Anti-influenza virus activities of flavonoids from the medicinal plant Elsholtzia rugulosa

Anti-influenza virus activities of flavonoids from the medicinal plant Elsholtzia rugulosa
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DOI:
10.1055/s-2008-1074558
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发表时间:
2008-06-01
期刊:
影响因子:
2.7
通讯作者:
Du, Guan-Hua
Du, Guan-Hua
中科院分区:
医学3区
文献类型:
--
作者:
Liu, Ai-Lin;Liu, Bo;Du, Guan-Hua

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野香薷(Elsholtzia rugulosa)为唇形科(Lamiaceae)植物,是一种常用的中草药,广泛用于治疗感冒、发热。为阐明该植物抗流感病毒的作用机制及有效成分,建立了流感病毒神经氨酸酶(NA)活性测定法和体外抗流感病毒活性测定法,并以NA活性为指标指导活性成分的分离。最终分离得到5个活性成分,分别为芹菜素(1)、木犀草素(2)、芹菜素(3)、木犀草素(4)和木犀草素3 '-葡萄糖醛酸甲酯(5)。它们都属于黄酮类化合物。体外抗病毒活性测定采用细胞病变效应(CPE)还原法,结果表明它们均具有抗流感病毒活性。其中芹菜素和木犀草素对H3 N2流感病毒的抑制活性最高,其IC 50值分别为1.43 μ g/mL和2.06 μ g/mL。本文对不同化学结构的黄酮类化合物的构效关系及其抗流感病毒活性进行了研究。
Elsholtzia rugulosa (Lamiaceae), a common Chinese herb, is widely used in the treatment of cold and fever. In order to elucidate the action mechanism and the active principles from the plant against anti-influenza virus, the influenza virus neuraminidase (NA) activity assay and in vitro antiviral activity assay were established, and the isolation of the active principles was guided by NA activity. Finally, 5 active constituents were obtained, namely apigenin (1), luteolin (2), apiin (3), galuteolin (4) and luteolin 3'-glucuronyl acid methyl ester (5), respectively. They all belong to the flavonoids. The in vitro antiviral assay using a cytopathic effect (CPE) reduction method showed that they all possessed anti-influenza virus activity. Among them, apigenin and luteolin exhibited the highest activities against influenza virus (H3N2) with IC50 values of 1.43 mu g/mL and 2.06 mu g/mL, respectively. The structure-activity relationship (SAR) of these flavonoids with different chemical structures and their anti-influenza virus activities was addressed in this study.