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Id: biblio-907513
Autor: Vizcaíno-Páez, Samuel; Pineda, Rodrigo; García, Carlos; Gil, Jesús; Durango, Diego.
Título: Metabolism and antifungal activity of safrole, dillapiole, and derivatives against botryodiplodia theobromae and colletotrichum acutatum / Metabolismo y actividad antifúngica de safrol, dilapiol, y derivados contra botryodiplodia theobromae y colletotrichum acutatum
Fonte: Bol. latinoam. Caribe plantas med. aromát;15(1):1-17, ene. 2016. ilus, graf, tab.
Idioma: en.
Projeto: Universidad Nacional de Colombia.
Resumo: The direct in vitro fungitoxicity and metabolism of safrole and dillapiole (isolated from Piper auritum and Piper holtonii, respectively) by Botryodiplodia theobromae and Colletotrichum acutatum were investigated. Higher values of mycelial growth inhibition for both fungi were obtained for dillapiole, as compared with safrole. B. theobromae was able to metabolize both compounds to their respective vicinal diols, reaching 65 percent relative abundance during the biotransformation of dillapiole; while C. acutatum only transformed safrole to various metabolites with relative abundances under 5 percent. According to the low antifungal activity of the major metabolic products (< 5 percent for vicinal diols), a detoxification process was implied. Studies on the influence of some substituents in the aromatic ring of safrole and dillapiole on the antifungal activity against B. theobromae were also carried out. As result, the safrole nitrated derivative, 6-nitrosafrole, showed a fungitoxicity level similar to that displayed by the commercial fungicide Carbendazim® under the conditions used. In light of this, safrole and dillapiole could be suggested as feasible structural templates for developing new antifungal agents.

Se investigó la fungitoxicidad directa in vitro y el metabolismo de safrol y dilapiol (obtenidos desde Piper auritum and Piper holtonii, respectivamente) por Botryodiplodia theobromae y Colletotrichum acutatum. Los valores mayores de inhibición del crecimiento micelial de ambos hongos se obtuvieron para dilapiol, en comparación con safrol. B. theobromae metabolizó ambos compuestos a sus respectivos dioles vecinales, alcanzando abundancias relativas del 65 por ciento durante la biotransformación del dilapiol; mientras que C. acutatum solo transformó safrol en varios metabolitos con abundancias relativas menores al 5 por ciento. De acuerdo con la baja actividad antifúngica de los productos metabólicos mayoritarios (< 5 por ciento para los dioles vecinales), se sugiere un proceso de desintoxicación. Adicionalmente, se evaluó la influencia de algunos sustituyentes en el anillo aromático de safrol y dilapiol sobre la actividad antifúngica contra B. theobromae. Como resultado, el derivado nitrado del safrol, el 6–nitro safrol, presentó un nivel de fungitoxicidad similar al exhibido por el fungicida comercial Carbendazim® bajo las condiciones usadas. A la luz de lo anterior, safrol y dilapiol podrían ser sugeridos como plantillas estructurales adecuadas para el desarrollo de nuevos agentes antifúngicos.
Descritores: Antifúngicos/farmacologia
Dioxóis/farmacologia
Fungos Mitospóricos
Safrol/farmacologia
-Antifúngicos/metabolismo
Biotransformação
Colletotrichum
Dioxóis/metabolismo
Técnicas In Vitro
Safrol/metabolismo
Responsável: CL1.1 - Biblioteca Central


