1. Anthecularin: a novel sesquiterpene lactone from Anthemis auriculata with antiprotozoal activity
- Author
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Remo Perozzo, Helen Skaltsa, Anthony Linden, Deniz Tasdemir, Reto Brun, and Anastasia Karioti
- Subjects
Models, Molecular ,Stereochemistry ,medicine.drug_class ,Plasmodium falciparum ,Antiprotozoal Agents ,Sesquiterpene lactone ,Crystallography, X-Ray ,Antimalarials ,Lactones ,Ic50 values ,medicine ,Animals ,IC50 ,chemistry.chemical_classification ,biology ,Molecular Structure ,Chemistry ,Organic Chemistry ,Stereoisomerism ,Asteraceae ,Plant Components, Aerial ,biology.organism_classification ,Enzyme ,Antiprotozoal ,Anthemis auriculata ,Anthemis ,Sesquiterpenes ,Anthecularin - Abstract
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.
- Published
- 2007