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首页> 外文期刊>Journal of Medicinal Chemistry >Design of a sialylglycopolymer with a chitosan backbone having efficient inhibitory activity against influenza virus infection
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Design of a sialylglycopolymer with a chitosan backbone having efficient inhibitory activity against influenza virus infection

机译:具有有效抑制流感病毒感染活性的壳聚糖骨架的唾液酸糖基聚合物的设计

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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.
机译:我们在这里验证了由天然产物,壳聚糖和鸡蛋黄制备的唾液酸糖基聚合物对流感病毒感染的抑制活性,并估计了该分子对有效抑制的需求。抑制活性显然取决于两个因素,即壳聚糖骨架的长度(聚合度:DP)和缀合的唾液酸寡糖侧链的量(取代度:DS)。抑制效率随DP值的增加而增加,当DP为1430时获得最高的抑制活性。当相邻的唾液寡糖侧链出现时,DS值增加至15.6%,病毒感染的抑制率达到90%以上。接近4 nm,几乎是血凝素三聚体中两个受体结合口袋之间的距离。这些结果表明,唾液酸糖基聚合物可以是安全有效的抗流感药物的极好的候选者。

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