少花斑鸠菊（菊科）倍半萜内酯的体外抗疟原虫和细胞毒性活性
In vitro antiplasmodial and cytotoxic activities of sesquiterpene lactones from Vernonia fimbrillifera Less. (Asteraceae).
作者信息
Bordignon Annélise, Frédérich Michel, Ledoux Allison, Campos Pierre-Eric, Clerc Patricia, Hermann Thomas, Quetin-Leclercq Joëlle, Cieckiewicz Ewa
机构信息
a Laboratory of Pharmacognosy, CIRM , University of Liège , Liège , Belgium.
b Laboratoire de Chimie des Substances Naturelles et de Sciences des Aliments (LCSNSA), Faculté des Sciences et Technologies , Université de La Réunion , Saint-Denis , La Réunion.
出版信息
Nat Prod Res. 2018 Jun;32(12):1463-1466. doi: 10.1080/14786419.2017.1350665. Epub 2017 Jul 10.
Due to the in vitro antiplasmodial activity of leaf extracts from Vernonia fimbrillifera Less. (Asteraceae), a bioactivity-guided fractionation was carried out. Three sesquiterpene lactones were isolated, namely 8-(4'-hydroxymethacrylate)-dehydromelitensin (1), onopordopicrin (2) and 8α-[4'-hydroxymethacryloyloxy]-4-epi-sonchucarpolide (3). Their structures were elucidated by spectroscopic methods (1D and 2D NMR and MS analyses) and by comparison with published data. The isolated compounds exhibited antiplasmodial activity with IC values ≤ 5 μg/mL. Cytotoxicity of the compounds against a human cancer cell line (HeLa) and a mouse lung epithelial cell line (MLE12) was assessed to determine selectivity. Compound 3 displayed promising selective antiplasmodial activity (SI > 10).
由于飞扬草（菊科）叶提取物具有体外抗疟原虫活性，因此进行了生物活性导向的分离。分离出三种倍半萜内酯，即8-(4'-羟基甲基丙烯酸酯)-脱氢蜂斗菜素（1）、苦苣菜素（2）和8α-[4'-羟基甲基丙烯酰氧基]-4-表异土木香内酯（3）。通过光谱方法（一维和二维核磁共振以及质谱分析）并与已发表的数据进行比较来阐明它们的结构。分离出的化合物表现出抗疟原虫活性，IC值≤5μg/mL。评估了这些化合物对人癌细胞系（HeLa）和小鼠肺上皮细胞系（MLE12）的细胞毒性以确定其选择性。化合物3显示出有前景的选择性抗疟原虫活性（选择性指数>10）。
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