Atividade tripanocida de flavonoides e limonoides isolados de extratos ativos de plantas de Myrsinaceae e Meliaceae

The activity of crude extracts of three Rapanea species (Myrsinaceae) and Cipadessa fruticosa (Meliaceae) was evaluated in vitro against the trypomastigote forms of Trypanosoma cruzi. Thirty-three extracts from different organs of these species were assayed and eleven of them showed significant activity (lysis % >50). The fractionation of an active extract from branches of R. lancifolia (99.5%) led to the isolation of two flavonoids: quercetin and taxifolin, which have weak trypanocidal activity. Additionally, one active extract from fruits of C. fruticosa (97.7%) afforded mexicanolide limonoids: cipadesin, mexicanolide, febrifugin and cipadesin A, that were slightly active on T. cruzi. Moreover, other two flavonoids (flavone and 7-methoxyflavone), previously assayed against T. cruzi, were isolated from the hexane extract from branches of C. fruticosa (100%). The results presented here suggest that the plants evaluated could be a source of new active compounds against T. cruzi.A atividade de extratos brutos de três espécies de Rapanea (Myrsinaceae) e de Cipadessa fruticosa (Meliaceae) foi avaliada in vitro contra formas tripomastigotas de Trypanosoma cruzi. Foram obtidos 33 extratos de diferentes órgãos das espécies estudadas, sendo que onze deles apresentaram atividades significantes (% de lise > 50) nos ensaios realizados. O fracionamento de um extrato ativo dos galhos de R. lancifolia (99,5%) resultou no isolamento de dois flavonoides (quercetina e taxifolina), que apresentaram baixa atividade tripanocida. De um extrato ativo dos frutos de C. fruticosa (97,7%) foram isolados os limonoides mexicanolídeos cipadesina, mexicanolídeo, febrifugina e cipadesina A, que foram moderadamente ativos sobre T. cruzi. Além disso, outros dois flavonoides (flavona e 7-metoxiflavona), previamente ensaiados contra T. cruzi, foram isolados do extrato hexânico dos galhos de C. fruticosa (100%). Os resultados obtidos aqui sugerem que as plantas avaliadas podem constituir fontes de novas substâncias ativas sobre o T. cruzi.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Ensino Superior (CAPES)FINEP - Financiadora de Estudos e Projeto

The compositional landscape of minicircle sequences isolated from active lesions and scars of American cutaneous leishmaniasis

Submitted by sandra infurna ([email protected]) on 2016-07-14T15:41:26Z No. of bitstreams: 1 octavio_fernandes_etal_IOC_2013.pdf: 998508 bytes, checksum: e842184f76aed4b07fa8930601e0bbe3 (MD5)Approved for entry into archive by sandra infurna ([email protected]) on 2016-07-14T15:51:04Z (GMT) No. of bitstreams: 1 octavio_fernandes_etal_IOC_2013.pdf: 998508 bytes, checksum: e842184f76aed4b07fa8930601e0bbe3 (MD5)Made available in DSpace on 2016-07-14T15:51:04Z (GMT). No. of bitstreams: 1 octavio_fernandes_etal_IOC_2013.pdf: 998508 bytes, checksum: e842184f76aed4b07fa8930601e0bbe3 (MD5) Previous issue date: 2013Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Departamento de Imunologia. Laboratório de Imunopatalogia e Biologia Molecular. Recife, PE, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Departamento de Imunologia. Laboratório de Imunopatalogia e Biologia Molecular. Recife, PE, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Departamento de Imunologia. Laboratório de Imunopatalogia e Biologia Molecular. Recife, PE, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Departamento de Imunologia. Laboratório de Imunopatalogia e Biologia Molecular. Recife, PE, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório Interdisciplinar de Pesquisas Médicas. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Departamento de Imunologia. Laboratório de Imunopatalogia e Biologia Molecular. Recife, PE, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório Interdisciplinar de Pesquisas Médicas. Rio de Janeiro, RJ, Brasil.American cutaneous leishmaniasis (ACL) is characterized by cutaneous lesions that heal spontaneously or after specific treatment. This paper reports on the analysis of kDNA minicircle sequences from clinical samples (typical lesions and scars) that were PCR-amplified with specific primers for Leishmania species of the subgenus Viannia

