| Title | Design, synthesis and biological evaluation of gentiopicroside derivatives as potential antiviral inhibitors |
| Authors | Wu, Shaoping Yang, Lili Sun, Wenji Si, Longlong Xiao, Sulong Wang, Qi Dechoux, Luc Thorimbert, Serge Sollogoub, Matthieu Zhou, Demin Zhang, Yongmin |
| Affiliation | Northwest Univ, Biomed Key Lab Shaanxi Prov, Minist Educ, Key Lab Resource Biol & Biotechnol Western China, Xian 710069, Peoples R China. UPMC Univ Paris 06, Sorbonne Univ, Inst Parisien Chim Mol, CNRS UMR 8232, 4 Pl Jussieu, F-75005 Paris, France. Jianghan Univ, Inst Interdisciplinary Res, Wuhan Econ & Technol Dev Zone, Wuhan 430056, Peoples R China. Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China. UPMC Univ Paris 06, Sorbonne Univ, CNRS UMR 8232, 4 Pl Jussieu, F-75005 Paris, France. |
| Keywords | Natural product Secoiridoid Gentiopicroside derivatives Antiviral agents Anti-influenza virus LUTEA SSP-SYMPHYANDRA HCV ENTRY INHIBITORS HEPATITIS-C VIRUS LIVER-INJURY D-MANNOSE MICE SECOIRIDOIDS INFLUENZA CLEAVAGE STANDARD |
| Issue Date | 2017 |
| Publisher | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY |
| Citation | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY.2017,130,308-319. |
| Abstract | Based on classical drug design theory, a novel series of gentiopicroside derivatives was designed and synthesized. All synthesized compounds were then biologically evaluated for their inhibition of influenza virus and anti-HCV activity in vitro. Some of the gentiopicroside derivatives, such as 11a, 13d and 16 showed interesting anti-influenza virus activity with IC50 at 39.5 mu M, 45.2 mu M and 44.0 mu M, respectively. However, no significant anti-HCV activity was found for all of gentiopicroside derivatives. The preliminary results indicate that modification of the sugar moiety on gentiopicroside was helpful for enhancing the anti-influenza activities. Our works demonstrate the importance of secoiridoid natural products as new leads in the development of potential antiviral inhibitors. (c) 2017 Elsevier Masson SAS. All rights reserved. |
| URI | http://hdl.handle.net/20.500.11897/473917 |
| ISSN | 0223-5234 |
| DOI | 10.1016/j.ejmech.2017.02.028 |
| Indexed | SCI(E) |
| Appears in Collections: | 药学院 天然药物与仿生药物国家重点实验室 |
