Synthesis and antibacterial activity of C-2 or C-5 modified and D ring rejiggered canthin-6-one analogues
文献类型：期刊论文
| 作者 | Dai, Jiangkun1; Dan, Wenjia1; Li, Nian1; Wang, Ruixue1; Zhang, Yao1; Li, Nannan1; Wang, Ruizhi1; Wang, Junru1,2 |
| 刊名 | FOOD CHEMISTRY
 |
| 出版日期 | 2018-07-01 |
| 卷号 | 253页码:211-220 |
| 关键词 | Synthesis Canthin-6-one analogues Antibacterial Structure-activity relationships Cell membrane DNA topoisomerases |
| ISSN号 | 0308-8146 |
| DOI | 10.1016/j.foodchem.2018.01.166 |
| 文献子类 | Article |
| 英文摘要 | Thirty-one canthin-6-one analogues, mainly including C-2 or C-5 or D ring modified canthin-6-ones, were designed and synthesized in order to study their antibacterial activity and structure-activity relationships. The analogue 28 with the highest bioactivity had a peak minimum inhibitory concentration of 4 mu g/ml and showed low cytotoxicity against L02 cells and good "drug-like" properties. The antibacterial effect of 28 was characterized further by scanning electron microscopy, cytoplasmic beta-galactosidase leakage assay, molecular docking evaluation, UV-visible analysis and isothermal titration calorimetry (ITC) measurement. The results showed that 28 may exert its bactericidal effect by damaging bacterial cell membranes and disrupting the function of DNA topoisomerases, both of which could lead to rapid cell death. |
| WOS关键词 | BIOLOGICAL EVALUATION ; BETA-CARBOLINE ; DNA-BINDING ; POTENTIAL ANTICANCER ; DESIGN ; AGENTS ; ALKALOIDS ; COMPLEXATION ; COMBINATION ; INHIBITORS |
| 资助项目 | National Natural Science Foundation of China[31270388] ; National Natural Science Foundation of China[81773603] ; Open Foundation of Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education (Northwest University, China)[00000000] ; State Key Laboratory of Drug Research[SIMM1705KF-09] ; Northwest AF University[201610712088] ; Northwest AF University[S201710712026] |
| WOS研究方向 | Chemistry ; Food Science & Technology ; Nutrition & Dietetics |
| 语种 | 英语 |
| WOS记录号 | WOS:000426649300028 |
| 出版者 | ELSEVIER SCI LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279694]  |
| 专题 | 新药研究国家重点实验室 中科院受体结构与功能重点实验室 |
| 通讯作者 | Wang, Junru |
| 作者单位 | 1.Northwest A&F Univ, Coll Chem & Pharm, Shaanxi Key Lab Nat Prod & Chem Biol, 22 Xinong Rd, Yangling 712100, Shaanxi, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Chong Zhi Rd,Zhangjiang Hi Tech Pk, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Dai, Jiangkun,Dan, Wenjia,Li, Nian,et al. Synthesis and antibacterial activity of C-2 or C-5 modified and D ring rejiggered canthin-6-one analogues[J]. FOOD CHEMISTRY,2018,253:211-220. |
| APA | Dai, Jiangkun.,Dan, Wenjia.,Li, Nian.,Wang, Ruixue.,Zhang, Yao.,...&Wang, Junru.(2018).Synthesis and antibacterial activity of C-2 or C-5 modified and D ring rejiggered canthin-6-one analogues.FOOD CHEMISTRY,253,211-220. |
| MLA | Dai, Jiangkun,et al."Synthesis and antibacterial activity of C-2 or C-5 modified and D ring rejiggered canthin-6-one analogues".FOOD CHEMISTRY 253(2018):211-220. |
入库方式： OAI收割
来源：上海药物研究所
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