灰毡毛忍冬中的倍半萜内酯及其体外抗锥虫活性。
Sesquiterpene Lactones from Vernonia cinerascens Sch. Bip. and Their in Vitro Antitrypanosomal Activity.
机构信息
Institute of Pharmaceutical Biology and Phytochemistry (IPBP), University of Münster, PharmaCampus Corrensstraße 48, D-48149 Münster, Germany.
Department of Chemistry, Egerton University, P.O. Box 536, Egerton 20115, Kenya.
出版信息
Molecules. 2018 Jan 27;23(2):248. doi: 10.3390/molecules23020248.
In the endeavor to obtain new antitrypanosomal agents, particularly sesquiterpene lactones, from Kenyan plants of the family Asteraceae, Sch. Bip. was investigated. Bioactivity-guided fractionation and isolation in conjunction with LC/MS-based dereplication has led to the identification of vernodalol () and isolation of vernodalin (), 11β,13-dihydrovernodalin (), 11β,13-dihydrovernolide (), vernolide (), 11β,13-dihydrohydroxyvernolide (), hydroxyvernolide (), and a new germacrolide type sesquiterpene lactone vernocinerascolide () from the dichloromethane extract of leaves. Compounds - were characterized by extensive analysis of their 1D and 2D NMR spectroscopic and HR/MS spectrometric data. All the compounds were evaluated for their in vitro biological activity against bloodstream forms of and for cytotoxicity against the mammalian cell line L6. Vernodalin () was the most active compound with an IC value of 0.16 µM and a selectivity index of 35. Its closely related congener 11β,13-dihydrovernodalin () registered an IC value of 1.1 µM and a selectivity index of 4.2.
为了从肯尼亚菊科植物中获得新的抗锥虫药物，特别是倍半萜内酯，研究了 Sch. Bip。生物活性导向的分离和结合 LC/MS 基础的去重，导致了 vernodalol () 的鉴定和 vernodalin ()、11β,13-dihydrovernodalin ()、11β,13-dihydrovernolide ()、vernolide ()、11β,13-dihydrohydroxyvernolide ()、hydroxyvernolide () 和一种新的倍半萜内酯 vernocinerascolide () 的分离，它们均来自 叶的二氯甲烷提取物。通过对其 1D 和 2D NMR 光谱和 HR/MS 光谱数据的广泛分析，对化合物 - 进行了表征。所有化合物都针对其对 血红细胞期 的体外生物活性和对哺乳动物细胞系 L6 的细胞毒性进行了评估。vernodalin () 是最具活性的化合物，IC 值为 0.16 µM，选择性指数为 35。其密切相关的同系物 11β,13-dihydrovernodalin () 的 IC 值为 1.1 µM，选择性指数为 4.2。
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