Anti-HIV-1 activities of compounds isolated from the medicinal plant Rhus chinensis
Anti-HIV-1 activities of compounds isolated from the medicinal plant Rhus chinensis
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从药用植物漆树中分离出的化合物的抗 HIV-1 活性
DOI：
10.1016/j.jep.2008.01.037
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发表时间：
2008-05-08
影响因子：
5.4
通讯作者：
Zheng, Yong-Tang
中科院分区：
文献类型：
--
作者：
Wang, Rui-Rui;Gu, Qiong;Zheng, Yong-Tang
研究目的：以前，我们报道了药用植物盐肤木的石油醚级分RC-1和EtOAc级分RC-2显示出有效的抗HIV-1活性。为了解决RC-1和RC-2的抗HIV-1成分，分离出17个化合物。方法：倒置显微镜下观察化合物对HIV-1诱导的合胞体形成的抑制作用，MTT法检测化合物对细胞的毒性和保护作用，ELISA法检测化合物对p24抗原表达水平和RT活性的抑制作用，荧光信号检测化合物对重组HIV-1 PR的抑制作用。化合物1和13有效抑制HIV-1诱导的合胞体形成，TI值分别为42.31和19.07。化合物4、5、6、9和10的效力较低，TI值分别为8.94、8.22、4.14、5.11和5.34。化合物1是一种苯并呋喃酮类化合物，以前被报道为一种新的抗HIV-1药物，可能靶向HIV-1生命周期的后期步骤。化合物13抑制HIV-1复制的EC_（50）为7.16 μ g/ml，其作用靶点可能在整合步骤之前。结论：这些化合物可能是药用植物盐肤木提取物抗HIV-1活性的一部分。(C)2008爱思唯尔爱尔兰有限公司保留所有权利。
Aim of the study: Previously, we reported that the petroleum ether fraction, RC-1, and EtOAc fraction, RC-2, of the medicinal plant Rhus chinensis showed potent anti-HIV-1 activities. To address anti-HIV-1 constituents of RC-1 and RC-2, 17 compounds were isolated. Anti-HIV-1 activities and possible action mechanisms of these compounds were investigated.Methods: The syncytial formation induced by HIV-1 was determined under the inverted microscope, cellular toxicity and protection assay were assessed by MTT method, reduction of p24 antigen expression level and RT activity were measured by ELISA, and inhibition of recombinant HIV-1 PR was monitored by the fluorescent signal.Results: The compounds 1 and 13 inhibited HIV-1-induced syncytium formation potently with TI value of 42.31 and 19.07, respectively. Compounds 4, 5, 6, 9 and 10 were less potent with TI value of 8.94, 8.22, 4.14, 5.11 and 5.34, respectively. Compound 1, a benzofuranone-type compound, previously reported as a novel anti-HIV-1 agent, might target late-steps of HIV-1 life cycle. Compound 13 inhibited HIV-1 replication with EC50 of 7.16 mu g/ml and might target at/before integration step.Conclusion: These compounds might contribute to anti-HIV-1 activities extracts of the medicinal plant Rhus chinensis. (C) 2008 Elsevier Ireland Ltd. All rights reserved.