Yazawa Kurumi, Kurokawa Masahiko, Obuchi Masatsugu, Li Ying, Yamada Rie, Sadanari Hidetaka, Matsubara Keiko, Watanabe Kunitomo, Koketsu Mamoru, Tuchida Yuuzo, Murayama Tsugiya
Department of Microbiology and Immunology, Faculty of Pharmaceutical Sciences, Hokuriku University, Kanazawa, Japan.
Antivir Chem Chemother. 2011 Aug 23;22(1):1-11. doi: 10.3851/IMP1782.
We examined the anti-influenza virus activity of tricin, 4',5,7-trihydroxy-3',5'-dimethoxyflavone, against five viruses: A/Solomon islands/3/2006 (H1N1), A/Hiroshima/52/2005 (H3N2), A/California/07/2009 (H1N1pdm), A/Narita/1/2009 (H1N1pdm) and B/Malaysia/2506/2004 strains in vitro and against A/PR/8/34 virus in vivo.
The effect of tricin was studied by an infectious virus yield reduction assay. The anti-influenza virus mechanism of the tricin was examined by western blot analysis, real-time reverse transcriptase PCR analysis, haemagglutination inhibition (HI) assay and neuraminidase (NA) inhibition assay. The anti-influenza virus efficacy of tricin was further examined in a murine influenza virus infection model.
Tricin of 3.3 to 30 μM significantly reduced seasonal A (H1N1), (H3N2) viruses, novel A (H1N1pdm) virus, as well as B virus in a dose-dependent manner. The 50% effective concentrations of tricin were 3.4 μM for seasonal A (H3N2) virus, 4.9 μM for B virus and 8.2 μM for A/Narita (H1N1pdm) virus. Tricin decreased the expression of haemagglutinin (HA) protein and matrix (M) protein, and messenger RNA expression of HA and M of influenza virus in the infected cells. Tricin exhibited little or no effects on influenza virus HI and NA activities. In the mouse infection model, tricin was significantly effective in reducing body weight loss, and also effective in prolonging survival times of infected mice.
Tricin was indicated to possess anti-influenza virus activity and to ameliorate body weight loss and survival rate of influenza-A-virus-infected mice. Tricin is a novel compound with potential anti-influenza virus activity in vitro and in vivo.
我们检测了小麦黄素(4',5,7-三羟基-3',5'-二甲氧基黄酮)对五种病毒的抗流感病毒活性,这五种病毒分别为:A/所罗门群岛/3/2006(H1N1)、A/广岛/52/2005(H3N2)、A/加利福尼亚/07/2009(H1N1pdm)、A/成田/1/2009(H1N1pdm)和B/马来西亚/2506/2004毒株,检测在体外进行,同时还检测了其对体内A/PR/8/34病毒的作用。
通过感染性病毒产量减少试验研究小麦黄素的作用。通过蛋白质免疫印迹分析、实时逆转录聚合酶链反应分析、血凝抑制(HI)试验和神经氨酸酶(NA)抑制试验检测小麦黄素的抗流感病毒机制。在小鼠流感病毒感染模型中进一步检测小麦黄素的抗流感病毒功效。
3.3至30μM的小麦黄素以剂量依赖方式显著降低季节性A(H1N1)、(H3N2)病毒、新型A(H1N1pdm)病毒以及B病毒。小麦黄素对季节性A(H3N2)病毒的50%有效浓度为3.4μM,对B病毒为4.9μM,对A/成田(H1N1pdm)病毒为8.2μM。小麦黄素降低了感染细胞中血凝素(HA)蛋白和基质(M)蛋白的表达,以及流感病毒HA和M的信使核糖核酸表达。小麦黄素对流感病毒HI和NA活性几乎没有影响。在小鼠感染模型中,小麦黄素在减轻体重减轻方面显著有效,并且在延长感染小鼠的存活时间方面也有效。
表明小麦黄素具有抗流感病毒活性,并能改善甲型流感病毒感染小鼠的体重减轻和存活率。小麦黄素是一种在体外和体内均具有潜在抗流感病毒活性的新型化合物。