Design of a sialylglycopolymer with a chitosan backbone having efficient inhibitory activity against influenza virus infection.
Design of a sialylglycopolymer with a chitosan backbone having efficient inhibitory activity against influenza virus infection.
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DOI：
10.1021/jm8000967
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发表时间：
2008-07
影响因子：
7.3
通讯作者：
Myco Umemura;M. Itoh;Y. Makimura;Kohji Yamazaki;M. Umekawa;Ayano Masui;Y. Matahira;M. Shibata;H. Ashida;Kenji Yamamoto
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文献类型：
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作者：
Myco Umemura;M. Itoh;Y. Makimura;Kohji Yamazaki;M. Umekawa;Ayano Masui;Y. Matahira;M. Shibata;H. Ashida;Kenji Yamamoto
我们验证了由天然产物壳聚糖和蛋黄制备的唾液酸糖共聚物对流感病毒感染的抑制活性，并估计了有效抑制该分子所需的分子。抑制活性明显依赖于壳聚糖骨架的长度(聚合度：DP)和共轭唾液酸寡糖侧链的量(取代度：DS)两个因素。抑制效率随DP值的增加而增加，当DP值为1430时，抑制活性最高。当相邻唾液酸寡糖侧链靠近血凝素三聚体中两个受体结合口袋之间的距离为4 nm时，病毒感染的抑制率可达90%以上，取代度增加到15.6%。这些结果表明，唾液酸糖共聚物可能是一种安全有效的抗流感药物的优秀候选者。
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.