RESUMO
It is aimed to investigate the cytotoxic effects of the various extracts from the leaf and seed of Centaurea derderiifolia on the growth human cervical adenocarcinoma (HeLa) cells by xCELLigence method and to isolate the cytotoxic constituents. The results showed that subfractions 2 and 3 exhibited remarkable inhibitory effect against HeLa (IC50 < 10 µg/mL). The chloroform extract of leaf displayed the highest cytotoxic effect on HeLa cells (IC50 < 50 µg/mL) and was therefore subjected to a bioassay-guided multistep separation procedure. The pure compounds were elucidated by spectroscopic and mass-spectrometric analyses, including 1 D-, 2 D-NMR. In addition to cytotoxic effects of the isolated constituents, their antioxidant activities were also studied. On the other hand, subfraction 4 exhibited the highest DPPH radical scavenging activity (IC50 = 0.76 ± 0.03 mg/mL). ß-sitosterol-3-O-ß-d-glucopyranoside was isolated for the first time from this plant and three compounds from the bioactive subfractions were identified.
Assuntos
Antioxidantes/farmacologia , Centaurea/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Morte Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Impedância Elétrica , Células HeLa , Humanos , Espectroscopia de Prótons por Ressonância MagnéticaRESUMO
The aim of this study was to examine the anticancer activities and phytochemical profiles of Dicranum scoparium against HeLa cell lines. The bio-guided fractionation studies of dichloromethane extract have high antiproliferative activities. Fractions 7, 9, 19, 20 are rich source of unsaturated fatty acids, and- in the case of Fr-19 may improve the antiproliferative activities as well as increase the unsaturated fatty acid content. The effect of proliferative activities in hexane extract can be attributed to the saturated fatty acid composition of D. scoparium. The Fr-9 exhibited strong antiproliferative activity at concentrations of 100 and 50 µg mL(-1) compared to 5-FU. The fractions of 7, 9, 19 and 20 from dichloromethane extracts exhibited antiproliferative activities at a concentration of 100 µg mL(-1). The HPLC-TOF/MS studies gave nine compounds from the most active fraction of dichloromethane at concentrations of 250 and 100 µg mL(-1). The lower activities were obtained from the fractions including steroid derivatives.
Assuntos
Briófitas/química , Compostos Orgânicos Voláteis/farmacologia , Proliferação de Células/efeitos dos fármacos , Cromatografia Gasosa , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Células HeLa , Humanos , Espectrometria de Massas , Estrutura Molecular , Extratos Vegetais/química , Relação Estrutura-Atividade , Compostos Orgânicos Voláteis/química , Compostos Orgânicos Voláteis/isolamento & purificaçãoRESUMO
BACKGROUND: A detailed phytochemical analysis of Origanum vulgare L. ssp. viride (Boiss.) Hayek was carried out and the antioxidant activities of five different crude extracts were determined. The antiproliferative activities of the extracts were determined using the xCELLigence system (Real Time Cell Analyzer). RESULTS: Differences between the essential oil and volatile organic compound profiles of the plant were shown. The main component of the essential oil was caryophyllene oxide, while the main volatile organic compounds were sabinene and eucalyptol as determined by HS-GC/MS. Phenolic contents of the extracts were determined qualitatively and quantitatively by HPLC/TOF-MS. Ten phenolic compounds were found in the extracts from O. vulgare and Origanum acutidens: rosmarinic acid (in highest abundance), chicoric acid, caffeic acid, p-coumaric acid, gallic acid, quercetin, apigenin-7-glucoside, kaempferol, naringenin and 4-hydroxybenzaldehyde. CONCLUSION: This study provides first results on the antiproliferative and antioxidant properties and detailed phytochemical screening of O. vulgare ssp. viride (Boiss.) Hayek.