Busca de inibidores da enzima glicossomal gliceraldeído 3-fosfato desidrogenase de Trypanosoma cruzi

The inhibitory activity of crude extracts of Meliaceae and Rutaceae plants on glycosomal glyceraldehyde-3-phosphate dehydrogenase (gGAPDH) enzyme from Trypanosoma cruzi was evaluated at 100 μg/mL. Forty-six extracts were tested and fifteen of them showed significant inhibitory activity (IA % > 50). The majority of the assayed extracts of Meliaceae plants (Cedrela fissilis, Cipadessa fruticosa and Trichilia ramalhoi) showed high ability to inhibit the enzymatic activity. The fractionation of the hexane extract from branches of C. fruticosa led to the isolation of three flavonoids: flavone, 7-methoxyflavone and 3',4',5',5,7-pentamethoxyflavone. The two last compounds showed high ability to inhibit the gGAPDH activity. Therefore, the assayed Meliaceae species could be considered as a promising source of lead compounds against Chagas' disease.Nesse trabalho foi avaliada a atividade inibitória sobre a enzima glicossomal gliceraldeído-3-fosfato desidrogenase de T. cruzi (gGAPDH) de extratos vegetais oriundos de plantas das famílias Meliaceae e Rutaceae, na concentração de 100 μg/mL. Foram testados 46 extratos, dos quais 15 apresentaram atividade inibitória significativa (% AI > 50). A maioria dos extratos de plantas da família Meliaceae (Cedrela fissilis, Cipadessa fruticosa e Trichilia ramalhoi) apresentou grande potencial em inibir a atividade enzimática. O fracionamento do extrato hexânico dos galhos de C. fruticosa permitiu o isolamento de três flavonóides: flavona, 7-metoxiflavona e 3',4',5',5,7-pentametoxiflavona. Os dois últimos foram ativos na inibição da atividade de gGAPDH. Desta forma, as três espécies de Meliaceae testadas podem ser consideradas promissoras na busca de compostos protótipos para o controle da doença de Chagas.Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Coordenação de Aperfeiçoamento de Pessoal de Ensino Superior (CAPES)FINEP - Financiadora de Estudos e Projeto

Nanopartículas de poli-'épsilon'-caprolactona carregadas com hidrocortisona: preparação usando planejamento fatorial e sua avaliação

Polymeric-nanoparticle systems such as nanocapsules and nanospheres have a great potential in applications for nanoencapsulation of corticosteroids which show low solubility in water. The physicochemical characteristics of nanoparticle suspensions are important pre-requisites for the successful development of new dosage form. In this study, hydrocortisone-loaded poly-ε-caprolactone nanoparticles have been prepared by the interfacial deposition method. A 3-factor 2-level factorial design was used to study and optimize nanoparticles formulation. This factorial design was used to study the contrasts and effects of independent variables on particle size distribution, morphology, surface charge, drug content, entrapment efficiency and in vitro drug release profiles. The screened independent variables were: the concentration of hydrocortisone, poly-ε-caprolactone and isodecyl oleate. A High Performance Liquid Chromatography method was developed and validated for hydrocortisone quantification. Special attention was given to both absolute recovery and entrapment efficiency. The results of optimized formulations showed a narrow size distribution with a polydispersity index near to 0.200. The particle sizes were on average 109.2 and 236.5nm to nanospheres and nanocapsules, respectively. In the best formulations the zeta potential was higher than 30 mV (in module) and the absolute recovery and entrapment efficiency were higher 82% and nearly 60%, respectively. The main variables were the quantity of the polymer and of the oil. Nanoparticles observed by the Scanning Electron Microscope depicted extremely spherical shape. In vitro release studies were performed through dialysis with continuous stream. Nanocapsules and nanospheres showed a similar pure diffusion release mechanism according to Korsmeyer-Peppas’s model.CNPqCAPESFAPES

