Antiplasmodial activity of aporphine alkaloids and sesquiterpene lactones from Liriodendron tulipifera L.
Antiplasmodial activity of aporphine alkaloids and sesquiterpene lactones from Liriodendron tulipifera L.
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DOI：
10.1016/j.jep.2010.08.059
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发表时间：
2011-01-07
影响因子：
5.4
通讯作者：
Raskin, Ilya
中科院分区：
文献类型：
--
作者：
Graziose, Rocky;Rathinasabapathy, Thirumurugan;Raskin, Ilya
研究目的：本研究的目的是分离和表征传统上使用的抗疟植物鹅掌楸的活性成分，通过抗疟原虫检测指导fractionation.Materials和方法：树皮和叶子提取的极性增加的溶剂。使用快速色谱法、逆流色谱法和制备型HPLC产生级分，并进行体外抗疟原虫和细胞毒性测定。结果与讨论：6种已知的阿朴啡生物碱，即asiomobine（1），norushinsunine（2），norglaucine（3），liriodenine（4），anonaine（5）和oxoglaucine（6），被发现与树皮的抗疟原虫活性有关。叶产生两种已知的具有抗疟原虫活性的倍半萜内酯，过氧铁（7）和异铁（8）。化合物（2）的抗疟原虫活性（IC 50 = 29.6 μ g/mL），（3）（IC 50 = 22.0 μ g/mL），（6）（IC 50 = 9.1 μ g/mL），（7）（IC 50 = 6.2 μ g/mL）和（8）（IC 50 = 1.8 μ g/mL）。结论：这项工作支持历史上使用鹅掌楸作为美国的抗疟疾药物，并表征其抗疟原虫成分。(C)2010爱思唯尔爱尔兰有限公司版权所有。
Aim of the study: The objective of this study was to isolate and characterize the active constituents of the traditionally used antimalarial plant Liriodendron tulipifera by antiplasmodial-assay guided fractionation.Materials and methods: Bark and leaves were extracted with solvents of increasing polarity. Fractions were generated using flash chromatography, counter current chromatography and preparative HPLC and subjected to in vitro antiplasmodial and cytotoxicity assays. Active fractions were subjected to further fractionation until pure compounds were isolated, for which the IC50 values were calculated.Results and discussion: Six known aporphine alkaloids, asimilobine (1), norushinsunine (2), norglaucine (3), liriodenine (4), anonaine (5) and oxoglaucine (6) were found to be responsible for the antiplasmodial activity of the bark. Leaves yielded two known sesquiterpene lactones, peroxyferolide (7) and lipiferolide (8) with antiplasmodial activity. The antiplasmodial activity of (2) (IC50 = 29.6 mu g/mL), (3) (IC50 = 22.0 mu g/mL), (6) (IC50 = 9.1 mu g/mL), (7) (IC50 = 6.2 mu g/mL) and (8) (IC50 = 1.8 mu g/mL) are reported for the first time.Conclusion: This work supports the historical use of Liriodendron tulipifera as an antimalarial remedy of the United States and characterizes its antiplasmodial constituents. (C) 2010 Elsevier Ireland Ltd. All rights reserved.