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合成黄酮-3-基酯的抗小核糖核酸病毒活性

Anti-picornavirus activity of synthetic flavon-3-yl esters.

作者信息

Conti C, Mastromarino P, Sgro R, Desideri N

机构信息

Institute of Microbiology, School of Medicine, Rome, Italy.

出版信息

Antivir Chem Chemother. 1998 Nov;9(6):511-5. doi: 10.1177/095632029800900607.

DOI:10.1177/095632029800900607
PMID:9865389
Abstract

The in vitro antiviral activity against picornaviruses (rhinovirus serotype 1B and 14, and poliovirus type 2) of new synthetic 3-hydroxyflavones, 3-acetoxyflavones, and substituted cinnamic and benzoic acid flavon-3-yl esters was evaluated. The maximum non-toxic concentration of compounds was determined in a human cell line (HeLa) suitable for the replication of the three viruses. Their antiviral potency was measured by a plaque reduction assay. Generally, rhinoviruses exhibited a higher sensitivity to the new flavonoids than poliovirus. Flavones, with sterically small substituents in position 3, showed good activity against both rhinoviruses tested. However, the introduction of bulky substituents in the same position resulted in analogues with a higher toxicity and often with a lower efficacy.

摘要

评估了新型合成3-羟基黄酮、3-乙酰氧基黄酮以及取代肉桂酸和苯甲酸黄酮-3-基酯对小核糖核酸病毒(鼻病毒血清型1B和14以及脊髓灰质炎病毒2型)的体外抗病毒活性。在适合这三种病毒复制的人细胞系(HeLa)中测定了化合物的最大无毒浓度。通过蚀斑减少试验测量了它们的抗病毒效力。一般来说,鼻病毒对新型类黄酮的敏感性高于脊髓灰质炎病毒。在3位具有空间位阻小的取代基的黄酮对所测试的两种鼻病毒均表现出良好活性。然而,在同一位置引入庞大的取代基会导致类似物具有更高的毒性,且往往效力更低。

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