Atividade inseticida de óleos essenciais de Pelargonium graveolens l'Herit e Lippia alba (Mill) N. E. Brown sobre Spodoptera frugiperda (J. E. Smith)

Insecticidal activity of essential oils of Pelargonium graveolens, Lippia alba and compounds geraniol, linalool, 1,8-cineole, limonene, carvone, citral and Azamax® were evaluated against Spodoptera frugiperda. Topical application assay showed essential oil of P. graveolens has acute toxicity against Spodoptera frugiperda larvae (third instar) with LD50 1.13 µg/mg per insect and LD90 2.56 µg/mg per insect. Three essential oils of L. alba also exhibited insecticidal activity with LD50 ranging from 1.20 to 1.56 µg/mg per insect and LD90 from 2.60 to 3.75 µg/mg per insect. Geraniol, linalool, carvone and citral caused significant mortality of 30, 90, 84 and 64% respectively, compared to negative control. The bioinsecticide, Azamax®, caused lower mortality than the compounds of the essential oils

One More Piece in the VACV Ecological Puzzle: Could Peridomestic Rodents Be the Link between Wildlife and Bovine Vaccinia Outbreaks in Brazil?

BACKGROUND: Despite the fact that smallpox eradication was declared by the World Health Organization (WHO) in 1980, other poxviruses have emerged and re-emerged, with significant public health and economic impacts. Vaccinia virus (VACV), a poxvirus used during the WHO smallpox vaccination campaign, has been involved in zoonotic infections in Brazilian rural areas (Bovine Vaccinia outbreaks - BV), affecting dairy cattle and milkers. Little is known about VACV's natural hosts and its epidemiological and ecological characteristics. Although VACV was isolated and/or serologically detected in Brazilian wild animals, the link between wildlife and farms has not yet been elucidated. METHODOLOGY/PRINCIPAL FINDINGS: In this study, we describe for the first time, to our knowledge, the isolation of a VACV (Mariana virus - MARV) from a mouse during a BV outbreak. Genetic data, in association with biological assays, showed that this isolate was the same etiological agent causing exanthematic lesions observed in the cattle and human inhabitants of a particular BV-affected area. Phylogenetic analysis grouped MARV with other VACV isolated during BV outbreaks. CONCLUSION/SIGNIFICANCE: These data provide new biological and epidemiological information on VACV and lead to an interesting question: could peridomestic rodents be the link between wildlife and BV outbreaks

Improved Canine and Human Visceral Leishmaniasis Immunodiagnosis Using Combinations of Synthetic Peptides in Enzyme-Linked Immunosorbent Assay

Visceral leishmaniasis is endemic in many areas of tropical and subtropical America where it constitutes a significant public health problem. It is usually diagnosed by enzyme-linked immunosorbent assays (ELISA) using crude Leishmania antigens, but a variety of other immunological methods may also be applied. Although these approaches are useful, historically their sensitivity and specificity have often been compromised by the use of complex mixtures of antigens. In this context, the use of combinations of purified, well-characterized antigens appears preferable and may yield better results. In the present study, combinations of peptides derived from the previously described Leishmania diagnostic antigens A2, NH, LACK and K39 were used in ELISA against sera from 106 dogs and 44 human patients. Improved sensitivities and specificities, close to 100%, for both sera of patients and dogs was observed for ELISA using some combinations of the peptides, including the detection of VL in dogs with low anti-Leishmania antibody titers and asymptomatic infection. So, the use of combinations of B cell predicted synthetic peptides derived from antigens A2, NH, LACK and K39 may provide an alternative for improved sensitivities and specificities for immunodiagnostic assays of VL