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Id: lil-748267
Autor: Miguel, Tatiana de Á.; Bordini, Jaqueline G.; Saito, Gervásio H.; Andrade, Célia G.T. de J.; Ono, Mario A.; Hirooka, Elisa Y.; Vizoni, Édio; Ono, Elisabete Y.S..
Título: Effect of fungicide on Fusarium verticillioides mycelial morphology and fumonisin B1 production
Fonte: Braz. j. microbiol;46(1):293-299, 05/2015. tab, graf.
Idioma: en.
Resumo: The effect of fludioxonil + metalaxyl-M on the mycelial morphology, sporulation and fumonisin B1 production by Fusarium verticillioides 103 F was evaluated. Scanning electron microscopy analysis showed that the fungicide caused inhibition of hyphal growth and defects on hyphae morphology such as cell wall disruption, withered hyphae, and excessive septation. In addition, extracellular material around the hyphae was rarely observed in the presence of fludioxonil + metalaxyl-M. While promoting the reduction of mycelial growth, the fungicide increased sporulation of F. verticillioides compared to the control, and the highest production occurred on the 14th day in the treatments and on the 10th day in the control cultures. Fumonisin B1 production in the culture media containing the fungicide (treatment) was detected from the 7th day incubation, whereas in cultures without fungicide (control) it was detected on the 10th day. The highest fumonisin B1 production occurred on the 14th day, both for the control and for the treatment. Fludioxonil + metalaxyl - M can interfere in F. verticillioides mycelial morphology and sporulation and increase fumonisin B1 levels. These data indicate the importance of understanding the effects of fungicide to minimize the occurrence of toxigenic fungi and fumonisins.
Descritores: Fumonisinas/metabolismo
Fungicidas Industriais/farmacologia
Fusarium/efeitos dos fármacos
Fusarium/metabolismo
Hifas/efeitos dos fármacos
Hifas/ultraestrutura
-Alanina/análogos & derivados
Alanina/farmacologia
Dioxóis/farmacologia
Fusarium/crescimento & desenvolvimento
Fusarium/ultraestrutura
Hifas/crescimento & desenvolvimento
Microscopia Eletrônica de Varredura
Pirróis/farmacologia
Esporos Fúngicos/crescimento & desenvolvimento
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: BR1.1 - BIREME


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Id: lil-560655
Autor: Aly, Ibrahim RB; Hendawy, Mohamed A; Ali, Eman; Hassan, Eman; Nosseir, Mona MF.
Título: Immunological and parasitological parameters after treatment with dexamethasone in murine Schistosoma mansoni
Fonte: Mem. Inst. Oswaldo Cruz;105(6):729-735, Sept. 2010. tab.
Idioma: en.
Resumo: This work aimed to evaluate the effect of diphenyl dimethyl bicarboxylate (DDB) and dexamethasone alone and in combination with praziquantel on various parasitological, immunological and pathological parameters reflecting disease severity and morbidity in murine schistosomiasis. DDB and dexamethasone had no effect on worm burden but altered tissue egg distribution. This indicates that, under the schedule used, neither drug interfered with the development of adult worms or oviposition, but both can modulate liver pathology. Dexamethasone resulted in a greater reduction in granuloma size than did DDB. Dexamethasone-treated mice also showed lower levels of serum gamma interferon (IFN-γ), interleukin-12 (IL-12) and IL-4, together with higher IL-10 levels, than infected untreated control animals. These data suggest that dexamethasone is a convenient and promising coadjuvant agent that results in decreased morbidity in murine schistosomiasis.
Descritores: Adjuvantes Imunológicos
Anti-Helmínticos
Dexametasona
Dioxóis
Glucocorticoides
Praziquantel
Esquistossomose mansoni
-Adjuvantes Imunológicos
Anti-Helmínticos
Citocinas/sangue
Citocinas/imunologia
Dexametasona
Dioxóis
Quimioterapia Combinada/métodos
Glucocorticoides
Granuloma
Granuloma/patologia
Fígado
Fígado/patologia
Praziquantel
Índice de Gravidade de Doença
Esquistossomose mansoni/imunologia
Esquistossomose mansoni
Esquistossomose mansoni/patologia
Limites: Animais
Masculino
Camundongos
Responsável: BR1.1 - BIREME


