Highly potent anti-HIV-1 activity isolated from fermented Polygonum tinctorium Aiton
Highly potent anti-HIV-1 activity isolated from fermented Polygonum tinctorium Aiton
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DOI：
10.1016/j.antiviral.2005.02.003
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发表时间：
2005-06-01
影响因子：
7.6
通讯作者：
Yamamoto, N
中科院分区：
文献类型：
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作者：
Zhong, Y;Yoshinaka, Y;Yamamoto, N
发酵的蓼属植物艾顿（Polygonaceae）的水溶性提取物苏库莫在体外表现出对HIV I型的有效抑制活性。该提取物有效地抑制MT-4细胞中的急性HIV-1（IIIB）感染，EC 50值为0.5 μ g/ml，但即使在高浓度（CC 50> 1000 μ g/ml）下也表现出对MT-4细胞的低细胞毒性。它还抑制HIV感染细胞和未感染Molt-4细胞共培养物中巨细胞的形成。发现苏库莫提取物与病毒包膜糖蛋白和细胞受体相互作用，从而阻断病毒-细胞结合和病毒诱导的合胞体形成。该提取物的抗HIV-1活性与其对HIV-1结合的抑制作用之间存在良好的相关性。它还抑制单纯疱疹病毒I型在Vero细胞中的复制，EC 50为11.56 μ g/ml。另一方面，当在3.2 - 400 μ g/ml的浓度范围内测试时，如细胞病变效应（CPE）的显微图像分析所示，没有明显的抗甲型流感病毒、脊髓灰质炎病毒或SARS冠状病毒的活性。物理化学研究表明，在1N HCl或1N NaOH中于100 ℃煮沸后，以及用100 mM NaIO4处理后，提取物中的抗HIV活性基本上保持不变。链霉蛋白酶消化后提取物的抑制活性也没有降低。提取物中的活性因子可能是具有聚阴离子亚结构和分子量为10，000 - 50，000的新型化合物。(c)2005 Elsevier B.V.保留所有权利。
A water-soluble extract of fermented Polygonum tinctorium Aiton (Polygonaceae) called Sukumo, exhibited a potent inhibitory activity against HIV type I in vitro. The extract potently suppressed acute HIV-1 (IIIB) infection in MT-4 cells with EC50 values of 0.5 mu g/ml but exhibited low cytotoxicity to MT-4 cells even at a high concentration (CC50 > 1000 mu g/ml). It also inhibited giant cell formation in co-cultures of HIV-infected cells and uninfected Molt-4 cells. Sukumo extract was found to interact with both the viral envelope glycoprotein and cellular receptors, thus blocking virus-cell binding and virus-induced syncytium formation. There was a good correlation between the extract's anti-HIV-1 activity and its inhibitory effects on HIV-1 binding. It also suppressed replication of herpes simplex virus type I in Vero cells with an EC50 of 11.56 mu g/ml. On the other hand, there was no appreciable activity against influenza A virus, poliovirus or SARS corona virus when tested at concentrations ranging from 3.2-400 mu g/ml as shown by microscopic image analysis for cytopathic effect (CPE). Physico-chemical studies revealed that the anti-HIV activity in the extract was essentially maintained after boiling at 100 degrees C in 1N HCl or 1N NaOH, and after treatment with 100 mM NaIO4. The inhibitory activity of the extract was also not reduced after pronase digestion. The active factor in the extract is likely to be a novel compound(s) having a polyanionic substructure and a molecular weight of 10,000-50,000. (c) 2005 Elsevier B.V. All rights reserved.