Chemical constituents of Anacolosa pervilleana and their antiviral activities
Chemical constituents of Anacolosa pervilleana and their antiviral activities
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DOI：
10.1016/j.fitote.2012.05.004
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发表时间：
2012-09-01
期刊：
影响因子：
3.4
通讯作者：
Litaudon, Marc
中科院分区：
文献类型：
--
作者：
Bourjot, Melanie;Leyssen, Pieter;Litaudon, Marc
为了鉴定基孔肯雅热 (CHIN) 和登革热 (DENV) 病毒复制的新型抑制剂，在基于病毒细胞的 CHIKV 测定和 DENV NS5 RNA 依赖性 RNA 聚合酶 (RdRp) 测定中，对马达加斯加植物的 820 种乙酸乙酯提取物进行了系统研究。选择从 Anacolosa pervilleana 叶子中获得的提取物是因为其在两项测定中均具有显着活性。一种名为 anacolosine 的新 (E)-tridec-2-en-4-ynedioic 酸 (1)，以及三种已知的乙炔酸，octadeca-9,11,13-三炔酸 (2)、(13E)-octadec-13-en-9,11-二炔酸 (3)、(13E)-octadec-13-en-11-ynoic 酸 (4)、两种分离出萜类化合物、羽扇豆酮 (5) 和 β-amyron (6)，以及一种氰苷 (S)-sambunigrin (7)。通过核磁共振波谱和质谱数据的综合分析阐明了它们的结构。评估了这些化合物对 CHIKV、DENV RdRp 和西尼罗河聚合酶病毒 (WNV RdRp) 的抑制效力。两种萜类化合物都显示出针对 CHIKV 的中等活性（EC50 分别为 77 和 86 μM），并且在 DENV RdRp 测定中乙炔酸产生的 IC50 值约为 3 μM。 (C) 2012 Elsevier B.V. 保留所有权利。
In an effort to identify novel inhibitors of Chikungunya (CHIN) and Dengue (DENV) virus replication, a systematic study with 820 ethyl acetate extracts of Madagascan plants was performed in a virus-cell-based assay for CHIKV and a DENV NS5 RNA-dependant RNA polymerase (RdRp) assay. The extract obtained from the leaves of Anacolosa pervilleana was selected for its significant activity in both assays. One new (E)-tridec-2-en-4-ynedioic acid named anacolosine (1), together with three known acetylenic acids, the octadeca-9,11,13-triynoic acid (2), (13E)-octadec-13-en-9,11-diynoic acid (3), (13E)-octadec-13-en-11-ynoic acid (4), two terpenoids, lupenone (5) and beta-amyrone (6), and one cyanogenic glycoside, (S)-sambunigrin (7) were isolated. Their structures were elucidated by comprehensive analyses of NMR spectroscopy and mass spectrometry data. The inhibitory potency of these compounds was evaluated on CHIKV, DENV RdRp and West-Nile polymerase virus (WNV RdRp). Both terpenoids showed a moderate activity against CHIKV (EC50 77 and 86 mu M, respectively) and the acetylenic acids produced IC50 values around 3 mu M in the DENV RdRp assay. (C) 2012 Elsevier B.V. All rights reserved.