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Texto completo SciELO Brasil
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Id: biblio-952842
Autor: Jimenez, Paula Christine; Wilke, Diego Veras; Costa-Lotufo, Leticia Veras.
Título: Marine drugs for cancer: surfacing biotechnological innovations from the oceans
Fonte: Clinics;73(supl.1):e482s, 2018. graf.
Idioma: en.
Resumo: This review will discuss the contributions of marine natural molecules, a source only recently found to have pharmaceutical prospects, to the development of anticancer drugs. Of the seven clinically utilized compounds with a marine origin, four are used for the treatment of cancer. The development of these drugs has afforded valuable knowledge and crucial insights to meet the most common challenges in this endeavor, such as toxicity and supply. In this context, the development of these compounds will be discussed herein to illustrate, with successful examples provided by cytarabine, trabectedin, eribulin and brentuximab vedotin, the steps involved in this process as well as the scientific advances and technological innovation potential associated with developing a new drug from marine resources.
Descritores: Biotecnologia/métodos
Organismos Aquáticos/química
Desenvolvimento de Medicamentos/métodos
Neoplasias/tratamento farmacológico
Antineoplásicos/uso terapêutico
-Oceanos e Mares
Imunoconjugados/uso terapêutico
Descoberta de Drogas
Brentuximab Vedotin
Tipo de Publ: Revisão
Responsável: BR1.1 - BIREME

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Texto completo SciELO Chile
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Id: biblio-950746
Autor: Bae, Seunghee; Lim, Kyung Mi; Cha, Hwa Jun; An, In-Sook; Lee, Jeong Pyo; Lee, Kwang Sik; Lee, Ghang Tai; Lee, Kun Kook; Jung, Ho Jung; Ahn, Kyu Joong; An, Sungkwan.
Título: Arctiin blocks hydrogen peroxide-induced senescence and cell death though microRNA expression changes in human dermal papilla cells
Fonte: Biol. Res;47:1-11, 2014. graf, tab.
Idioma: en.
Projeto: Korean Health Technology R& D Project; . Ministry of Health & Welfare, Republic of Korea.
Resumo: BACKGROUND: Accumulating evidence indicates that reactive oxygen species (ROS) are an important etiological factor for the induction of dermal papilla cell senescence and hair loss, which is also known alopecia. Arctiin is an active lignin isolated from Arctium lappa and has anti-inflammation, anti-microbial, and anti-carcinogenic effects. In the present study, we found that arctiin exerts anti-oxidative effects on human hair dermal papilla cells (HHDPCs). RESULTS: To better understand the mechanism, we analyzed the level of hydrogen peroxide (H2O2)-induced cytotoxicity, cell death, ROS production and senescence after arctiin pretreatment of HHDPCs. The results showed that arctiin pretreatment significantly inhibited the H2O2-induced reduction in cell viability. Moreover, H2O2-induced sub-G1 phase accumulation and G2 cell cycle arrest were also downregulated by arctiin pretreatment. Interestingly, the increase in intracellular ROS mediated by H2O2 was drastically decreased in HHDPCs cultured in the presence of arctiin. This effect was confirmed by senescence associated-beta galactosidase (SA-ß-gal) assay results; we found that arctiin pretreatment impaired H2O2-induced senescence in HHDPCs. Using microRNA (miRNA) microarray and bioinformatic analysis, we showed that this anti-oxidative effect of arctiin in HHDPCs was related with mitogen-activated protein kinase (MAPK) and Wnt signaling pathways. CONCLUSIONS: Taken together, our data suggest that arctiin has a protective effect on ROS-induced cell dysfunction in HHDPCs and may therefore be useful for alopecia prevention and treatment strategies.
Descritores: Envelhecimento/metabolismo
Espécies Reativas de Oxigênio/antagonistas & inibidores
Folículo Piloso/efeitos dos fármacos
-Envelhecimento/efeitos dos fármacos
Regulação para Baixo/efeitos dos fármacos
Regulação para Cima/efeitos dos fármacos
Linhagem Celular
Sobrevivência Celular/efeitos dos fármacos
Morte Celular/efeitos dos fármacos
Folículo Piloso/citologia
Folículo Piloso/metabolismo
Derme/efeitos dos fármacos
Análise de Sequência com Séries de Oligonucleotídeos
MicroRNAs/efeitos dos fármacos
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Peróxido de Hidrogênio/farmacologia
Limites: Humanos
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: CL1.1 - Biblioteca Central

