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| Synthesis and alpha-Glucosidase Inhibitory Mechanisms of Bis(2,3-dibromo-4,5-dihydroxybenzyl) Ether, a Potential Marine Bromophenol alpha-Glucosidase Inhibitor | |
| Liu, Ming1; Zhang, Wei2; Wei, Jianteng1; Lin, Xiukun1 | |
| 2011-09-01 | |
| 发表期刊 | MARINE DRUGS
 |
| ISSN | 1660-3397 |
| 卷号 | 9期号:9页码:1554-1565 |
| 文章类型 | Article |
| 摘要 | Bis(2,3-dibromo-4,5-dihydroxybenzyl) ether (BDDE), derived from the marine algae, is a potential alpha-glucosidase inhibitor for type 2 diabetes treatment. In the present study, a synthetic route was established as a valid approach to obtain BDDE. Fluorescence spectra, circular dichroism spectra and molecular docking methods were employed to elucidate the inhibitory mechanisms of BDDE against alpha-glucosidase. The results showed that BDDE could be prepared effectively and efficiently with the established synthetic methods. Synthetic BDDE bound with alpha-glucosidase and induced minor conformational changes of the enzyme. The docking results indicated the interaction between BDDE and alpha-glucosidase was driven by both hydrophobic forces and hydrogen bonds. The docked BDDE molecule was completely buried in the alpha-glucosidase binding pocket with part of the molecule reaching the catalytic center and overlapping with the position of glucose, and the rest of the molecule extending towards protein surface. This study provides useful information for the understanding of the BDDE-alpha-glucosidase interaction and for the development of novel alpha-glucosidase inhibitors.; Bis(2,3-dibromo-4,5-dihydroxybenzyl) ether (BDDE), derived from the marine algae, is a potential alpha-glucosidase inhibitor for type 2 diabetes treatment. In the present study, a synthetic route was established as a valid approach to obtain BDDE. Fluorescence spectra, circular dichroism spectra and molecular docking methods were employed to elucidate the inhibitory mechanisms of BDDE against alpha-glucosidase. The results showed that BDDE could be prepared effectively and efficiently with the established synthetic methods. Synthetic BDDE bound with alpha-glucosidase and induced minor conformational changes of the enzyme. The docking results indicated the interaction between BDDE and alpha-glucosidase was driven by both hydrophobic forces and hydrogen bonds. The docked BDDE molecule was completely buried in the alpha-glucosidase binding pocket with part of the molecule reaching the catalytic center and overlapping with the position of glucose, and the rest of the molecule extending towards protein surface. This study provides useful information for the understanding of the BDDE-alpha-glucosidase interaction and for the development of novel alpha-glucosidase inhibitors. |
| 关键词 | Bromophenol Alpha-glucosidase Inhibitor Bis(2 3-dibromo-4 5-dihydroxybenzyl) Ether |
| 学科领域 | Pharmacology & Pharmacy |
| DOI | 10.3390/md9091554 |
| URL | 查看原文 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000298927500009 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.qdio.ac.cn/handle/337002/11953 |
| 专题 | 实验海洋生物学重点实验室 |
| 作者单位 | 1.Chinese Acad Sci, Inst Oceanol, Qingdao 266071, Peoples R China 2.So Res Inst, Birmingham, AL 35205 USA |
| 第一作者单位 | 中国科学院海洋研究所 |
| 推荐引用方式 GB/T 7714 | Liu, Ming,Zhang, Wei,Wei, Jianteng,et al. Synthesis and alpha-Glucosidase Inhibitory Mechanisms of Bis(2,3-dibromo-4,5-dihydroxybenzyl) Ether, a Potential Marine Bromophenol alpha-Glucosidase Inhibitor[J]. MARINE DRUGS,2011,9(9):1554-1565. |
| APA | Liu, Ming,Zhang, Wei,Wei, Jianteng,&Lin, Xiukun.(2011).Synthesis and alpha-Glucosidase Inhibitory Mechanisms of Bis(2,3-dibromo-4,5-dihydroxybenzyl) Ether, a Potential Marine Bromophenol alpha-Glucosidase Inhibitor.MARINE DRUGS,9(9),1554-1565. |
| MLA | Liu, Ming,et al."Synthesis and alpha-Glucosidase Inhibitory Mechanisms of Bis(2,3-dibromo-4,5-dihydroxybenzyl) Ether, a Potential Marine Bromophenol alpha-Glucosidase Inhibitor".MARINE DRUGS 9.9(2011):1554-1565. |
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