Karioti Anastasia, Skaltsa Helen, Linden Anthony, Perozzo Remo, Brun Reto, Tasdemir Deniz
Department of Pharmacognosy and Chemistry of Natural Products, School of Pharmacy, University of Athens, 157 71 Athens, Greece.
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。
