tetano
Editor, Senior Moderator
Eur J Med Chem. 2018 Feb 1;146:194-205. doi: 10.1016/j.ejmech.2018.01.040. [Epub ahead of print]
[h=1]Design, synthesis and biological evaluation of water-soluble per-O-methylated cyclodextrin-C60 conjugates as anti-influenza virus agents.[/h] Zhu X[SUP]1[/SUP], Xiao S[SUP]2[/SUP], Zhou D[SUP]2[/SUP], Sollogoub M[SUP]1[/SUP], Zhang Y[SUP]3[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] The most common fullerene member C[SUB]60[/SUB] displays many biological applications, such as, anticancer, human immunodeficiency virus and hepatitis C virus inhibitors, O[SUB]2[/SUB] uptake inhibitor and vectors for drug and DNA. Nevertheless, the innate hydrophobicity of C[SUB]60[/SUB] constrains its further development. We introduced cyclodextrins to enhance the water-solubility of C[SUB]60[/SUB]. Nine cyclodextrin-C[SUB]60[/SUB] conjugates, including seven α-cyclodextrin-C[SUB]60[/SUB] conjugates and two γ-cyclodextrin-C[SUB]60[/SUB] 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 γ-cyclodextrin-C[SUB]60[/SUB] conjugates, which were relatively more water-soluble, exerted higher inhibition with IC[SUB]50[/SUB] values of 87.73 μM and 75.06 μM, respectively, than seven α-cyclodextrin-C[SUB]60[/SUB] conjugates.
[h=4]KEYWORDS:[/h] Anti-influenza virus; Cyclodextrin-C(60) conjugates; Synthesis; Water-soluble
PMID: 29407950 DOI: 10.1016/j.ejmech.2018.01.040
[h=1]Design, synthesis and biological evaluation of water-soluble per-O-methylated cyclodextrin-C60 conjugates as anti-influenza virus agents.[/h] Zhu X[SUP]1[/SUP], Xiao S[SUP]2[/SUP], Zhou D[SUP]2[/SUP], Sollogoub M[SUP]1[/SUP], Zhang Y[SUP]3[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] The most common fullerene member C[SUB]60[/SUB] displays many biological applications, such as, anticancer, human immunodeficiency virus and hepatitis C virus inhibitors, O[SUB]2[/SUB] uptake inhibitor and vectors for drug and DNA. Nevertheless, the innate hydrophobicity of C[SUB]60[/SUB] constrains its further development. We introduced cyclodextrins to enhance the water-solubility of C[SUB]60[/SUB]. Nine cyclodextrin-C[SUB]60[/SUB] conjugates, including seven α-cyclodextrin-C[SUB]60[/SUB] conjugates and two γ-cyclodextrin-C[SUB]60[/SUB] 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 γ-cyclodextrin-C[SUB]60[/SUB] conjugates, which were relatively more water-soluble, exerted higher inhibition with IC[SUB]50[/SUB] values of 87.73 μM and 75.06 μM, respectively, than seven α-cyclodextrin-C[SUB]60[/SUB] conjugates.
[h=4]KEYWORDS:[/h] Anti-influenza virus; Cyclodextrin-C(60) conjugates; Synthesis; Water-soluble
PMID: 29407950 DOI: 10.1016/j.ejmech.2018.01.040