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Texto completo SciELO Brasil
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Id: biblio-886664
Título: Simultaneous Determination of Furan and Vinyl Acetate in Vapor Phase of Mainstream Cigarette Smoke by GC-MS
Fonte: An. acad. bras. ciênc;89(1,supl):383-390, May. 2017. tab, graf.
Idioma: en.
Projeto: National Science Foundation of China; . Henan Science and Technology Innovation Talent Support Program.
Resumo: ABSTRACT A simple and sensitive method for simultaneous determination of furan and vinyl acetate (VA) in vapor phase of mainstream cigarette smoke with cold trap and gas chromatography-mass spectrometry (GC-MS) was developed. A Cambridge filter pad (CFP) was placed in front of the impingers of smoking machine to remove the particle phase from cigarette smoke. Furan and VA in vapor phase of mainstream cigarette smoke were collected in two impingers connected in series by filled with methanol at -78°C. The solutions were added with deuterium-labeled furan-d4 and VA-d6 as internal standards and analyzed by GC-MS. The results showed that the calibration curves for furan and VA were linear (r2 > 0.9995) over the studied concentration range. The intra- and inter-day precision values for furan and VA were <7.07% and <9.62%, respectively. The extraction recoveries of furan and VA were in the range of 94.5-97.7% and 92.3-94.9%, respectively. Moreover, the limits of detection for furan and VA were 0.028 µg mL-1 and 1.3 ng mL-1, respectively. The validated method has been successfully applied to determine the emissions of furan and VA in the vapor phase of mainstream cigarette smoke under International Organization for Standardization (ISO) and Canadian Intense (CI) smoking regimen.
Descritores: Fumaça/análise
Compostos de Vinila/análise
Reprodutibilidade dos Testes
Cromatografia Gasosa-Espectrometria de Massas
Tipo de Publ: Estudo de Validação
Responsável: BR1.1 - BIREME

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Id: biblio-889166
Autor: Li, Yun-Cheng; Gou, Zi-Xi; Zhang, Ying; Xia, Zi-Yuan; Tang, Yue-Qin; Kida, Kenji.
Título: Inhibitor tolerance of a recombinant flocculating industrial Saccharomyces cerevisiae strain during glucose and xylose co-fermentation
Fonte: Braz. j. microbiol;48(4):791-800, Oct.-Dec. 2017. graf.
Idioma: en.
Projeto: National Natural Science Foundation of China; . Talent Project for Science and Technology Innovation of Sichuan Province.
Resumo: ABSTRACT Lignocellulose-derived inhibitors have negative effects on the ethanol fermentation capacity of Saccharomyces cerevisiae. In this study, the effects of eight typical inhibitors, including weak acids, furans, and phenols, on glucose and xylose co-fermentation of the recombinant xylose-fermenting flocculating industrial S. cerevisiae strain NAPX37 were evaluated by batch fermentation. Inhibition on glucose fermentation, not that on xylose fermentation, correlated with delayed cell growth. The weak acids and the phenols showed additive effects. The effect of inhibitors on glucose fermentation was as follows (from strongest to weakest): vanillin > phenol > syringaldehyde > 5-HMF > furfural > levulinic acid > acetic acid > formic acid. The effect of inhibitors on xylose fermentation was as follows (from strongest to weakest): phenol > vanillin > syringaldehyde > furfural > 5-HMF > formic acid > levulinic acid > acetic acid. The NAPX37 strain showed substantial tolerance to typical inhibitors and showed good fermentation characteristics, when a medium with inhibitor cocktail or rape straw hydrolysate was used. This research provides important clues for inhibitors tolerance of recombinant industrial xylose-fermenting S. cerevisiae.
Descritores: Saccharomyces cerevisiae/efeitos dos fármacos
Saccharomyces cerevisiae/crescimento & desenvolvimento
Saccharomyces cerevisiae/genética
Saccharomyces cerevisiae/metabolismo
Microbiologia Industrial
Responsável: BR1.1 - BIREME

