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Antiviral activity of hop constituents against a series of DNA and RNA viruses.

机译:啤酒花成分对一系列DNA和RNA病毒的抗病毒活性。

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We investigated whether crude hop extracts and purified hop components representing every major chemical class of hop compound have antiviral activity. These hop constituents were tested for antiviral activity against bovine viral diarrhea virus (BVDV) as a surrogate model of hepatitis C virus (HCV), human immunodeficiency virus (HIV), influenza A virus (FLU-A), influenza B virus (FLU-B), rhinovirus (Rhino), respiratory syncytial virus (RSV), yellow fever virus (YFV), cytomegalovirus (CMV), hepatitis B virus (HBV), and herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2). The extracts all failed to prevent the replication of HIV, FLU-A, FLU-B, RSV and YFV. A xanthohumol-enriched hop extract displayed a weak to moderate antiviral activity against BVDV (therapeutic index (TI)=6.0), HSV-2 (TI=>5.3), Rhino (TI=4.0) and HSV-1 (TI=>1.9) with IC(50) values in the low microg/ml range. Pure iso-alpha-acids demonstrated low to moderate antiviral activity against both BVDV (TI=9.1) and CMV (TI=4.2) with IC(50) values in the low microg/ml range. No antiviral activity was detected using beta-acids or a hop oil extract. Ultra-pure preparations (>99% pure) were used to show that xanthohumol accounted for the antiviral activity observed in the xanthohumol-enriched hop extract against BVDV, HSV-1 and HSV-2. Xanthohumol was found to be a more potent antiviral agent against these viruses than the isomer iso-xanthohumol. With Rhino, the opposite trend was observed with iso-xanthohumol showing superior antiviral activity to that observed with xanthohumol. Xanthohumol also showed antiviral activity against CMV, suggesting that it might have a generalized anti-herpesvirus antiviral activity. Again, superior antiviral activity was observed with the xanthohumol isomer against CMV. In summary, iso-alpha-acids and xanthohumol were shown to have a low-to-moderate antiviral activity against several viruses. These hop constituents might serve as interesting lead compounds from which more active anti-HCV, anti-Rhino and anti-herpesvirus antiviral agents could be synthesized.
机译:我们调查了代表啤酒花化合物每种主要化学类别的啤酒花粗提取物和纯化的啤酒花成分是否具有抗病毒活性。测试了这些蛇麻草成分对牛病毒性腹泻病毒(BVDV)的抗病毒活性,作为丙型肝炎病毒(HCV),人免疫缺陷病毒(HIV),甲型流感病毒(FLU-A),乙型流感病毒(FLU- B),鼻病毒(Rhino),呼吸道合胞病毒(RSV),黄热病病毒(YFV),巨细胞病毒(CMV),乙型肝炎病毒(HBV)和1型单纯疱疹病毒(HSV-1)和2型单纯疱疹病毒(HSV) -2)。提取物均未能阻止HIV,FLU-A,FLU-B,RSV和YFV的复制。富含黄腐酚的啤酒花提取物显示出对BVDV(治疗指数(TI)= 6.0),HSV-2(TI => 5.3),犀牛(TI = 4.0)和HSV-1(TI => 1.9)的弱至中度抗病毒活性)的IC(50)值在低microg / ml范围内。纯的异α-酸显示出对BVDV(TI = 9.1)和CMV(TI = 4.2)的低至中度抗病毒活性,IC(50)值在低微克/毫升范围内。使用β-酸或啤酒花油提取物未检测到抗病毒活性。超纯制剂(纯度> 99%)用于表明黄腐酚在富含黄腐酚的啤酒花提取物中观察到了对BVDV,HSV-1和HSV-2的抗病毒活性。发现黄腐酚比异构体异黄腐酚对这些病毒有更强的抗病毒作用。在Rhino上,异黄腐酚观察到相反的趋势,显示出优于黄腐酚的抗病毒活性。 Xanthohumol还显示出抗CMV的抗病毒活性,表明它可能具有广义的抗疱疹病毒抗病毒活性。再次,黄嘌呤酚异构体对CMV观察到了优异的抗病毒活性。总之,异α-酸和黄腐酚被证明对几种病毒具有低到中等的抗病毒活性。这些蛇麻草成分可以作为有趣的先导化合物,从中可以合成更具活性的抗HCV,抗犀牛和抗疱疹病毒抗病毒药。

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