Structure-activity relationships of flavonoids as natural inhibitors against E. coli beta-glucuronidase
文献类型：期刊论文
| 作者 | Wu, Da-Chang2; Zou, Li-Wei3; Dou, Tong-Yi4; Yang, Ling3; Zhang, Tong-Yan1; Hou, Jie2; Weng, Zi-Miao2; Wang, Ping3; Ge, Guang-Bo4; Dai, Zi-Ru4 |
| 刊名 | FOOD AND CHEMICAL TOXICOLOGY
 |
| 出版日期 | 2017-11-01 |
| 卷号 | 109页码:975-983 |
| 关键词 | Flavonoids E. Coli bE.a-glucuronidasE. Structure-inhibition Relationships Scutellarein Luteolin |
| ISSN号 | 0278-6915 |
| DOI | 10.1016/j.fct.2017.03.042 |
| 文献子类 | Article |
| 英文摘要 | Bacterial beta-glucuronidases play key roles in the deconjugation of a variety of endogenous and drug glucuronides, thus have been recognized as important targets to modulate the enterohepatic circulation of various glucuronides. In this study, more than 30 natural flavonoids were collected and their inhibitory effects against E. coli beta-glucuronidase (EcGUS) were assayed. The results demonstrated that some flavonoids including scutellarein, luteolin, baicalein, quercetin and scutellarin displayed strong to moderate inhibitory effects against EcGUS, with the IC50 values ranging from 5.76 mu M to 29.64 mu M, while iso-flavones and dihydroflavones displayed weak inhibitory effects against EcGUS. Further investigation on inhibition kinetics revealed that scutellarein and luteolin functioned as potent competitive inhibitors against EcGUS-mediated PNPG hydrolysis, with the K-i values less than 3.0 mu M. Molecular docking simulations demonstrated that scutellarein and luteolin could be well-docked into the catalytic site of EcGUS, while the binding areas of these two natural inhibitors on EcGUS were highly overlapped with that of PNPG on EcGUS. Additionally, the structure-inhibition relationships of natural flavonoids against EcGUS are also summarized, which will be very helpful for the medicinal chemists to design and develop more potent flavonoid-type inhibitors against EcGUS. (C) 2017 Elsevier Ltd. All rights reserved. |
| WOS关键词 | HUMAN UDP-GLUCURONOSYLTRANSFERASES ; HUMAN CARBOXYLESTERASE 2 ; CANCER DRUG TOXICITY ; DIETARY POLYPHENOLS ; INTESTINAL BACTERIA ; METABOLISM ; IRINOTECAN ; ENZYMES ; DISEASE ; LIVER |
| WOS研究方向 | Food Science & Technology ; Toxicology |
| 语种 | 英语 |
| WOS记录号 | WOS:000415911500019 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://cas-ir.dicp.ac.cn/handle/321008/169270]  |
| 专题 | 大连化学物理研究所_中国科学院大连化学物理研究所 |
| 通讯作者 | Zhang, Tong-Yan; Hou, Jie |
| 作者单位 | 1.Zhengzhou Univ Light Ind, Zhengzhou 450001, Henan, Peoples R China 2.Dalian Med Univ, Dalian 116044, Peoples R China 3.Shanghai Univ Tradit Chinese Med, Shanghai 201203, Peoples R China 4.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wu, Da-Chang,Zou, Li-Wei,Dou, Tong-Yi,et al. Structure-activity relationships of flavonoids as natural inhibitors against E. coli beta-glucuronidase[J]. FOOD AND CHEMICAL TOXICOLOGY,2017,109:975-983. |
| APA | Wu, Da-Chang.,Zou, Li-Wei.,Dou, Tong-Yi.,Yang, Ling.,Zhang, Tong-Yan.,...&Dai, Zi-Ru.(2017).Structure-activity relationships of flavonoids as natural inhibitors against E. coli beta-glucuronidase.FOOD AND CHEMICAL TOXICOLOGY,109,975-983. |
| MLA | Wu, Da-Chang,et al."Structure-activity relationships of flavonoids as natural inhibitors against E. coli beta-glucuronidase".FOOD AND CHEMICAL TOXICOLOGY 109(2017):975-983. |
入库方式： OAI收割
来源：大连化学物理研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。