Faculty of Medicine, University of Antwerp (U.I.A.), Universiteits-plein 1, B-2610 Antwerp, Belgium.
Planta Med. 1984 Dec;50(6):513-7. doi: 10.1055/s-2007-969786.
An investigation of the constituents responsible for the pronounced antiviral activity observed for extracts of EUPHORBIA GRANTII Oliv. stems has afforded four related 3-methoxyflavones exhibiting remarkable activities against picornaviruses and vesicular stomatitis virus. All compounds were found to be derivatives of 3-methylquercetin. The concentration of 3-methylquercetin (3-MQ) and 3,3'-dimethyl-quercetin (3,3'-DMQ) inhibiting 90 % of polio type 1 and coxsackie B4 viruses in tissue culture was about 0.01 microg/ml, whereas the 50 % cytotoxic concentration was 40 microg/ml. When administered intraperitoneally, 3-MQ protected mice from viremia and lethal infections from coxsac kie B4 virus at a daily dose of 20 mg/kg for a period of nine days. Biochemical studies on the mechanism of action of 3-MQ or 3,3'-DMQ on poliovirus replication suggested that these 3-methoxyflavones are able to protect the host cells from a viral induced shutdown of the cellular protein synthesis. Preliminary structure activity relationship studies have shown the 3-methoxyfunction of the flavones to be essential for the observed antiviral effects.
对大戟属植物茎提取物中具有显著抗病毒活性的成分进行研究，得到了四种相关的 3-甲氧基黄酮，它们对小核糖核酸病毒和水疱性口炎病毒具有显著的活性。所有化合物均被发现是 3-甲基槲皮素的衍生物。3-甲基槲皮素（3-MQ）和 3,3'-二甲氧基槲皮素（3,3'-DMQ）在组织培养中抑制脊髓灰质炎 1 型和柯萨奇 B4 病毒的浓度约为 0.01μg/ml，而 50%细胞毒性浓度为 40μg/ml。当腹腔内给药时，3-MQ 以每天 20mg/kg 的剂量连续 9 天给药，可保护小鼠免受柯萨奇 B4 病毒的病毒血症和致死性感染。对 3-MQ 或 3,3'-DMQ 对脊髓灰质炎病毒复制作用机制的生化研究表明，这些 3-甲氧基黄酮能够保护宿主细胞免受病毒诱导的细胞蛋白质合成关闭。初步的构效关系研究表明，黄酮类化合物的 3-甲氧基功能对于观察到的抗病毒作用是必不可少的。
