RESUMO
The antitumor potential of Gymnosperma glutinosum was previously reported using the in vitro and in vivo L5178Y-R lymphoma murine model. The present study was carried out to isolate and identify the cytotoxic compounds present in the Gymnosperma glutinosum leaf hexane extract. Gymnosperma glutinosum was collected in the semi-arid region of Escobedo, State of Nuevo León, México, but it is commonly found in northeastern Mexico; it is traditionally used as a treatment for diarrhea, ulcers and rheumatism. G. glutinosum leaves were extracted with hexane and further fractioned and subfractioned over silica gel by gradient elution with hexane, chloroform, ethyl acetate and methanol. The cytotoxicity of fractions and subfractions was assessed in vitro against L5178Y-R lymphoma cells. Structure elucidation of the active compounds was determined by spectroscopic methods. Fractions and subfractions showed significant (p < 0.05) and concentration-dependent 20% to 56% cytotoxicity against L5178Y-R cells at concentrations ranging from 7.8 µg/mL to 500 µg/mL. The bioassay-guided fractionation of the hexane extract resulted in the isolation and identification of the alkane hentriacontane and the diterpene ent-labd-7-en-13S,14R,15-triol as the metabolites responsible for the activity.
Assuntos
Alcanos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Asteraceae/química , Diterpenos/farmacologia , Linfoma/patologia , Extratos Vegetais/farmacologia , Alcanos/química , Alcanos/isolamento & purificação , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Diterpenos/química , Diterpenos/isolamento & purificação , México , Camundongos , Extratos Vegetais/química , Folhas de Planta/químicaRESUMO
The present study was undertaken to validate the antitumor potential of Gymnosperma glutinosum from regional people's account, using the in vitro and in vivo L5178Y-R lymphoma murine model. Non-polar G. glutinosum crude extracts were tested on L5178Y-R cells. We found significant (p < 0.05) cytotoxic activity (up to 40%) of the hexane extract, which was further fractioned; fraction 1 (F1) was then observed to produce up to 51% apoptosis-mediated L5178Y-R cytotoxicity in vitro at concentrations lower than 0.98 microg/ml, and possess significant in vivo antitumor activity. This study may support further evaluation of active F1 in clinical trials.