Citotoxic Activity of Extracts and Sesquiterpene Lactones from Stachycephalum argentinum

The extracts and sesquiterpene lactones of S.argentinum were assayed to determine their biological activity on Artemia salina. The most active compound was costunolide (1) with LD50= 62 ppm. Introduction Our previous phytochemical study of Stachychephalum argentinum (Asteraceae), revelead the presence of several skeletal types sesquiterpene lactones [1]. In order to explore new natural bioactive products, we started an study of different extracts from S. argentinum and some of the sesquiterpene lactones isolated, to determine the citotoxic effect against the microorganism Artemia salina (Leach). The Brine Shrimp Bioassay determine that compounds with values of LD50< 1000 ppm could be considered as citotoxic products [2]. Experimental Citotoxic Bioassay against Artemia salina was has been described previously [3]. Results and Discussion Extracts B and C resulted in a marked loss of toxic activity against A. salina. Extract B showed 60% lethality and Extract C showed 33% lethality at 1000 ppm. Active compounds against this organism appeared to be costunolide (1) (100%), 15acetoxycostunolide (2) (60%) and 8-desoxysalonitenolide (3) (100%). Compounds such as the eudesmanolides: 4, 5 and 6 were inactive against A. salina. The most citotoxic compound was costunolide (1) with LD50= 62 ppm. Molecules 2000, 5 434 References and Notes 1. Lactonas sesquiterpénicas de S. argentinum. IV Simposio Internacional Química de Productos Naturales y sus Aplicaciones,1998, Talca, Chile. 2. Meyer, N.; Ferrigni, N.R.; Putnan, J.E.; et al. Planta Médica 1982, 45, 31. 3. Mc Laughlin, J. L.; Colman-Saizarbitoria, T.; Anderson, J.E. Rev.Venezolana de Quimica 1995, 18, 13. O R O R CH3 (1) costunolide CH2OAc (2) 15-acetoxycostunolide CH2OH (3) 8-desoxysalonitenolide (4) santamarin O OH