D-Alanine: D-alanine ligase as a new target for the flavonoids quercetin and apigenin
文献类型：期刊论文
| 作者 | Wu, Dalei; Kong, Yunhua; Chen, Cong Han Jing; Hu, Lihong; Jiang, Hualiang ; Shen, Xu
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| 刊名 | INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS
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| 出版日期 | 2008-11 |
| 卷号 | 32期号:5页码:421-426 |
| 关键词 | Flavonoids Quercetin Apigenin D-Alanine:D-alanine ligase D-Cycloserine MIC |
| ISSN号 | 0924-8579 |
| DOI | 10.1016/j.ijantimicag.2008.06.010 |
| 文献子类 | Article |
| 英文摘要 | Flavonoids are polyphenolic compounds that are ubiquitous in nature. They possess varied promising properties for medical use. Quercetin (3,3',4',5,7-pentahydroxyflavone) and apigenin (4',5,7-trihydroxyflavone) are two representative flavonoids, both of which have been reported to possess antibacterial activity by acting on multiple targets. Here, we determined that D-alanine: D-alanine ligase (Ddl) is another new target for quercetin and apigenin. Kinetic analysis indicated that these two flavonoids function as reversible inhibitors that are competitive with the substrate ATP of Ddl, whereas they are non-competitive with the other substrate D-Ala. The fact that quercetin showed lower 50% inhibitory concentration (IC50) and inhibitor binding constant (K-i) values than apigenin against both the Helicobacter pylori Ddl and the Escherichia coli DdlB implies that the two additional hydroxyls on the flavone skeleton of quercetin in structure might facilitate its inhibitory activity and binding affinity to Ddl. This work is expected to help shed more light on the potential antibacterial mechanism of flavonoids. (C) 2008 Elsevier B. V. and the International Society of Chemotherapy. All rights reserved. |
| WOS关键词 | ALANYL-D-ALANINE ; HELICOBACTER-PYLORI ; D-CYCLOSERINE ; DNA GYRASE ; INHIBITION ; ENZYMES ; BIOSYNTHESIS ; MECHANISMS ; FABZ |
| 资助项目 | State Key Program of Basic Research of China[2004CB518905] ; State Key Program of Basic Research of China[2006AA09Z447] ; State Key Program of Basic Research of China[2007CB914304] ; National Natural Science Foundation of China[30525024] ; National Natural Science Foundation of China[90713046] ; National Natural Science Foundation of China[20721003] ; Shanghai Science and Technology Commission[06JC14080] ; Shanghai Science and Technology Commission[03DZ19228] ; CAS Foundation[KSCX1-YW-R-18] |
| WOS研究方向 | Infectious Diseases ; Microbiology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000261995800011 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279453]  |
| 专题 | 上海中药现代化研究中心 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 药理学第三研究室 |
| 通讯作者 | Hu, Lihong |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wu, Dalei,Kong, Yunhua,Chen, Cong Han Jing,et al. D-Alanine: D-alanine ligase as a new target for the flavonoids quercetin and apigenin[J]. INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS,2008,32(5):421-426. |
| APA | Wu, Dalei,Kong, Yunhua,Chen, Cong Han Jing,Hu, Lihong,Jiang, Hualiang,&Shen, Xu.(2008).D-Alanine: D-alanine ligase as a new target for the flavonoids quercetin and apigenin.INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS,32(5),421-426. |
| MLA | Wu, Dalei,et al."D-Alanine: D-alanine ligase as a new target for the flavonoids quercetin and apigenin".INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS 32.5(2008):421-426. |
入库方式： OAI收割
来源：上海药物研究所
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