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

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• 作者：Myco Umemura ; Masae Itoh ; Yutaka Makimura ; Kohji Yamazaki ; Midori Umekawa ; Ayano Masui ; Yoshiharu Matahira ; Mari Shibata ; Hisashi Ashida ; Kenji Yamamoto
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：August 14, 2008
• 年：2008
• 卷：51
• 期：15
• 页码：4496-4503
• 全文大小：331K
• 年卷期：v.51,no.15(August 14, 2008)
• ISSN：1520-4804

文摘

We verified here the inhibitory activity of a sialylglycopolymer prepared from natural products, chitosan and hen egg yolk, against influenza virus infection and estimated the requirements of the molecule for efficient inhibition. The inhibitory activity clearly depended on two factors, the length (the degree of polymerization: DP) of the chitosan backbone and the amount (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.