RESUMEN
Campomanesia adamantium, a native species of the Brazilian Cerrado, is characterized as a natural source of phenolic compounds and has known potential anticancer activities. This study aimed to evaluate the chemical profile of dichloromethane extracts of pulp (DEGPU) and peel (DEGPE) from the fruits of C. adamantium and to identify compounds with antiproliferative effects in vitro against melanoma cells by sulforhodamine B (SRB) assay, apoptosis induction assay, caspase-3 activation assay, nitric oxide (NO) release in coculture of B16-F10 cells and murine peritoneal macrophages. The chemical profiles of DEGPU and DEGPE were analyzed by high performance liquid chromatography coupled to diode array detector and mass spectrometer using the electrospray ionization interface (HPLC-DAD-ESI-MS/MS). Thirteen compounds were identified in both extracts and the chromatographic study of the most active extract in SRB assay DEGPU (GI50 of 16.17 µg/mL) resulted in the isolation of seven compounds. The isolated compound dimethylchalcone (DMC) had the highest antiproliferative activity against B16-F10 with a GI50 of 7.11 µg/mL. DEGPU extract activated caspase-3 in 29% of cells at 25 µg/mL and caused a 50% decrease in NO release in coculture. DEGPU can be characterized as a source of bioactive compounds such as DMC, as seen from its antiproliferative effect in vitro by inducing B16-F10 cells to undergo apoptosis, essential feature in the search for new anticancer drugs.
Asunto(s)
Proliferación Celular/efectos de los fármacos , Chalcona/farmacología , Melanoma/tratamiento farmacológico , Myrtaceae/química , Extractos Vegetales/farmacología , Animales , Apoptosis/efectos de los fármacos , Brasil , Caspasa 3/genética , Caspasa 3/metabolismo , Chalcona/química , Chalcona/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Humanos , Melanoma/fisiopatología , Melanoma Experimental , Ratones , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Espectrometría de Masas en TándemRESUMEN
The bioactive ethyl acetate phase obtained from the latex of Croton urucurana Baillon afforded a novel orbitide (1), [1-9-NαC]-crourorb A1, that proved active against NCI-ADR/RES (ovary, multidrug-resistance phenotype) cells with the same potency as doxorubicin (positive control) and inactive up to the highest concentration tested against nontumor NIH/3T3 cells. The structure elucidation was based on 1D and 2D NMR spectroscopy, further supported by HRESIMS data and by application of Marfey's method for determination of the absolute configuration of its amino acid residues. This is the first orbitide obtained from C. urucurana.