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Id: biblio-907482
Autor: Baquero, Eduard; Quiñones, Winston; Franzblau, Scott; Torres, Fernando; Archbold, Rosendo; Echeverri, Fernando.
Título: Furan type lignans with antimycobacterial activity / Lignanos del tipo furano con actividad antimicobacterial
Fonte: Bol. latinoam. Caribe plantas med. aromát;14(3):171-178, mayo 2015. ilus, tab.
Idioma: en.
Resumo: Compounds such as triclosan, diclofenac and trimetropin posses antibacterial activity, including mycobacterial; their structures are based on two aromatic rings joined by a methylene or a heteroatom. Since a similar structural system is found in natural diarylfuran- based lignans, we studied plants known with this type of lignans, as potential active against Mycobacterium tuberculosis. Fractions of the active extracts were tested for anti-TB activity and their chemical constituents analyzed by NMR spectroscopy. Several extracts and chromatographical fractions exhibited > 90 percent inhibition of M. tuberculosis at 128 ug/mL. Methylpluviatilol, a pure compound isolated from Virola sebifera, was active at this concentration.. These findings suggest that plant species of the families here studied may yield novel lead compounds for the development of antimycobacterial agents.

Compuestos tales como triclosan, diclofenac y trimetoprim poseen actividad antibacterial, incluyendo la antimicobacterial; sus estructuras están basadas en dos anillos aromáticos unidos por un metileno o un heteroátomo. Debido a que en la naturaleza se encuentra un sistema estructural similar del tipo diarilfurano en los lignanos, así como otros subtipos, nosotros estudiamos plantas contra Mycobacterium tuberculosis, de las que se sabe contienen lignanos Las fracciones cromatográficas de los extractos activos fueron ensayadas para actividad anti.Tb y sus constituyentes químicos se analizaron por espectroscopía de RMN. Varios extractos y fracciones cromatográficas exhibieron una inhibición superior al 90 por ciento a 128 ug/mL; el compuesto metilpluviatilol, aislado de mostró una inhibición del 99 por ciento a esa concentración. Esos hechos sugieren que las especies de plantas de las familias aquí estudiadas podrían suministrar nuevos compuestos líderes para el desarrollo de agentes antimicobacteriales.
Descritores: Antibacterianos/farmacologia
Mycobacterium tuberculosis
Espectroscopia de Ressonância Magnética
Responsável: CL1.1 - Biblioteca Central

