RESUMEN
CONTEXT: Cucurbitacins are a group of triterpenoids that have a cucurbitane skeleton with a wide range of biological activities. OBJECTIVES: This study evaluated the anticancer properties of one cucurbitacin isolated from Cayaponia racemosa Cong. (Cucurbitaceae), 2ß,3ß,16α,20(R),25-pentahydroxy-22-oxocucurbita-5-en (1), with in vitro and in vivo models. MATERIALS AND METHODS: In vitro cytotoxic activity was determined with human leukemia (HL60) and normal blood cells (PBMC). Sarcoma 180 was used as in vivo model. RESULTS: The cucurbitacin (1) reduced the number of viable cells; however, there was no changed in the number of non-viable cells at 5 µg/mL. Selectivity towards cancer cells was suggested by the absence of activity on normal proliferating lymphocytes at the concentrations tested (IC50 >25 µg/ml). Morphological analysis of compound 1-treated cells showed typical apoptotic features, such as intense deposition of granules in the cytoplasm (eosinophilia), DNA fragmentation and irregularities in the plasma membrane. In addition, the cells treated with compound 1 presented intense vacuolization and disruption of the plasma membrane. Acridine orange/Ethidium bromide staining confirmed these findings, revealing an increased number of apoptotic cells. In the Sarcoma 180 tumor model, compound 1 showed 52 and 62% of antitumor activity, either alone (25 mg/kg/day) or in association with the chemotherapeutic agent 5-FU (10 + 10 mg/kg/day), respectively. Moreover, either alone or associated with 5-FU, treatment with compound 1 caused an increase in spleen weight and morphological alterations related to immunostimulatory properties. CONCLUSION: These data indicate that these naturally occurring compounds have anticancer potential.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Cucurbitaceae , Leucemia Promielocítica Aguda/patología , Sarcoma 180/tratamiento farmacológico , Triterpenos/farmacología , Adolescente , Adulto , Animales , Antibióticos Antineoplásicos/farmacología , Antimetabolitos Antineoplásicos/farmacología , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/toxicidad , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Forma de la Célula/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Cucurbitaceae/química , Relación Dosis-Respuesta a Droga , Doxorrubicina/farmacología , Fluorouracilo/farmacología , Células HL-60 , Humanos , Concentración 50 Inhibidora , Leucocitos Mononucleares/efectos de los fármacos , Ratones , Plantas Medicinales , Sarcoma 180/patología , Factores de Tiempo , Triterpenos/aislamiento & purificación , Triterpenos/toxicidad , Carga Tumoral/efectos de los fármacos , Adulto JovenRESUMEN
A new indole alkaloid of the pyridocarbazole type, named 6N-hydroxy-olivacine, and two known compounds, 2N-oxide-olivacine and olivacine, were isolated from roots of Peschiera affinis. The structures of the compounds were determined by spectroscopic {IR and extensive NMR (COSY, HMQC, HMBCand NOESY)} and EIMS analysis.
Asunto(s)
Apocynaceae/química , Alcaloides Indólicos/química , Espectroscopía de Resonancia Magnética , Estructura Molecular , Espectrometría de Masa por Ionización de ElectrosprayRESUMEN
Uma análise dos componentes da água-de-coco (Cocos nucifera L.) de duas variedades da fruta (verde e amarelo) por hidrodestilação e extração com solvente, mostrou a presença de álcoois, cetonas, tióis, ácidos carboxílicos, fenóis, e ésteres. Significativa atividade antioxidante foi observada, usando o método DPPH, para as amostras obtidas por hidrodestilação e extração de éter de petróleo para ambas as variedades do coco.
An analysis of the constituents of coconut (Cocos nucifera L.) water from two fruit varieties (green and yellow) by hydrodistillation and solvent extraction showed the presence of alcohols, ketones, thiols, carboxylic acids, phenols, and esters. Substantial antioxidant activity was observed, using the DPPH assay, for the samples obtained by hydrodistillation and petroleum ether extraction of both coconut varieties.
RESUMEN
Isocatalpanol and tecomaquinone I were obtained from roots of Lippia sidoides, a medicinal plant from northeast Brazil. Reduction of tecomaquinone I with NaBH4 yielded a new derivative. Structural elucidation was done on the basis of spectral data, mainly by high-field NMR and electron ionization mass spectrometry.