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1.
Appl Microbiol Biotechnol ; 101(2): 711-723, 2017 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-27757508

RESUMEN

Actinomycetes are known to produce numerous secondary bioactive metabolites of pharmaceutical interest. The purpose of this study was to isolate, characterize, and investigate the antibacterial, antifungal, and anticancer activities of metabolites produced by Actinobacteria isolated from the rhizosphere of Paullinia cupana. The Actinobacteria was identified as Streptomyces hygroscopicus ACTMS-9H. Based on a bioguided study, the methanolic biomass extract obtained from submerged cultivation had the most potent antibacterial, antifungal, and cytotoxic activities. This extract was partitioned with n-hexane, ethyl acetate, and 2-butanol. Elaiophylin was isolated from the methanolic biomass extract, and its molecular formula was determined (C54H88O18) based on 1H and 13C NMR, IR and MS analyses. The 2-butanol phase was fractionated into four fractions (EB1, EB2A, EB2B, and EB3M). Chemical prospecting indicated the presence of alkaloids, saponins, and reducing sugars in the methanolic extract and 2-butanol phase. The elaiophylin displayed anticancer activity in HEp-2 and HL-60 cells with an IC50 of 1 µg/mL. The EB1 fraction was selectively toxic to HL-60 cells with IC50 of 9 ng/mL. Bioautography showed that the EB1 fraction contained an alkaloid with antibacterial and antifungal activities (MIC values ≤1.9 and <3.9 µg/mL, respectively). In conclusion, the EB1 fraction and elaiophylin of S. hygroscopicus have potent antimicrobial, antifungal, and anticancer activities.


Asunto(s)
Antiinfecciosos/aislamiento & purificación , Antineoplásicos/aislamiento & purificación , Productos Biológicos/aislamiento & purificación , Microbiología del Suelo , Streptomyces/aislamiento & purificación , Streptomyces/fisiología , Antiinfecciosos/química , Antineoplásicos/química , Bacterias/efectos de los fármacos , Productos Biológicos/química , Brasil , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Hongos/efectos de los fármacos , Humanos , Concentración 50 Inhibidora , Pruebas de Sensibilidad Microbiana , Paullinia/crecimiento & desarrollo , Rizosfera , Análisis Espectral , Streptomyces/química , Streptomyces/metabolismo
2.
Int J Mol Sci ; 13(4): 4124-4140, 2012.
Artículo en Inglés | MEDLINE | ID: mdl-22605969

RESUMEN

In the study, we have examined the antitumor and antimicrobial activities of the methanol extract, the fractions, a fraction of total alkaloids and two alkaloids isolated from the stem of Erythroxylum caatingae Plowman. All test fractions, except the hexane fractions, showed antimicrobial activity on gram-positive bacteria and fungi. The acetate: methanol (95:5), acetate, chloroform and hexane fractions show the highest cytotoxicity activity against the NCI-H292, HEp-2 and K562 cell lines using MTT. The absence of hemolysis in the erythrocytes of mice was observed in these fractions and 6ß-Benzoyloxy-3α-(3,4,5- trimethoxybenzoyloxy) tropane (catuabine B). Staining with Annexin V-FITC and JC-1 was used to verify the mechanism of action of the compounds of E. caatingae that showed cytotoxicity less than 30 µg/mL in leukemic cells. After 48 h of incubation, we observed that the acetate: methanol (95:5), acetate, and chloroform fractions, as well as the catuabine B, increased in the number of cells in early apoptosis, from 53.0 to 74.8%. An analysis of the potential of the mitochondrial membrane by incorporation of JC-1 showed that most cells during incubation of the acetate: methanol (95:5) and acetate fractions (63.85 and 59.2%) were stained, suggesting the involvement of an intrinsic pathway of apoptosis.


Asunto(s)
Antiinfecciosos/farmacología , Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Erythroxylaceae/metabolismo , Tallos de la Planta/metabolismo , Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Animales , Antiinfecciosos/aislamiento & purificación , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular , Descubrimiento de Drogas , Eritrocitos/efectos de los fármacos , Femenino , Hongos/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Hemólisis/efectos de los fármacos , Células Hep G2 , Humanos , Leucemia/tratamiento farmacológico , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Ratones , Pruebas de Sensibilidad Microbiana , Membranas Mitocondriales/efectos de los fármacos , Extractos Vegetales/farmacología
3.
Rev. bras. farmacogn ; 18(3): 436-440, jul.-set. 2008. tab
Artículo en Portugués | LILACS | ID: lil-496119

RESUMEN

Lippia alba (Mill.) N. E. Brown (Verbenaceae), amplamente distribuída em todo o território brasileiro, é conhecida popularmente como erva cidreira e utilizada na medicina popular como analgésica, febrífuga, antiinflamatória, antigripal e nas afecções hepáticas. Extratos brutos foram preparados a partir de plantas cultivadas, de modo padronizado, em horta medicinal do Laboratório de Fitoterapia da Empresa Pernambucana de Pesquisa Agropecuária (IPA) para a verificação da atividade antimicrobiana, in vitro, pelo método de difusão em disco de papel. A concentração inibitória mínima (CIM) foi determinada para os extratos que exibiram melhores atividades. Os resultados obtidos mostraram que os extratos clorofórmico, acetônico e etanólico da raiz foram ativos frente a Staphylococcus aureus, Micrococcus luteus, Bacillus subtilis, Mycobacterium smegmatis, Candida albicans e Monilia sitophila e os extratos hexânicos, etanólicos e metanólicos das folhas inibiram S. aureus, M. luteus, B. subtilis, M. smegmatis e M. sitophila. A menor concentração inibitória (CIM = 31,2 µg/mL), foi obtida para o extrato clorofórmico da raiz frente a B. subtilis e M. luteus.


Lippia alba (Mill.) N. E. Brown (Verbenaceae), commonly known as "erva cidreira", is widely distributed throughout Brazil and is used in folk medicine as an analgesic, anti-inflammatory, cold remedy, as well as to reduce fevers and treat hepatic afflictions. Crude extracts of L. alba were prepared from plants cultivated in the medicinal garden of the Laboratório de Fitoterapia of the Empresa Pernambucana de Pesquisa Agropecuária (IPA), State of Pernambuco, Brazil, using standard techniques to test their in vitro antibacterial activity using the paper disk-diffusion method. The minimum inhibitory concentration (MIC) was determined for those extracts demonstrating the highest activity. The results demonstrated that the chloroform, acetone and ethanol extracts of root material were active against the growth of Staphylococcus aureus, Micrococcus luteus, Bacillus subtilis, Mycobacterium smegmatis, Candida albicans and Monilia sitophila, while the hexane, ethanol and methanol extracts of leaves inhibited the growth of S. aureus, M. luteus, B. subtilis, M. smegmatis and M. sitophila. The lowest inhibitory concentration (MIC = 31.2 µg/mL) was obtained with the chloroform root extract against B. subtilis and M. luteus.

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