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Id: biblio-875665
Autor: Francisco, Ana Paula.
Título: Toxicidade equivalente da atmosfera por dioxinas, furanos e bifenilas policloradas,com uso de duas técnicas de coleta, passiva e ativa / Equivalent toxicity of the atmosphere for dioxins, furans and polychlorinated biphenyls, using two air sampling techniques, passive and active.
Fonte: São Paulo; s.n; 2017. 133 p.
Idioma: pt.
Tese: Apresentada a Universidade de São Paulo. Faculdade de Saúde Pública. Departamento de Saúde Ambiental para obtenção do grau de Doutor.
Resumo: Introdução: Dioxinas, furanos e bifenilas policloradas são poluentes tóxicos para a saúde humana incluindo riscos de incidência de cânceres, efeitos de neurodesenvolvimento, lesões dérmicas, cloroacne. Estes compostos são poluentes orgânicos persistentes (POPs) que podem ser transportados de longas distâncias da fonte de emissão e se bioacumular em ecossistemas. A atmosfera poluída foi recentemente classificada como carcinogênica para os seres humanos pela Organização Mundial da Saúde, mostrando a importância de sua caracterização, principalmente para compostos tóxicos. Entretanto, técnica de coleta ativa tem custo elevado para POPs, e existem poucos estudos de calibração que validem a substituição. Objetivos: Avaliar a toxicidade equivalente da atmosfera por dioxinas, furanos e bifenilas cloradas, utilizando técnicas de coleta ativa e passiva, e verificar gradiente de concentração nos ambientes urbano, urbano/industrial e de background. Método: Amostras de ar foram coletadas, utilizando coletores ativos e passivos, durante dois períodos consecutivos de quatro meses: de setembro a dezembro de 2014 (período 1) e de maio a agosto de 2015 (período 2) em três cidades de São Paulo, SP, em ambientes urbano, urbano/industrial e de background. Todas as amostras foram extraídas com solução de tolueno:acetona (9:1) em Soxhlet por 24 h e padrões marcados (13C12-PCDD/Fs e 13C12-PCBs) foram adicionados em cada amostra antes do processo de extração. Os extratos foram purificados em coluna de sílica mista (40 por cento H2SO4 e 10 por cento AgNO3) seguida por coluna de alumina. O procedimento analítico foi realizado utilizando HRGC/HRMS (High Resolution Gas Chromatograph/High Resolution Mass Spectrometer) operando em ionização de impacto de elétrons com energia de 35 eV no modo SIM (Select Ion Monitoring) e resolução de 10.000. Resultados mostraram que: (1) existe variação sazonal para concentrações de PCDD/Fs no ar entre os períodos 1 e 2 (p=0,03), enquanto as concentrações de dl-PCBs não foram estatisticamente diferentes nestes períodos (p=0,52); (2) existe gradiente de concentração de PCDD/Fs e dl- PCBs que aumenta na seguinte ordem: background

Introduction: Dioxins, furans and polychlorinated biphenyls are toxic pollutants for human health including risks of cancer incidence, neurodevelopmental effects, dermal lesions, chloracne. These compounds are persistent organic pollutants (POPs) that can be transported to long distances from the emission source and they are bioaccumulated in ecosystems. Recently, the outdoor air pollution were classified as carcinogenic to humans by the World Health Organization, showing the importance of its characterization for toxic compounds. However, active air monitoring has a high cost for POPs, and there is a few calibration studies which support that substitution. Objective: To assess the equivalent toxicity of the atmosphere regarding the measurement of dioxins, furans and polychlorinated biphenyls, using active and passive air samplers, and to evatuate the contrasting concentrations at urban, urban/industrial and background sites. Method: Air samples were collected, using active and passive samplers, over two consecutive periods of four months: from September to December 2014 (period 1) and from May to August 2015 (period 2) at three cities in São Paulo, SP, covering urban, urban/industrial and background sites. All samples were extracted with toluene:acetone (9:1) in a Soxhlet apparatus for 24 hours and surrogate standards (13C12-PCDD/F and 13C12-PCBs) were spiked on each sample media prior to extraction procedure. The extracts were purified on an silica column (40 per cent H2SO4 and 10 per cent AgNO3) followed by an alumina column. The analytical procedure was carried out using HRGC/HRMS (High Resolution Gas Chromatograph/High Resolution Mass Spectrometer) operating in electron impact ionization with an energy of 35 eV in SIM (selected ion monitoring) mode and 10.000 resolution power. Results show that (1) there are seasonal variations for PCDD/F concentrations in air between period 1 and 2 (p=0.03), whereas dl-PCB levels were not statistically different (p=0.52) in those periods. (2) PCDD/F and dl-PCB air levels are in the following order: background
Descritores: Poluição do Ar
Coleta de Dados/métodos
Bifenilos Policlorados
-Vazamento de Gases
Zonas Industriais
Compostos Orgânicos/toxicidade
Área Urbana
Responsável: BR67.1 - CIR - Biblioteca - Centro de Informação e Referência
BR67.1; DR1372