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Id: lil-538167
Autor: Waghabi, Mariana C; Coutinho-Silva, Robson; Feige, Jean-Jacques; Higuchi, Maria de Lourdes; Becker, David; Burnstock, Geoffrey; Araújo-Jorge, Tânia C de.
Título: Gap junction reduction in cardiomyocytes following transforming growth factor-â treatment and Trypanosoma cruzi infection
Fonte: Mem. Inst. Oswaldo Cruz;104(8):1083-1090, Dec. 2009. ilus, tab.
Idioma: en.
Projeto: CNPq; . FAPERJ; . PRONEX; . Wellcome Trust.
Resumo: Gap junction connexin-43 (Cx43) molecules are responsible for electrical impulse conduction in the heart and are affected by transforming growth factor-â (TGF-â). This cytokine increases during Trypanosoma cruzi infection, modulating fibrosis and the parasite cell cycle. We studied Cx43 expression in cardiomyocytes exposed or not to TGF-â T. cruzi, or SB-431542, an inhibitor of TGF-â receptor type I (ALK-5). Cx43 expression was also examined in hearts with dilated cardiopathy from chronic Chagas disease patients, in which TGF-â signalling had been shown previously to be highly activated. We demonstrated that TGF-â treatment induced disorganised gap junctions in non-infected cardiomyocytes, leading to a punctate, diffuse and non-uniform Cx43 staining. A similar pattern was detected in T. cruzi-infected cardiomyocytes concomitant with high TGF-â secretion. Both results were reversed if the cells were incubated with SB-431542. Similar tests were performed using human chronic chagasic patients and we confirmed a down-regulation of Cx43 expression, an altered distribution of plaques in the heart and a significant reduction in the number and length of Cx43 plaques, which correlated negatively with cardiomegaly. We conclude that elevated TGF-â levels during T. cruzi infection promote heart fibrosis and disorganise gap junctions, possibly contributing to abnormal impulse conduction and arrhythmia that characterise severe cardiopathy in Chagas disease.
Descritores: Benzamidas/uso terapêutico
Doença de Chagas/metabolismo
/metabolismo
CONNEXIN ABBREVIATIONS AS TOPICABATTOIRS/metabolismo
Dioxóis/uso terapêutico
Junções Comunicantes/metabolismo
Miócitos Cardíacos/química
Receptores de Fatores de Crescimento Transformadores beta/antagonistas & inibidores
Fator de Crescimento Transformador beta/uso terapêutico
-Doença de Chagas/tratamento farmacológico
Imunofluorescência
Junções Comunicantes/efeitos dos fármacos
Imuno-Histoquímica
Microscopia Confocal
Miócitos Cardíacos/efeitos dos fármacos
Miócitos Cardíacos/metabolismo
Limites: Adulto
Animais
Feminino
Humanos
Masculino
Camundongos
Pessoa de Meia-Idade
Responsável: BR1.1 - BIREME


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Id: lil-127825
Autor: Li, Xiao-Yu.
Título: Bioactivity of neolignans from fructus Schizandrae
Fonte: Mem. Inst. Oswaldo Cruz;86(suppl. 2, n.esp):31-7, Oct. 1991. ilus, tab.
Idioma: en.
Conferência: Apresentado em: Brazilian-Sino Symposium on Chemistry and Pharmacology of Natural Products, Rio de Janeiro, Dec. 10-14, 1989.
Resumo: Fructus Schisandrae sinensis Baill, a traditional Chinese medicine, used as tonic and sedative, has been shown at the beginning of 70's to lower the elevated serum glutamic-pyruvic transaminase (SGPT) levels of patients suffering from chronic viral hepatitis. Durign past 20 years, a series of neolignans have been isolated and identified as effective principles. Pharmacological studies revealed that they increased liver protein and glicogen synthesis, antagonized liver injuries from CCl4 and thioacetamide. The mechanism of SGPT lowering was considered as a hepato-protective and membrane stabilize action, although inhibition of the activity of liver GPT may also be existed. It was found that some principles of Schisandrae have an inducing effect on hepatic microsomal drug-metabolizing enzynme system P-450, thus explained their anti-toxic, anti-carcinogenic and anti-mutagenic effects. A synthetic derivative compound of Schisandrin called DDB has most of the above mentioned actions now used widely in Chine as a hepato-protective drug with high effectiveness in normalizing liver functions and very low side effects. From Schisandrin to synthesized DDB, pointed out a successful way in the development of new drugs from natural products
Descritores: Medicamentos de Ervas Chinesas/farmacologia
Lignina/farmacologia
-Alanina Transaminase/efeitos dos fármacos
Dioxóis/farmacologia
Medicamentos de Ervas Chinesas/química
Medicamentos de Ervas Chinesas/uso terapêutico
Fígado
Fígado/metabolismo
Hidrocarbonetos Cíclicos/farmacologia
Lignina/química
Lignina/uso terapêutico
Limites: Humanos
Animais
Responsável: BR1.1 - BIREME



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