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首页> 外文期刊>Antiviral chemistry & chemotherapy >Epigallocatechin gallate inhibits the HIV reverse transcription step.
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Epigallocatechin gallate inhibits the HIV reverse transcription step.

机译：表没食子儿茶素没食子酸酯抑制HIV逆转录步骤。

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摘要

Epigallocatechin gallate (EGCG), the most abundant catechin in green tea, has been reported to inhibit HIV-1 replication prior to its integration into host DNA via various proposed mechanisms; however, the specific main target(s) of EGCG remain unclear. In this study, we investigated a number of these proposed detailed mechanism(s) using a cell-based model.Multinuclear activation of galactosidase indicator assays were used for all experiments, including examination of the time of addition and the synergisms with a nucleoside reverse transcriptase inhibitor, 3'-azido-3'-deoxythymidine (AZT).The experiments revealed that EGCG suppressed both HIV-1(IIIB) and HIV-2(EHO) infection in HeLa-CD4-LTR-β-gal cells, with relatively low 50% effective concentrations of 1.6 and 2.0 μM, respectively. The inhibitory profile of EGCG generated using a time-of-addition assay was identical to that of a non-nucleoside reverse transcriptase inhibitor (NNRTI), MKC-442. Furthermore, synergistic inhibition was observed in EGCG with AZT.Based on our findings, EGCG appears to act mainly as an allosteric reverse transcriptase inhibitor with mechanisms different from those of currently approved NNRTIs that directly interact with the NNRTI binding pocket. Thus, EGCG is a good candidate for use as an additional or supportive anti-HIV agent derived from natural plants.
机译：表没食子儿茶素没食子酸酯（EGCG）是绿茶中最丰富的儿茶素，据报道，在通过各种提议的机制将其整合到宿主DNA中之前，它会抑制HIV-1复制。但是，EGCG的具体主要目标仍不清楚。在这项研究中，我们使用基于细胞的模型研究了许多这些拟议的详细机制。半乳糖苷酶指示剂测定法的多核激活用于所有实验，包括检查加入时间和与核苷逆转录酶的协同作用。抑制剂3'-azido-3'-deoxythymidine（AZT）。实验表明，EGCG抑制HeLa-CD4-LTR-β-gal细胞中的HIV-1（IIIB）和HIV-2（EHO）感染， 50％的有效浓度分别为1.6和2.0μM。使用添加时间测定法生成的EGCG的抑制谱与非核苷逆转录酶抑制剂（NNRTI）MKC-442相同。此外，在EGCG和AZT中观察到协同抑制作用。基于我们的发现，EGCG似乎主要是一种变构逆转录酶抑制剂，其机制不同于目前批准的与NNRTI结合口袋直接相互作用的NNRTIs。因此，EGCG是用作衍生自天然植物的附加或支持性抗HIV剂的良好候选者。

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