Flavonoid baicalin inhibits HIV-1 infection at the level of viral entry
Flavonoid baicalin inhibits HIV-1 infection at the level of viral entry
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DOI：
10.1006/bbrc.2000.3485
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发表时间：
2000-09-24
影响因子：
3.1
通讯作者：
Wang, JM
中科院分区：
文献类型：
--
作者：
Li, BQ;Fu, T;Wang, JM
黄芩苷（Baicalin，BA）是从药用植物黄芩中提取的一种黄酮类化合物，具有抗炎和抗HIV-1活性。为了阐明BG抗炎作用的机制，我们最近发现这种类黄酮化合物能够与选定的趋化因子形成复合物，并减弱其结合和激活细胞表面受体的能力。这些观察结果促使我们研究BA是否可以通过干扰病毒进入来抑制HIV-1感染，这一过程已知涉及HIV-1包膜蛋白与细胞CD 4和趋化因子受体之间的相互作用。结果表明，BA在非细胞毒性浓度下，能抑制HIV-1 Env蛋白与表达CD_4/CXCR_4或CD_4/CCR_5的细胞的融合，并能阻断HIV-1早期强终止DNA在细胞内的复制。由于BA不抑制HIV-1gp 120与CD_4的结合，我们推测BA可能干扰HIV-1 Env与趋化因子辅助受体的相互作用，阻断HIV-1进入靶细胞，因此，BA可作为开发新型抗HIV-1药物的基础。
Baicalin (BA) is a flavonoid compound purified from medicinal plant Scutellaria baicalensis Georgi and has been shown to possess anti-inflammatory and anti-HIV-1 activities. In an effort to elucidate the mechanism of the anti-inflammatory effect of BG we recently found that this flavonoid compound was able to form complexes with selected chemokines and attenuated their capacity to bind and activate receptors on the cell surface. These observations prompted us to investigate whether BA could inhibit HIV-1 infection by interfering with viral entry, a process known to involve interaction between HIV-1 envelope proteins and the cellular CD4 and chemokine receptors. We found that BA at the noncytotoxic concentrations, inhibited both T cell tropic (X4) and monocyte tropic (R5) HIV-1 Env protein mediated fusion with cells expressing CD4/CXCR4 or CD4/CCR5, Furthermore, presence of BA at the initial stage of HIV-1 viral adsorption blocked the replication of HIV-1 early strong stop DNA in cells. Since BA did not inhibit binding of HIV-1 gp120 to CD4, we propose that BA may interfere with the interaction of HIV-1 Env with chemokine coreceptors and block HIV-1 entry of target cells, Therefore, BA can be used as a basis for developing novel anti-HIV-l agents.