Romero Marta R, Serrano Maria A, Efferth Thomas, Alvarez Marcelino, Marin Jose J
Laboratory of Experimental Hepatology and Drug Targeting (HEVEFARM), University of Salamanca, Salamanca, Spain.
Planta Med. 2007 Jun;73(6):552-8. doi: 10.1055/s-2007-967184. Epub 2007 Apr 26.
The effect as antiviral agents versus viral hepatitis B and C of three compounds purified from natural products commonly used as remedies in traditional Chinese medicine, cantharidin, cephalotaxine and homoharingtonine, was investigated. To assess the activity of these compounds against flavivirus, we used bovine viral diarrhoea virus (BVDV) as a surrogate for hepatitis C virus (HCV). Anti-BVDV activity was determined by reduction in BVDV-RNA production and protection of infected embryonic bovine trachea (EBTr) cells against the cytopathic effect of BVDV. The effect versus hepatitis B virus (HBV) was investigated by measuring HBsAg and HBV-DNA release from hepatoblastoma HepG2 2.2.15 cells infected with HBV. As positive control we used the standard anti-HBV and anti-HCV drugs, lamivudine and ribavirin, respectively. Up to 100 microM lamivudine and ribavirin did not induce cell toxicity, whereas they induced dose-dependent anti-HBV and anti-BVDV effects, respectively. In the same range, cantharidin, cephalotaxine and homoharringtonine induced toxicity in EBTr cells and had no protective effect against BVDV. In contrast, they were able to inhibit HBV production at concentrations 10- to 100-fold lower than those inducing cell toxicity, which suggests that they are useless for the treatment of infection by flaviviruses, but potentially useful in combined therapy against hepatitis B.
研究了从常用作中药的天然产物中纯化得到的三种化合物——斑蝥素、三尖杉碱和高三尖杉酯碱——作为抗乙型和丙型病毒性肝炎药物的效果。为了评估这些化合物对黄病毒的活性,我们使用牛病毒性腹泻病毒(BVDV)作为丙型肝炎病毒(HCV)的替代物。通过降低BVDV-RNA的产生以及保护受感染的胚胎牛气管(EBTr)细胞免受BVDV的细胞病变效应来确定抗BVDV活性。通过测量感染HBV的肝癌HepG2 2.2.15细胞中HBsAg和HBV-DNA的释放来研究其对乙型肝炎病毒(HBV)的作用。作为阳性对照,我们分别使用了标准抗HBV和抗HCV药物拉米夫定和利巴韦林。高达100 microM的拉米夫定和利巴韦林不会诱导细胞毒性,而它们分别诱导剂量依赖性的抗HBV和抗BVDV作用。在相同范围内,斑蝥素、三尖杉碱和高三尖杉酯碱在EBTr细胞中诱导毒性,并且对BVDV没有保护作用。相比之下,它们能够在比诱导细胞毒性的浓度低10至100倍的浓度下抑制HBV产生,这表明它们对黄病毒感染的治疗无用,但可能对联合治疗乙型肝炎有用。