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首页> 外文期刊>Antiviral chemistry & chemotherapy >In vitro and in vivo anti-influenza virus activity of diarylheptanoids isolatedfrom Alpinia officinarum.
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In vitro and in vivo anti-influenza virus activity of diarylheptanoids isolatedfrom Alpinia officinarum.

机译：从高良姜中分离得到的二芳基庚烷类化合物的体外和体内抗流感病毒活性。

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BACKGROUND: Diarylheptanoids (AO-0002[7-(4''-hydroxy-3''-methoxyphenyl)-1-phenyl-4E-hepten-3-one] and AO-0011[(5S)-5-hydroxy-7-(4''-hydroxyphenyl)-1-phenyl-3-heptanone]) isolated fromAlpinia officinarum have been reported to exhibit anti-influenza virus activityin vitro. Hence, efficacies against influenza virus infection and the mode ofantiviral action were evaluated in vivo and in vitro, respectively.METHODS: In a murine influenza virus infection model, diarylheptanoids wereorally administered three times daily to mice infected with influenza A/PR/8/34virus for 6 days after infection. AO-0002 was examined for its antiviral activityagainst the wild types of influenza viruses A/PR/8/34 (H1N1),oseltamivir-resistant A/PR/8/34 (H1N1), A/Bangkok/93/03 (H1N1), A/Ishikawa/7/82(H3N2), A/Fukushima/13/43 (H3N2), B/Singapore/222/79 and B/Fukushima/15/93 inplaque reduction or yield reduction assays. The mode of anti-influenza virusaction was assessed by a virus adsorption assay, immunofluorescence assay ofviral antigens, and inhibition of viral messenger RNA synthesis using real-timereverse transcriptase PCR.RESULTS: AO-0002 at 100 mg/kg was significantly effective in reducing the bodyweight loss and prolonging survival times of infected mice without toxicity, butAO-0011 was not. AO-0002 at 30 and 100 mg/kg significantly reduced virus titresin bronchoalveolar lavage fluids of the lungs on days 3 and 6 after infection.AO-0002 exhibited anti-influenza virus activity against all viruses used,including the oseltamivir-resistant strain in vitro. The compound had no effecton virus adsorption or invasion into cells, but dose-dependently suppressed theexpression of viral messenger RNA and antigens.CONCLUSIONS: AO-0002 was suggested to have a different anti-influenza virusaction to that of oseltamivir and was verified to show anti-influenza activity invitro and in vivo.
机译：背景：二芳基庚烷类化合物（AO-0002 [7-（4''-羟基-3''-甲氧基苯基）-1-苯基-4E-庚烯-3-一]和AO-0011 [（5S）-5-羟基-7据报道，从高良姜中分离出的-（（4′-羟苯基）-1-苯基-3-庚酮]）在体外表现出抗流感病毒活性。因此，分别在体内和体外评估了抗流感病毒感染的功效和抗病毒作用的方式。方法：在鼠流感病毒感染模型中，每天两次向感染A / PR / 8/34流感病毒的小鼠口服二芳基庚烷类药物感染后持续6天。检查了AO-0002对野生型流感病毒A / PR / 8/34（H1N1），耐耐奥司他韦的A / PR / 8/34（H1N1），A /曼谷/ 93/03（H1N1）的抗病毒活性，A /石川/ 7/82（H3N2），A /福岛/ 13/43（H3N2），B /新加坡/ 222/79和B /福岛/ 15/93斑块减少或产量减少测定。通过病毒吸附测定，病毒抗原的免疫荧光测定以及使用实时逆转录酶PCR抑制病毒信使RNA的合成来评估抗流感病毒的作用模式。结果：100 mg / kg的AO-0002可以有效地降低流感病毒的体重减轻并延长了无毒性感染小鼠的存活时间，但AO-0011没有。 AO-0002在感染后第3天和第6天以30和100 mg / kg的剂量显着降低肺中的病毒滴度，支气管肺泡灌洗液.AO-0002对所有使用的病毒均表现出抗流感病毒活性，包括体外对oseltamivir的耐​​药株。该化合物对病毒的吸附或侵袭没有影响，但剂量依赖性地抑制了病毒信使RNA和抗原的表达。结论：AO-0002被认为与奥司他韦具有不同的抗流感病毒作用，并被证明具有抗流感病毒的作用。 -流感活性在体外和体内。

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