| Synthesis and structure-activity relationship studies of water-soluble beta-cyclodextrin-glycyrrhetinic acid conjugates as potential anti-influenza virus agents | |
| Liang, Shuobin1; Li, Man1; Yu, Xiaojuan1; Jin, Hongwei1; Zhang, Yongmin3; Zhang, Lihe1; Zhou, Demin1; Xiao, Sulong1,2 | |
| 通讯作者 | Xiao, Sulong(slxiao@bjmu.edu.cn) |
| 2019-03-15 | |
| 发表期刊 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| ISSN | 0223-5234 |
| 卷号 | 166页码:328-338 |
| 摘要 | Glycyrrhetinic acid (GA) is a major constituent of the herb Glycyrrhiza glabra, and many of its derivatives demonstrate a broad spectrum of antiviral activities. In the current study,18 water-soluble beta-cyclodextrin (CD)-GA conjugates, in which GA was covalently coupled to the primary face of beta-CD using 1,2,3-triazole moiety along with varying lengths of linker, were synthesized via copper-catalyzed azide-alkyl cyclo-addition reaction. Benefited from the attached beta-CD moiety, all these conjugates showed lower hydro-phobicity (AlogP) compared with their parent compound GA. With the exception of per-O-methylated beta-CD-GA conjugate (35), all other conjugates showed no significant cytotoxicity to MDCK cells, and these conjugates were then screened against A/WSN/33 (H1N1) virus using the cytopathic effect assay. The preliminary results indicated that six conjugates showed promising antiviral activity, and the C-3 and C-30 of GA could tolerate some modifications. Our findings suggested that GA could be used as a lead compound for the development of potential anti-influenza virus agents. (C) 2019 Elsevier Masson SAS. All rights reserved. |
| 关键词 | Glycyrrhetinic acid Cyclodextrin Click reaction Influenza virus Inhibitors |
| DOI | 10.1016/j.ejmech.2019.01.074 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000461402400029 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/64991 |
| 专题 | 植物化学与西部植物资源持续利用国家重点实验室 |
| 通讯作者 | Xiao, Sulong |
| 作者单位 | 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China 2.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources West Ch, Kunming Inst Bot, Kunming 650201, Yunnan, Peoples R China 3.Sorbonne Univ, Inst Parisien Chim Mol, CNRS UMR 8232, 4 Pl Jussieu, F-75005 Paris, France |
| 推荐引用方式 GB/T 7714 | Liang, Shuobin,Li, Man,Yu, Xiaojuan,et al. Synthesis and structure-activity relationship studies of water-soluble beta-cyclodextrin-glycyrrhetinic acid conjugates as potential anti-influenza virus agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2019,166:328-338. |
| APA | Liang, Shuobin.,Li, Man.,Yu, Xiaojuan.,Jin, Hongwei.,Zhang, Yongmin.,...&Xiao, Sulong.(2019).Synthesis and structure-activity relationship studies of water-soluble beta-cyclodextrin-glycyrrhetinic acid conjugates as potential anti-influenza virus agents.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,166,328-338. |
| MLA | Liang, Shuobin,et al."Synthesis and structure-activity relationship studies of water-soluble beta-cyclodextrin-glycyrrhetinic acid conjugates as potential anti-influenza virus agents".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 166(2019):328-338. |
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