| Title | Design, synthesis and biological evaluation of water-soluble per-O-methylated cyclodextrin-C-60 conjugates as anti-influenza virus agents |
| Authors | Zhu, Xiaolei Xiao, Sulong Zhou, Demin Sollogoub, Matthieu Zhang, Yongmin |
| Affiliation | UPMC Univ Paris 06, Sorbonne Univ, CNRS, Inst Parisien Chim Mol,UMR 8232, 4 Pl Jussieu, F-75005 Paris, France. Jianghan Univ, Wuhan Econ & Technol Dev Zone, Inst Interdisciplinary Res, Wuhan 430056, Hubei, Peoples R China. Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100191, Peoples R China. |
| Keywords | Anti-influenza virus Synthesis Cyclodextrin-C-60 conjugates Water-soluble FULLERENE DERIVATIVES ENTRY INHIBITORS C-60 PROTEASE |
| Issue Date | 2018 |
| Publisher | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY |
| Citation | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 2018, 146, 194-205. |
| Abstract | The most common fullerene member C-60 displays many biological applications, such as, anticancer, human immunodeficiency virus and hepatitis C virus inhibitors, O-2 uptake inhibitor and vectors for drug and DNA. Nevertheless, the innate hydrophobicity of C-60 constrains its further development. We introduced cyclodextrins to enhance the water-solubility of C-60. Nine cyclodextrin-C-60 conjugates, including seven alpha-cyclodextrin-C-60 conjugates and two gamma-cyclodextrin-C-60 conjugates, were designed and synthesized. All of these conjugates did not show obvious cytotoxicity. The anti-influenza virus activity of nine conjugates was assessed. Two gamma-cyclodextrin-C-60 conjugates, which were relatively more water-soluble, exerted higher inhibition with IC50 values of 87.73 mu M and 75.06 mu M respectively, than seven tx-cyclodextrin-C-60 conjugates. (C) 2018 Elsevier Masson SAS. All rights reserved. |
| URI | http://hdl.handle.net/20.500.11897/506679 |
| ISSN | 0223-5234 |
| DOI | 10.1016/j.ejmech.2018.01.040 |
| Indexed | SCI(E) PubMed |
| Appears in Collections: | 药学院 天然药物与仿生药物国家重点实验室 |