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Texto completo SciELO Brasil
Texto completo
Id: lil-745854
Autor: Paula, Leonardo Koerich de; Solon-de-Mello, Priscilla de Almeida; Mattos, Claudia Trindade; Ruellas, Antônio Carlos de Oliveira; Sant'Anna, Eduardo Franzotti.
Título: Influence of magnification and superimposition of structures on cephalometric diagnosis
Fonte: Dental press j. orthod. (Impr.);20(2):29-34, Mar-Apr/2015. tab, graf.
Idioma: en.
Resumo: OBJECTIVE: The purpose of this study was to assess the influence of magnification and superimposition of structures on CBCT-generated lateral cephalometric radiographs (LCR) using different segments of the cranium. METHODS: CBCT scans of 10 patients were selected. Four LCR were generated using Dolphin Imaging(r) software: full-face, right side, left side and center of the head. A total of 40 images were imported into Radiocef Studio 2(r), and the angles of the most common cephalometric analyses were traced by the same observer twice and within a 10-day interval. Statistical analyses included intraexaminer agreement and comparison between methods by means of intraclass correlation coefficient (ICC) and Bland-Altman agreement tests. RESULTS: Intraexaminer agreement of the angles assessed by ICC was excellent (> 0.90) for 83% of measurements, good (between 0.75 and 0.90) for 15%, and moderate (between 0.50 and 0.75) for 2% of measurements. The comparison between methods by ICC was excellent for 68% of measurements, good for 26%, and moderate for 6%. Variables presenting wider confidence intervals (> 6o) in the Bland-Altman tests, in intraexaminer assessment, were: mandibular incisor angle, maxillary incisor angle, and occlusal plane angle. And in comparison methods the variables with wider confidence interval were: mandibular incisor, maxillary incisor, GoGn, occlusal plane angle, Frankfort horizontal plane (FHP), and CoA. CONCLUSION: Superimposition of structures seemed to influence the results more than magnification, and neither one of them significantly influenced the measurements. Considerable individual variability may occur, especially for mandibular and maxillary incisors, FHP and occlusal plane. .

OBJETIVO: o objetivo do presente estudo foi avaliar a influência da sobreposição estrutural e da magnificação nas radiografias cefalométricas laterais (RCL) geradas por meio de tomografias computadorizadas de feixe cônico (TCFC), usando diferentes segmentos do crânio. MÉTODOS: foram selecionadas 10 tomografias de pacientes. Quatro RCL foram geradas usando Dolphin Imaging, sendo face total, lado direito, lado esquerdo e o centro da cabeça. Um total de 40 imagens foi importado para o Radiocef Studio, e os ângulos das análises cefalométricas mais comuns foram medidos pelo mesmo observador, duas vezes, em um intervalo de 10 dias. As análises estatísticas incluíram concordância intraexaminador e comparação entre os métodos por meio do coeficiente de correlação intraclasse (ICC) e testes de concordância de Bland-Altman. RESULTADOS: a concordância intraexaminador dos ângulos avaliados pelo ICC foi excelente (> 0,90) para 83% das medições, boa (entre 0,75 e 0,90) para 15%, e moderada (entre 0,50 e 0,75) para 2% das medições. A comparação entre os métodos por ICC foi excelente para 68% das medições, boa para 26% e moderada para 6%. As variáveis que apresentaram intervalos de confiança mais amplos (> 6°) nos testes de Bland-Altman, na avaliação intraexaminador, foram: incisivo superior, incisivo inferior e plano oclusal, enquanto nos métodos de comparação, as variáveis com intervalos de confiança mais amplos foram: incisivo inferior, incisivo superior, GoGn, ângulo do plano oclusal, plano horizontal de Frankfort e CoA. CONCLUSÃO: a sobreposição estrutural pareceu influenciar os resultados mais do que a magnificação, mas os métodos não influenciaram significativamente as medições. Considerável variabilidade individual pode ocorrer especialmente para os incisivos superiores e inferiores, plano horizontal de Frankfort e plano oclusal. .
Descritores: Reparo do DNA
Desoxiguanosina/análogos & derivados
Proteínas de Escherichia coli/genética
Escherichia coli/genética
Regulação Bacteriana da Expressão Gênica
Mutagênese/efeitos da radiação
Açúcares Ácidos/metabolismo
Quebras de DNA de Cadeia Dupla
DNA Polimerase beta/genética
DNA Polimerase beta/metabolismo
Proteínas de Escherichia coli/metabolismo
Escherichia coli/metabolismo
Escherichia coli/efeitos da radiação
Endonucleases Flap/genética
Endonucleases Flap/metabolismo
Raios gama
Açúcares Ácidos/química
Tipo de Publ: Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Responsável: BR1.1 - BIREME

