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Métodos Terapéuticos y Terapias MTCI
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1.
Nat Prod Res ; 26(4): 364-9, 2012.
Artículo en Inglés | MEDLINE | ID: mdl-21432719

RESUMEN

Luehea candicans Mart. et Zucc. (Tiliaceae) is known as 'açoita-cavalo' and is one of the most important medicinal plants found in the Brazilian cerrado. The crude methanolic extracts of the branches and leaves and their fractions were evaluated using the following cancer cell lines: MCF-7 (breast), NCI-ADR (breast expressing the multidrug resistance phenotype), NCI-460 (lung), UACC-62 (melanoma), 786-0 (kidney), OVCAR (ovarian), PCO-3 (prostate), HT-29 (colon) and K-562 (leukaemia). The crude methanolic extracts from the branches (B) and leaves (L) were able to inhibit the growth of the K-562 and 786-0 cell lines in a dose-dependent manner, with GI(50) values of 8.1 and 5.4 µg mL(-1), respectively. The hexane (L1), chloroform (L2) and methanol (L4) fractions derived from extract L showed a high selectivity and pronounced cytostatic activity against 786-0 (GI(50) ~ 40 µg mL(-1)). A significant amount of lupeol was isolated from fraction L2. The chloroform (B2) and methanol (B3) fractions derived from extract (B) exhibited less selectivity, showing the highest cytostatic activity against K-562, NCI-ADR, OVCAR, MCF-7 and NCI-460 cells, with GI(50) values between 27 and 40 µg mL(-1). Lupeol, betulin, a mixture of steroids, (-)-epicatechin, vitexin and liriodendrin were isolated from these active fractions.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Malvaceae/química , Extractos Vegetales/farmacología , Plantas Medicinales/química , Antineoplásicos Fitogénicos/química , Brasil , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/patología , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Células HT29/efectos de los fármacos , Humanos , Células K562/efectos de los fármacos , Masculino , Neoplasias Ováricas/tratamiento farmacológico , Neoplasias Ováricas/patología , Triterpenos Pentacíclicos/aislamiento & purificación , Hojas de la Planta/química , Neoplasias de la Próstata/tratamiento farmacológico , Neoplasias de la Próstata/patología
2.
Phytother Res ; 24(3): 379-83, 2010 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-19653314

RESUMEN

The antiproliferative activity of two prenylated benzophenones isolated from Rheedia brasiliensis, the triprenylated garciniaphenone and the tetraprenylated benzophenone 7-epiclusianone, was investigated against human cancer cell lines. The antiproliferative activity on melanoma (UACC-62), breast (MCF-7), drug-resistant breast (NCI-ADR), lung/non-small cells (NCI460), ovarian (OVCAR 03), prostate (PC03), kidney (786-0), lung (NCI-460) and tongue (CRL-1624 and CRL-1623) cancer cells was determined using spectrophotometric quantification of the cellular protein content. The effect of these benzophenones on the activity of cathepsins B and G was also investigated. Garciniaphenone displayed cytostatic activity in all cell lines, whereas 7-epiclusianone showed a dose-dependent cytotoxic effect. The IC(50) values for cell proliferation revealed that 7-epiclusianone is more active than garciniaphenone against most of the cell lines. Furthermore, the antiproliferative effects demonstrated by garciniaphenone and 7-epiclusianone were related to their cathepsin inhibiting properties. In conclusion, 7-epiclusianone is a promising naturally occurring agent which displays multiple inhibitory effects which may be working in concert to inhibit cancer cell proliferation in vitro. The putative pathway by which 7-epiclusianone affects cancer cell development may involve cathepsin inhibition.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Benzofenonas/farmacología , Benzoquinonas/farmacología , Catepsinas/metabolismo , Clusiaceae/química , Extractos Vegetales/farmacología , Catepsinas/antagonistas & inhibidores , Línea Celular Tumoral , Proliferación Celular , Inhibidores Enzimáticos/farmacología , Humanos , Concentración 50 Inhibidora , Estructura Molecular
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