Department of Pharmaceutical Biology, University of Basel , Klingelbergstrasse 50, 4056 Basel, Switzerland.
Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute , Socinstrasse 57, 4000 Basel, Switzerland.
J Nat Prod. 2017 Feb 24;80(2):459-470. doi: 10.1021/acs.jnatprod.6b00980. Epub 2017 Jan 24.
A dichlomethane extract of Anthemis nobilis flower cones showed promising in vitro antiprotozoal activity against Trypanosoma brucei rhodesiense and Leishmania donovani, with IC values of 1.43 ± 0.50 and 1.40 ± 0.07 μg/mL, respectively. A comprehensive profiling of the most active fractions afforded 19 sesquiterpene lactones, including 15 germacranolides, two seco-sesquiterpenes, one guaianolide sesquiterpene lactone, and one cadinane acid. Of these, 13 compounds were found to be new natural products. The compounds were characterized by extensive spectroscopic data analysis (1D and 2D NMR, HRMS, circular dichroism) and computational methods, and their in vitro antiprotozoal activity was evaluated. The furanoheliangolide derivative 15 showed high potency and selectivity in vitro against T. b. rhodesiense bloodstream forms (IC 0.08 ± 0.01 μM; SI 63). In silico calculations were consistent with the drug-like properties of 15.
黄花蒿花穗的二氯甲烷提取物对布氏冈比亚锥虫和杜氏利什曼原虫表现出有前景的体外抗原生动物活性，IC 值分别为 1.43 ± 0.50 和 1.40 ± 0.07 μg/mL。对最活跃的馏分进行全面分析，得到了 19 种倍半萜内酯，包括 15 种大根香叶烯内酯、2 种倍半萜烯、1 种愈创木烷型倍半萜内酯和 1 种卡丹烷酸。其中，有 13 种化合物被发现为新的天然产物。这些化合物通过广泛的光谱数据分析（1D 和 2D NMR、高分辨质谱、圆二色性）和计算方法进行了表征，并评估了它们的体外抗原生动物活性。呋喃海良醇内酯衍生物 15 对布氏冈比亚锥虫血流形式表现出高活性和选择性（IC 0.08 ± 0.01 μM；SI 63）。计算符合 15 的类药性。
