The inhibitory effect of dehydroepiandrosterone and its derivatives against influenza A virus in vitro and in vivo

The inhibitory effect of dehydroepiandrosterone and its derivatives against influenza A virus in vitro and in vivo
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脱氢表雄酮及其衍生物对甲型流感病毒的体内外抑制作用

DOI:
10.1007/s00705-016-2993-6
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发表时间:
2016
影响因子:
2.7
通讯作者:
Li
Li
中科院分区:
医学4区
文献类型:
--
作者:
Qingyu Yang;Q. Mao;Manli Liu;Kaimei Wang;Zhaoyuan Wu;Wei Fang;Ziwen Yang;P. Luo;Shaoyong Ke;Li

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在体外细胞培养中,研究了脱氢表雄酮(DHEA)及其21个合成衍生物对甲型流感病毒(IAV)的抗病毒活性。我们的研究结果表明,三个DHEA类似物是有效的抑制IAV增殖在MDCK细胞,主要是阻断病毒感染的后附着阶段。在这些衍生物中,含有2-OH-Ph基团的衍生物(3 i)表现出最好的抑制H1N1和H3 N2 IAV的作用,并呈剂量依赖性。此外,用化合物3 i处理降低了子代病毒产量、病毒RNA合成和蛋白质表达。以25或50 mg/kg/天口服给药化合物3 i 5天,通过降低肺中的病毒滴度和促进受感染小鼠的存活,保护小鼠免受致死性A/FM/1/47(H1N1)攻击。我们的研究结果表明,DHEA-二腙衍生物可能提供有前途的铅支架进一步设计和潜在的抗病毒药物的合成。
The antiviral activity of dehydroepiandrosterone (DHEA) and 21 synthetic derivatives against influenza A virus (IAV) replication was investigated in vitro in cell culture. Our results revealed that three DHEA analogues were potent inhibitors of IAV multiplication in MDCK cells and mainly blocked the post-attachment stage of viral infection. Among these derivatives, one containing a 2-OH-Ph moiety (3i) exhibited the best inhibitory effects against H1N1 and H3N2 IAV in a dose-dependent manner. Moreover, treatment with compound 3i decreased progeny virus yields, viral RNA synthesis and protein expression. Orally administered compound 3i at 25 or 50 mg/kg/day for 5 days protected mice from lethal A/FM/1/47 (H1N1) challenge by reducing the viral titers in the lungs and promoting survival of infected mice. Our results suggest that DHEA-dihydrazone derivatives may provide promising lead scaffolds for further design and synthesis of potential antiviral agents.
雄烯二醇通过增加 I 型干扰素的产生来拮抗 1 型单纯疱疹病毒诱发的脑炎。
DOI: --
发表时间: 1998
期刊: Journal of immunology (Baltimore, Md. : 1950)
影响因子: --
作者:
Daigle,J;Carr,DJ
通讯作者: Carr,DJ
DOI: 10.1093/gerona/55.9.b418
发表时间: 2000
期刊: The journals of gerontology. Series A, Biological sciences and medical sciences
影响因子: --
作者:
Padgett,DA;MacCallum,RC;Loria,RM;Sheridan,JF
通讯作者: Sheridan,JF
脱氢表雄酮和 16 α-溴-表雄酮:EB 病毒诱导的人类淋巴细胞转化的抑制剂。
DOI: 10.1093/carcin/2.7.683
发表时间: 1981
期刊: Carcinogenesis
影响因子: 4.7
作者:
Henderson,E;Schwartz,A;Pashko,L;Abou-Gharbia,M;Swern,D
通讯作者: Swern,D