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EPs® 7630(南非钩麻提取物),一种从西洋梨根中提取的物质,具有体外和体内抗流感病毒活性。

EPs® 7630 (Umckaloabo®), an extract from Pelargonium sidoides roots, exerts anti-influenza virus activity in vitro and in vivo.

机构信息

Institute of Immunology, Centre de Recherche Public de la Santé/Laboratoire National de Santé, Luxembourg, Luxembourg.

出版信息

Antiviral Res. 2012 May;94(2):147-56. doi: 10.1016/j.antiviral.2012.03.006. Epub 2012 Mar 28.

Abstract

A prodelphinidin-rich extract from Pelargonium sidoides DC, EPs® 7630 (Umckaloabo®), which is licensed to treat respiratory tract infections such as acute bronchitis, was investigated for its antiviral effects. EPs® 7630 showed dose-dependent anti-influenza activity at non-toxic concentrations against pandemic H1N1, oseltamivir-sensitive and -resistant seasonal H1N1, seasonal H3N2 and the laboratory H1N1 strain A/Puerto Rico/8/34, while it had no antiviral activity against adenovirus or measles virus. The extract inhibited an early step of influenza infection and impaired viral hemagglutination as well as neuraminidase activity. However, EPs® 7630 did not exhibit a direct virucidal effect, as virus preincubation (unlike cell preincubation) with the extract did not influence infectivity. Importantly, EPs® 7630 showed no propensity to resistance development in vitro. Analysis of EPs® 7630 constituents revealed that prodelphinidins represent the active principle. Chain length influenced antiviral activity, as monomers and dimers were less effective than oligo- and polymers. Importantly, gallocatechin and its stereoisomer epigallocatechin exert antiviral activity also in their monomeric form. In addition, EPs® 7630 administered by inhalation significantly improved survival, body weight and body temperature of influenza-infected mice, without obvious toxicity, demonstrating the benefit of EPs® 7630 in treatment of influenza.

摘要

Pelargonium sidoides DC 的 prodelphinidin 丰富提取物,EPs®7630(Umckaloabo®),被授权用于治疗呼吸道感染,如急性支气管炎,其抗病毒作用得到了研究。EPs®7630 在非毒性浓度下对大流行性 H1N1、奥司他韦敏感和耐药季节性 H1N1、季节性 H3N2 和实验室 H1N1 株 A/Puerto Rico/8/34 表现出剂量依赖性的抗流感活性,而对腺病毒或麻疹病毒没有抗病毒活性。该提取物抑制流感感染的早期步骤,并损害病毒血凝和神经氨酸酶活性。然而,EPs®7630 没有表现出直接的病毒杀伤作用,因为与提取物预孵育病毒(不像细胞预孵育)并不影响感染性。重要的是,EPs®7630 在体外没有表现出耐药性发展的倾向。对 EPs®7630 成分的分析表明,原花青素是其活性成分。链长影响抗病毒活性,因为单体和二聚体不如寡聚体和聚合物有效。重要的是,没食子酸和其立体异构体表没食子儿茶素即使在单体形式下也具有抗病毒活性。此外,通过吸入给予 EPs®7630 可显著提高流感感染小鼠的存活率、体重和体温,而没有明显的毒性,表明 EPs®7630 在治疗流感方面的益处。

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