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Design of a Sialylglycopolymer with a Chitosan Backbone Having Efficient Inhibitory Activity against Influenza Virus Infection.

  作者 Umemura, Myco;Itoh, Masae;Makimura, Yutaka;Yamazaki, Kohji;Umekawa, Midori;Masui, Ayano;Matahira, Yoshiharu;Shibata, Mari;Ashida, Hisashi;Yamamoto, Kenji;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-15;  页码  4496-4503  
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[摘要]We verified here the inhibitory activity of a sialylglycopolymer prepd. from natural products, chitosan and hen egg yolk, against influenza virus infection and estd. the requirements of the mol. for efficient inhibition. The inhibitory activity clearly depended on two factors, the length (the d.p.: DP) of the chitosan backbone and the amt. (the degree of substitution: DS) of conjugated sialyloligosaccharide side chain. The inhibitory efficiency increased in accordance with the DP value, with the highest inhibitory activity obtained when the DP was 1430. The inhibition of virus infection reached more than 90% as the DS value increased up to 15.6% when the neighboring sialyloligosaccharide side chains came as close as 4 nm, which was nearly the distance between two receptor-binding pockets in a hemagglutinin trimer. These results demonstrate that the sialylglycopolymer could be an excellent candidate of the safe and efficient anti-influenza drug.

 
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