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Taddei, José Augusto de Aguiar Carrazedo
Texto completo
Id: lil-744698
Autor: Longo-Silva, Giovana; Toloni, Maysa Helena de Aguiar; Menezes, Risia Cristina Egito de; Asakura, Leiko; Oliveira, Maria Alice Araújo; Taddei, José Augusto de Aguiar Carrazedo.
Título: Introduction of soft drinks and processed juice in the diet of infants attending public day care centers / Introdução de refrigerantes e sucos industrializados na dieta de lactentes que frequentam creches públicas
Fonte: Rev. paul. pediatr;33(1):34-41, Jan-Mar/2015. tab, graf.
Idioma: en.
Projeto: Fundação de Amparo à Pesquisa do Estado e São Paulo.
Resumo: OBJECTIVE: Identifying at what age infants enrolled in public day care centers are introduced to soft drinks and industrialized juice, as well as comparing the nutritional composition of these goods with natural fruit juice. METHODS: A cross-sectional study with the mothers of 636 children (aged 0 to 36 months) from nurseries of day care centers, who were asked questions about the age of feeding introduction. This study evaluated the proximate composition of soft drinks and artificial juice, comparing them with those of natural fruit juice regarding energy, sugar, fiber, vitamin C, and sodium values. The chemical composition of fruit juice was obtained by consulting the Table of Food Composition and, for industrialized drinks, the average nutritional information on the labels of the five most consumed product brands. RESULTS: The artificial drinks were consumed before the first year of life by more than half of the children studied, however, approximately 10% consumed them before the age of 6 months. With regard to the comparison among the drinks, artificial fruit juice beverages and soft drinks proved to contain from nine to 13 times higher amounts of sodium, and 15 times less vitamin C than natural juices. CONCLUSIONS: The introduction of soft drinks and industrialized juice in the diet of infants was inopportune and premature.. When compared to natural fruit juice, these have inferior nutritional composition, which suggests the urgent need for measures based on strategies for food and nutrition education in order to promote awareness and the maintenance of healthy eating habits. .

OBJETIVO: Identificar a idade de introdução do refrigerante e de sucos industrializados na dieta de lactentes matriculados em berçários de creches públicas e comparar as composições nutricionais dessas bebidas com as do suco de fruta natural. MÉTODOS: Estudo transversal com 636 crianças (de zero a 36 meses) de berçários de creches, cujas mães foram entrevistadas sobre idade de introdução dos alimentos. Avaliaram-se as composições centesimais do refrigerante e sucos industrializados, comparando-as com as do suco de laranja natural para valor energético, açúcar, fibra, vitamina C e sódio. A composição centesimal do suco de laranja foi obtida por meio de consulta à Tabela de Composição de Alimentos e, para as bebidas industrializadas, utilizaram-se as médias das informações nutricionais contidas nos rótulos de cinco marcas mais consumidas dos produtos. RESULTADOS: O refrigerante e suco industrializado foram consumidos antes do primeiro ano de vida por mais da metade das crianças estudadas, sendo que cerca de 10% o consumiram antes dos seis meses. Quando comparadas à composição do suco de laranja natural, bebidas forneceram quantidades de 9 a 13 vezes superiores de sódio e 15 vezes inferiores de vitamina C. CONCLUSÕES: A introdução de refrigerantes e sucos industrializados na dieta dos lactentes foi inoportuna e precoce. Comparados ao suco de fruta natural, tais bebidas possuem composição nutricional inferior, sugerindo a necessidade de medidas fundamentadas em estratégias de educação alimentar e nutricional como forma de promover a formação e manutenção de hábitos alimentares saudáveis. .
Descritores: Antibacterianos/farmacologia
Bactérias/efeitos dos fármacos
Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos
Antibacterianos/síntese química
Relação Dose-Resposta a Droga
Testes de Sensibilidade Microbiana
Modelos Moleculares
Estrutura Molecular
Relação Estrutura-Atividade
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: BR1.1 - BIREME

