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

Abstract

Abstract: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.

Rapid and efficient method for the quantification of lychnopholide in rat plasma by liquid chromatography–tandem mass spectrometry for pharmacokinetic application

“…Distinct sesquiterpene lactones with subtle differences in their chemical structures may be found in 90% of the Eremanthus species, which belongs to the Vernonieae tribe of the Asteraceae family (Sousa et al ., ); this species is widely distributed in the Brazilian Cerrado ecoregion. Their extracts have been employed in traditional medicine to treat wounds, pain and inflammation (Lobo et al ., ). Among the sesquiterpenes lactones, lychnopholide (LYC), whose chemical structure is shown in Fig.…”

High-Resolution α-Glucosidase Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of Antidiabetic Compounds in Eremanthus crotonoides (Asteraceae)

“…The genus Eremanthus Less. comprises 27 species geographically restricted to the Brazillian Cerrado, but there are some exceptions, like E. crotonoides that can also be found in the Restinga [23]. Previous phytochemical analysis of the genus led to identification of flavonoids, quinic acid derivatives, terpenes and sesquiterpene lactones [23][24][25][26][27][28].…”

High-resolution α-glucosidase inhibition profiling combined with HPLC-HRMS-SPE-NMR for identification of anti-diabetic compounds in Eremanthus crotonoides (Asteraceae)

“…comprises 27 species geographically restricted to the Brazillian Cerrado, but there are some exceptions, like E. crotonoides that can also be found in the Restinga [23]. Previous phytochemical analysis of the genus led to identification of flavonoids, quinic acid derivatives, terpenes and sesquiterpene lactones [23][24][25][26][27][28]. Despite the importance of Asteraceae as plant-based remedies for management of diabetes, there are no reports on investigations of the antidiabetic activity of Eremanthus species.…”