Cytotoxic effect of a natural sesquiterpenlactone and derivatives against human tumor cells lines

BEER, M. F.; SULSEN, V.; RETA, G. F.; MARTINO V.; DONADEL O. J.

Estancia Grande

Congreso; XXXII Anual Meeting, Sociedad de Biología de Cuyo; 2014

Cancer is one of the most important causes of death worldwide. Chemotherapy is one of the best options in the treatment of cancer.However, currently used drugs have serious side effects. Sesquiterpenlactones (STLs) have received considerable attention due to theirantitumoral activity. In this sense, the aim of the present study was to evaluate the effect of cumanin, a natural STL, and four of itsderivatives on three human tumor cell lines. The sylilated derivatives were synthesized using trimethylchlorosilane,dimethylisopropylchlorosilane and terbuthyldiphenylchlorosilane, using imidazol as a catalitic converter. The acetate derivative wassynthesized using acetic anhydride and pyridine. The human tumor cell lines were maintained in 25 cm culture flasks in RPMI 1640medium supplemented with inactivated fetal calf serum and 2mM L-glutamine at 37ºC in a 5% CO2, 95% humidified air incubator.Chemosensitivity tests were performed using the SRB assay of the NCI. Each agent was tested in triplicates at different dilutions in therange 1-100μm. Cumanin was active with GI50 values between 24 and 32μM, whereas for the most active sylilated and acetatederivative, GI50 values were lower than 5μM. This study demonstrates the importance of natural products in the search of newantitumor agents and suggests that the development of cumanin derivatives could be used for therapeutic application.