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Aprotinin, a protease inhibitor, suppresses proteolytic activation of pandemic H1N1v influenza virus.

机译:抑制蛋白酶,一种蛋白酶抑制剂,抑制大流行性H1N1V流感病毒的蛋白水解活化。

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BACKGROUND: The recent emergence of pandemic influenza virus H1N1v stresses the need for the development of new anti-influenza drugs. METHODS: Host proteases responsible for viral haemagglutinin (HA) cleavage are attractive targets for such drugs. Aprotinin, a natural 58-amino-acid polypeptide from bovine lungs, was chosen for this purpose because it is a drug already approved for human use as an antiprotease compound to treat pancreatitis and bleeding, and because it inhibits a wide spectrum of serine proteases, some of which are involved in influenza virus activation. RESULTS: First, we show that HA of pandemic H1N1v was intensively cleaved and activated in different host systems (human tracheo-bronchial epithelium, human intestinal Caco-2 cells and chicken embryonated eggs). Second, aprotinin inhibited HA cleavage and replication of pandemic influenza virus H1N1v in all host systems, including human tracheo-bronchial epithelium. Third, aprotinin did not induce any apparent toxic side effects in these hosts. CONCLUSIONS: Aprotinin can be considered a promising drug against the novel H1N1v pandemic influenza virus.
机译:背景:最近流动性流感病毒H1N1V的出现强调了新的抗流感药物的发展。方法:负责病毒Haemagglutinin(HA)裂解的宿主蛋白酶是此类药物的吸引力。为此目的选择了来自牛肺的天然58-氨基酸多肽的抑肽蛋白,因为它是已经批准用于人类用作抗转油酶化合物的药物,以治疗胰腺炎和出血,并且因为它抑制了广谱的丝氨酸蛋白酶,其中一些参与流感病毒激活。结果:首先,我们表明,在不同的宿主系统(人的气管支气管上皮,人肠道CaCo-2细胞和鸡胚胎卵)中,大流行H1N1V的HA被强烈切割和激活。其次,抑肽蛋白抑制了所有宿主系统中的HA切割和大流行性流感病毒H1N1V的复制,包括人的气管支气管上皮。第三,抑肽肽在这些宿主中没有诱导任何明显的有毒副作用。结论:抑肽肽可以被认为是针对新型H1N1V大流行性流感病毒的有希望的药物。

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