Antiproliferative activity of Eremanthus crotonoides extracts and centratherin demonstrated in brain tumor cell lines

• Published in: Revista brasileira de farmacognosia Vol. 22; no. 6; pp. 1295 - 1300
• Main Authors: Lobo, Jonathas F. R., Castro, Elaine S., Gouvea, Dayana R., Fernandes, Caio P., Almeida, Fernanda B. de, Amorim, Lídia M. F. de, Burth, Patrícia, Rocha, Leandro, Santos, Marcelo G., Harmerski, Lidilhone, Lopes, Norberto P., Pinto, Angelo C.
• Format: Journal Article
• Language: English
• Published: Sociedade Brasileira de Farmacognosia 01.12.2012
• Subjects: PHARMACOLOGY & PHARMACY; centratherin; Eremanthus crotonoides; glioblastoma; sesquiterpene lactones; cytotoxic; Asteraceae
• ISSN: 0102-695X; 1981-528X
• DOI: 10.1590/S0102-695X2012005000131

The genus Eremanthus is recognized by the predominance of sesquiterpene lactones from the furanoheliangolide type, a class of substances extensively tested against cancer cell lines. Thus, the species E. crotonoides (DC.) Sch. Bip., Asteraceae, obtained on "restinga" vegetation was evaluated against U251 and U87-MG glioma cell lines using the MTT colorimetric assay. Dichloromethane fraction was cytotoxic to both glioblastoma multiforme cell lines. We then conducted UPLC-PDA-ESI-MS/MS analysis of the dichloromethane fraction, which allowed the identification of the sesquiterpene lactones centratherin and goyazensolide. The isolation of centratherin was performed using chromatographic techniques and the identification of this substance was confirmed according to NMR data. Cytotoxic activity of centratherin alone was also evaluated against both U251 and U87-MG cells, which showed IC50 values comparable with those obtained for the commercial anticancer drug doxorubicin. All the tested samples showed cytotoxic activity against glioblastoma multiforme cells which suggests that E. crotonoides extracts may be important sources of antiproliferative substances and that the centratherin may serve as prototype for developing new antiglioblastoma drugs.