RESUMO
The aim of this study was to evaluate the cytotoxic potential of Aristolochia foetida Kunth. Stems and leaves of A. foetida Kunth (Aristolochiaceae) have never been investigated pharmacologically. Recent studies of species of the Aristolochiaceae family found significant cytotoxic activities. Hexane, dichloromethane, ethyl acetate and methanol extracts were analyzed by 1H NMR and GC-MS to know the metabolites in each extract. In GC-MS analysis, the main compounds were methyl hexadecanoate (3); hexadecanoic acid (4); 2-butoxyethyl dodecanoate (9); ethyl hexadecanoate (20); methyl octadeca-9,12,15-trienoate (28) and (9Z,12Z,15Z)-octadeca-9,12,15-trienoic acid (40). The results showed a significant reduction in cell viability of the MCF-7 (breast cancer) cell line caused by organic extracts in a dose-dependent manner. The cytotoxicity activity of the dichloromethane extract from the stems (DSE) showed IC50 values of 45.9 µg/mL and the dichloromethane extract of the leaves (DLE) showed IC50 values of 47.3 µg/mL. DSE and DLE had the highest cytotoxic potential in an in vitro study against the MCF-7 cell line and non-tumor cells obtained from the bovine mammary epithelial (bMECs). DSE and DLE induced a loss in mitochondrial membrane potential (ΔΨm) and can cause cell death by apoptosis through the intrinsic pathway in the MCF-7 cell line. DSE and DLE are cytotoxic in cancer cells and cause late apoptosis. Higher concentrations of DSE and DLE are required to induce a cytotoxic effect in healthy mammary epithelial cells. This is the first report of the dichloromethane extract of A. foetida Kunth that induces late apoptosis in MCF-7 cancer cells and may be a candidate for pharmacological study against breast cancer.
RESUMO
The in vitro genotoxic effects of organic and water-soluble fractions of airborne particulate matter (PM10) with the cytokinesis blocked micronucleus (MN) test in human alveolar carcinoma cells A549 were investigated. Samples were collected in three different sites of São Paulo State, Brazil, and fifteen soluble metals and the sixteen EPÁs priority polycyclic aromatic hydrocarbons (PAH) were chemically determined. PAHs prevailing were fluoranthene and benzo(ghi)perylene. In the water-soluble extracts, highest concentration of metals was found for zinc, iron, and copper in all places of collection. Although PM10 concentration in all samples was in the range of 33.5-110.1µg/m3, lower than 120µg/m3 (limit established by São Paulo State's legislation for PM10 in 24h), MN results showed that of the 24 samples analyzed, five organic and seven water-soluble extracts presented a significant increase in MN frequency. The frequency of MN correlates with the total PAH concentration of the three sites investigated, and the concentration of PM10 is correlated with the biological effect in two of them. For the water-soluble fraction, all the sites presented a relation between the PM10 concentration and the MN frequency. Again, the genotoxic response showed a correlation with the total concentration of water-soluble metals in two of the three sites. Our results confirm the importance of the soluble fraction of PM10 to the genotoxic effect of airborne PM even at low concentration of water-soluble compounds. Thus, together with chemical analysis, the implementation of the MN protocol for both organic and water-soluble fraction biological monitoring could be used as a strategy in a routine air-quality monitoring program, complementing other usual analyses for air pollution control and protection of populations.
Assuntos
Células Epiteliais/efeitos dos fármacos , Pulmão/efeitos dos fármacos , Material Particulado/efeitos adversos , Material Particulado/química , Água/química , Células A549 , Poluentes Atmosféricos/efeitos adversos , Brasil , Linhagem Celular Tumoral , Monitoramento Ambiental/métodos , Humanos , Testes para Micronúcleos/métodos , Mutagênicos/efeitos adversos , Mutagênicos/química , Tamanho da Partícula , Hidrocarbonetos Policíclicos Aromáticos/efeitos adversos , Hidrocarbonetos Policíclicos Aromáticos/químicaRESUMO
The toxicity of organic plant extracts to Sitophilus zeamais Motschulsky (Coleoptera: Curculionidae) was assessed for three tropical plant species: branches, leaves, and seeds of Annona montana (Annonaceae), branches of Aristolochia paulistana (Aristolochiaceae), and leaves and branches of Casearia sylvestris (Salicaceae). The screening assay resulted that the extracts of A. montana seeds obtained with hexane (LC50 = 534.75 mg kg(-1) and LT50 = 6.10 days) and with dichloromethane (LC50 = 424.67 mg kg(-1) and LT50 = 5.03 days) were the most promising treatments, followed by the extract prepared from A. montana leaves with hexane (LC50 = 837.70 mg kg(-1) and LT50 = 4.90 days). Moreover, extracts (at 1,500 mg kg(-1)) prepared from C. sylvestris branches with dichloromethane and A. paulistana with hexane caused significant mortality (37% and 41.5%, respectively) beyond sublethal effects on S. zeamais. Therefore, based on the biological assays, extraction yield, and evaluation of the chromatographic profile of the crude extracts by TLC, the hexane extract of A. montana seeds was selected and fractioned using liquid-liquid partitioning. The hydroalcoholic fraction caused mortality of 55.5%, significantly superior to dichloromethane fraction, which caused 35.5% of mortality. Chemical analyses ((1)H NMR, HPLC, and TLC) were performed, and the results showed the presence of alkaloids and acetogenins in both active fractions, which have been associated with bioactivity. Therefore, extracts prepared from A. montana seeds (especially) is an interesting source of new compounds with promising grain-protectant properties.
