Design, synthesis and biological evaluation of water-soluble per-O-methylated cyclodextrin-C60 conjugates as anti-influenza virus agents.

Abstract:

:The most common fullerene member C60 displays many biological applications, such as, anticancer, human immunodeficiency virus and hepatitis C virus inhibitors, O2 uptake inhibitor and vectors for drug and DNA. Nevertheless, the innate hydrophobicity of C60 constrains its further development. We introduced cyclodextrins to enhance the water-solubility of C60. Nine cyclodextrin-C60 conjugates, including seven α-cyclodextrin-C60 conjugates and two γ-cyclodextrin-C60 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-C60 conjugates, which were relatively more water-soluble, exerted higher inhibition with IC50 values of 87.73 μM and 75.06 μM, respectively, than seven α-cyclodextrin-C60 conjugates.

journal_name

Eur J Med Chem

authors

Zhu X,Xiao S,Zhou D,Sollogoub M,Zhang Y

doi

10.1016/j.ejmech.2018.01.040

subject

Has Abstract

pub_date

2018-02-25 00:00:00

pages

194-205

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(18)30053-9

journal_volume

146

pub_type

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