbal medicine, has anti-tumor effects. The current study is the first to discover and examine the inhibitory activity of embelin against beta-lactamase NDM-1. The IC50 of embelin was 2.1 +/- 0.2 mu M when tested against NDM-1 carbapenemase. Most regions of the embelin molecule were buried within NDM-1's active site, and the hydroxyl group of embelin interacted directly with the metal ion Zn2+ as shown by molecular dynamic simulation. Systematic analysis of the antibacterial activities of embelin and antibiotics demonstrated that embelin restored meropenem activity against a panel of NDM-positive pathogens, such as Escherichia coli, Klebsiella pneumoniae, and Acinetobacter baumannii. Based on these results, embelin could be a promising carbapenem adjuvant candidate against NDM-1-producing bacterial strains. |
| WOS关键词 | METALLO-BETA-LACTAMASE ; ANTIBIOTIC-RESISTANCE ; LIGAND INTERACTIONS ; GLOBAL SPREAD ; PROTEIN ; INHIBITORS ; ENTEROBACTERIACEAE ; DISCOVERY ; MEDICINE ; DOCKING |
| 资助项目 | National Key Basic Research Program (973) of China[2015CB554202] ; National Natural Science Foundation of China[81401643] ; State Key Research Development Program of China[2016YFC1200301] ; State Key Laboratory of Pathogen and BioSecurity Program[SKLPBS1506] ; State Key Laboratory of Pathogen and BioSecurity Program[SKLPBS1530] ; State Key Laboratory of Pathogen and BioSecurity Program[SKLPBS1424] ; Beijing Nova Program[XX2018043] |
| WOS研究方向 | Microbiology |
| 语种 | 英语 |
| WOS记录号 | WOS:000423364900001 |
| 出版者 | FRONTIERS MEDIA SA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279946]  |
| 专题 | 上海中药现代化研究中心 |
| 通讯作者 | Li, Tao; Wang, Hui |
| 作者单位 | 1.Univ Elect Sci & Technol China, Ctr Informat Biomed, Chengdu, Sichuan, Peoples R China; 2.Beijing Inst Microbiol & Epidemiol, State Key Lab Pathogens & Biosecur, Beijing, Peoples R China; 3.Univ Elect Sci & Technol China, Minist Educ, Key Lab NeuroInformat, Chengdu, Sichuan, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ning, Nian-Zhi,Liu, Xiong,Chen, Fanghong,et al. Embelin Restores Carbapenem Efficacy against NDM-1-Positive Pathogens[J]. FRONTIERS IN MICROBIOLOGY,2018,9. |
| APA | Ning, Nian-Zhi.,Liu, Xiong.,Chen, Fanghong.,Zhou, Peng.,Hu, Lihong.,...&Wang, Hui.(2018).Embelin Restores Carbapenem Efficacy against NDM-1-Positive Pathogens.FRONTIERS IN MICROBIOLOGY,9. |
| MLA | Ning, Nian-Zhi,et al."Embelin Restores Carbapenem Efficacy against NDM-1-Positive Pathogens".FRONTIERS IN MICROBIOLOGY 9(2018). |
入库方式： OAI收割
来源：上海药物研究所
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