Effect of artemisinin/artesunate as inhibitors of hepatitis B virus production in an "in vitro" replicative system
Effect of artemisinin/artesunate as inhibitors of hepatitis B virus production in an "in vitro" replicative system
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DOI：
10.1016/j.antiviral.2005.07.005
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发表时间：
2005-11-01
影响因子：
7.6
通讯作者：
Marin, JJG
中科院分区：
文献类型：
--
作者：
Romero, MR;Efferth, T;Marin, JJG
研究了青蒿素及其衍生物青蒿琥酯等中药高纯度化合物的抗乙肝病毒作用。通过测定药物作用21d后细胞表面蛋白(HBs-Ag)和HBVDNA的释放，确定永久性转染组HepG2 2.2.15细胞产生HBV量。Southern-blotting检测释放的HBVDNA的形式。采用中性红滞留试验评价药物对宿主细胞的毒性。根据它们的潜在兴趣，这些化合物被分类如下：(I)无：它们对病毒产生没有影响(大豆苷元、大豆素、异黄酮苷、那度呋喃、拿多西农、四氢洋黄素和槲皮素)；(Ii)低：它们能显著减少病毒产生，但对宿主细胞(黄连素和单宁酸)也有诱导毒性；或它们对宿主细胞没有毒性作用，但只有中等能力减少病毒产生(姜黄素、黄芩素、黄芩苷、蟾酥、二烯丙基二硫、甘草酸和葛根素)；(3)高：在不影响宿主细胞活力的浓度(青蒿素和青蒿琥酯)下，它们能强烈抑制病毒的产生。此外，青蒿琥酯与拉莫夫定联用具有协同抗乙肝作用，值得进一步评价青蒿素/青蒿琥酯作为抗乙肝病毒药物的作用。(C)2005 Elsevier B.V.保留所有权利。
The antiviral effect against hepatitis B virus (HBV) of artemisinin, its derivative artesunate and other compounds highly purified from traditional Chinese medicine remedies, were investigated. HBV production by permanently transfected HepG2 2.2.15 cells was determined by measuring the release of surface protein (HBsAg) and HBV-DNA after drug exposure (0.01-100 mu M) for 21 days. The forms of HBV-DNA released were investigated by Southern-blotting. Neutral Red retention test was used to evaluate drug-induced toxicity on host cells. The compounds were classified according to their potential interest as follows: (i) none: they had no effect on viral production (daidzein, daidzin, isonardosinon, nardofuran, nardosinon, tetrahydronardosinon and quercetin); (ii) low: they were able to markedly reduce viral production, but also induced toxicity on host cells (berberine and tannic acid) or they had no toxic effect on host cells but only had a moderate ability to reduce viral production (curcumin, baicalein, baicalin, bufalin, diallyl disulphide, glycyrrhizic acid and puerarin); (iii) high: they induced strong inhibition of viral production at concentrations at which host cell viability was not affected (artemisinin and artesunate). Moreover, artesunate in conjunction with larmvudine had synergic anti-HBV effects, which warrants further evaluation of artemisinin/artesunate as antiviral agents against HBV infection. (c) 2005 Elsevier B.V. All rights reserved.