Assuntos
Besouros , Controle Biológico de Vetores , Extratos Vegetais/farmacologia , Animais , Annona , Grão Comestível , Inseticidas , GorgulhosRESUMO
Anti-fungi activity of organic extracts from the tree Fagara monophylla (Rutaceae) in Venezuela. The tree Fagara monophylla ranges throughout Tropical America. The genus Fagara has a diversity of alkaloid compounds with antibiotic properties; nevertheless, there are few reports antifungal activity of its organic compounds. Organic extracts from Venezuelan F. monophylla were tested for antimicrobial activity against Aspergillus terreus, A. flavus, Penicillium digitatum, P. funiculosum, P. citrinum, Paecilomyces and Candida albicans. Minimal Inhibitory Concentration (MIC) was determined. The susceptibility trials of organic fractions (Hex., CH2Cl2 and MeOH) showed that the highest inhibition was presented by MeOH against A. flavus (55 mm), P. digitatum (60 mm), P. funiculosum (56 mm) and C. albicans (26 mm). The activities of MeOH/EtOAc fractions 1 and 2 suggest a combined effect against A. flavus, P. digitatum and P. funiculosum. The MIC of 1 MeOH/ EtOAc subfraction activity was lower against C. albicans (32 µg/ml) and moderate (128 µg/ml) against P. digitatum. This organic extract has a great antifungal potential. The phytochemical proves and TLC testing on the organic extract, and the MeOH/EtOAc subfraction, respectively, indicated the presence of alkaloid compounds. Rev. Biol. Trop. 55 (3-4): 767-775. Epub 2007 December, 28.
Fagara monophylla está distribuida en América Tropical. El género Fagara tiene diversidad de compuestos alcaloides con propiedades antibacterianas; sin embargo existe escasa información acerca de su actividad antifúngica. Evaluamos extractos de F. monophylla in vitro con los hongos Aspergillus terreus, A. flavus, Penicillium digitatum, P. citrinum, P. funiculosum, Paecilomyces y Candida albicans determinando la Concentración Mínima Inhibitoria (CMI). Hicimos pruebas de susceptibilidad con las fracciones Hex., CH2Cl2 y la MeOH. La mayor inhibición la presentó la fracción MeOH frente a A. flavus (55 mm), P. digitatum (60 mm), P. funiculosum (56 mm) y C. albicans (26 mm). Las actividades mostradas por las fracciones 1 y 2 de MeOH/EtOAc sugieren la acción de un efecto combinado frente a A flavus, P, digitatum y P. funiculosum. La CMI de la subfracción 1 MeOH/EtOAc frente a Candida albicans fue baja (32 µg/ml), y para P. digitatum la CMI fue moderada (128 µg/ml). Este extracto orgánico posee gran potencial de actividad antifúngica. Las pruebas fitoquímicas y los ensayos realizados por TLC al extracto orgánico y a la subfracción 1 MeOH/EtOAc, respectivamente, mostraron la presencia de alcaloides.
Assuntos
Antifúngicos/farmacologia , Fungos Mitospóricos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Rutaceae/química , Testes de Sensibilidade Microbiana , VenezuelaRESUMO
The effect of the ethyl acetate extract of leaves and branches of Trichilia pallida was evaluated (at 0.001%) on larvae of S. frugiperda, fed on leaves of the corn genotypes 'Zapalote Chico', 'CMS 14C' and 'ESALQ-PB-4', considered resistant to this pest, and the susceptible genotype 'Piranão'. The parameters evaluated were length, weight and viability of larval and pupal stages. The extract increased the length of the larval stage, and larval and pupal weight, while resistant genotypes only reduced the pupal weight, did however not confirm the resistant behaviour. There was no interaction between genotype and extract.
Avaliou-se o efeito do extrato acetato de etila obtido de folhas e ramos de Trichillia pallida, (a 0,001%), sobre o desenvolvimento de Spodoptera frugiperda alimentada com folhas de quatro genótipos de milho, um suscetível, 'Piranão', e três resistentes, 'CMS 14C', 'Zapalote Chico', 'ESALQ-PB-4', à referida praga. Os parâmetros biológicos avaliados foram peso, duração e viabilidade das fases larval e pupal. Verificou-se que o extrato provocou alongamento da fase larval e redução dos pesos larval e pupal e que os genótipos resistentes não confirmaram esse comportamento pois quando comparados ao genótipo suscetível, apenas reduziram o peso pupal. Não houve interação significativa entre os fatores genótipo e extrato.
RESUMO
The effect of the ethyl acetate extract of leaves and branches of Trichilia pallida was evaluated (at 0.001%) on larvae of S. frugiperda, fed on leaves of the corn genotypes 'Zapalote Chico', 'CMS 14C' and 'ESALQ-PB-4', considered resistant to this pest, and the susceptible genotype 'Piranão'. The parameters evaluated were length, weight and viability of larval and pupal stages. The extract increased the length of the larval stage, and larval and pupal weight, while resistant genotypes only reduced the pupal weight, did however not confirm the resistant behaviour. There was no interaction between genotype and extract.
Avaliou-se o efeito do extrato acetato de etila obtido de folhas e ramos de Trichillia pallida, (a 0,001%), sobre o desenvolvimento de Spodoptera frugiperda alimentada com folhas de quatro genótipos de milho, um suscetível, 'Piranão', e três resistentes, 'CMS 14C', 'Zapalote Chico', 'ESALQ-PB-4', à referida praga. Os parâmetros biológicos avaliados foram peso, duração e viabilidade das fases larval e pupal. Verificou-se que o extrato provocou alongamento da fase larval e redução dos pesos larval e pupal e que os genótipos resistentes não confirmaram esse comportamento pois quando comparados ao genótipo suscetível, apenas reduziram o peso pupal. Não houve interação significativa entre os fatores genótipo e extrato.