耳状母菊素：一种来自耳状母菊的具有抗原生动物活性的新型倍半萜内酯。
Anthecularin: a novel sesquiterpene lactone from Anthemis auriculata with antiprotozoal activity.
作者信息
Karioti Anastasia, Skaltsa Helen, Linden Anthony, Perozzo Remo, Brun Reto, Tasdemir Deniz
机构信息
Department of Pharmacognosy and Chemistry of Natural Products, School of Pharmacy, University of Athens, 157 71 Athens, Greece.
出版信息
J Org Chem. 2007 Oct 12;72(21):8103-6. doi: 10.1021/jo701751w. Epub 2007 Sep 20.
Anthecularin (1), a minor sesquiterpene lactone with a novel ring system was isolated from Greek Anthemis auriculata (Asteraceae). Its structure was elucidated by means of NMR, HRMS, and X-ray crystallography. Anthecularin showed antitrypanosomal (IC50=10.1 microg/mL) and antiplasmodial activity (IC50=23.3 microg/mL) and inhibited two key enzymes of the plasmodial type II fatty acid biosynthesis pathway, PfFabI and PfFabG (IC50 values=14 and 28.3 microg/mL, respectively). A probable biogenesis of 1 is also proposed and discussed.
从希腊的耳叶春黄菊（菊科）中分离出了一种具有新型环系的次要倍半萜内酯——花药内酯（1）。通过核磁共振（NMR）、高分辨质谱（HRMS）和X射线晶体学确定了其结构。花药内酯显示出抗锥虫活性（半数抑制浓度[IC50]=10.1微克/毫升）和抗疟活性（IC50=23.3微克/毫升），并抑制疟原虫II型脂肪酸生物合成途径的两种关键酶，即恶性疟原虫脂肪酸合成酶I（PfFabI）和恶性疟原虫脂肪酸合成酶G（PfFabG）（IC50值分别为14和28.3微克/毫升）。此外，还提出并讨论了1的一种可能的生物合成途径。
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