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Id: lil-663714
Autor: Ortiz, Isabel C; Peláez, Carlos A; Orozco, Luz Yaneth; Zuleta, Margarita.
Título: Interacciones genotóxicas de mutágenos en mezclas binarias mediante ensayo cometa alcalino en linfocitos humanos / Interaction of mutagens in binary mixtures using the alkaline comet assay in human lymphocytes
Fonte: Biomédica (Bogotá);32(3):437-448, jul.-set. 2012. ilus, tab.
Idioma: es.
Resumo: Introducción. Los mutágenos contenidos en mezclas complejas presentan interacciones de sinergismo, aditivas o antagónicas. Se han desarrollado enfoques experimentales que permitan dilucidar el responsable de las interacciones en la mezcla. Objetivo. Desarrollar un diseño experimental para comprender los procesos que se llevan a cabo entre los compuestos presentes en las mezclas complejas. Materiales y métodos. Se expusieron linfocitos humanos a mezclas binarias de mutágenos B[a]P, DMBA, Trp-P-1 y MX durante una hora, con activación metabólica y sin ella. La viabilidad se evaluó con azul de tripano y, la genotoxicidad, con cometa alcalino. Resultados. Ningún hidrocarburo tuvo efecto con furanona. Con S9 y sin él, se observó que se presentaban interacciones tóxicas entre hidrocarburos. Se observó sinergismo sin S9 entre B[a]P y Trp-P-1 y, con actividad metabólica, entre DMBA y Trp-P-1. Sin S9 se observó interacción antagónica entre Trp-P-1 y DMBA y, con S9, entre Trp-P-1 y MX y entre MX y DMBA. Se observó un incremento dependiente de la dosis en la longitud de la cola. Hubo daño genotóxico medio y aumento de las células dañadas. Para todas las mezclas se pudo determinar la concentración mínima en la que se observaban efectos adversos y solo para algunas se determinó la concentración máxima en la cual no se observaron efectos adversos. Conclusión. Se hace un aporte para comprender los procesos que ocurren cuando en una mezcla hay presentes, al menos, dos mutágenos y se valida un modelo de análisis que permite dilucidar el compuesto que tiene efecto sobre otro. También, se demostró que según el tipo de compuestos en la mezcla, se tendrá o no un umbral de riesgo.

Introduction. Mutagens contained in complex mixtures can present synergistic interactions, either additive or antagonistic. Therefore, development of experimental approaches is necessary to elucidate which is the responsible agent for the effect in the mixtures. Objective. An experimental design was developed that allowed an understanding of the processes between the compounds of complex mixtures. Materials and methods. Human lymphocytes were exposed to binary mixtures of the mutagens B[a]P, DMBA, Trp-P-1 and MX for 1 hour with or without S9. Viability was assessed with trypan blue dye and the genotoxicity by the comet assay. Results. All of the hydrocarbon showed an effect with furanone. With and without S9, the most toxic interactions were observed between hydrocarbons. Synergistic interaction was observed without S9 between B [a] P and Trp-P-1 and between DMBA and Trp-P-1 with metabolic activity. Without S9 antagonistic interaction was observed only between Trp-P-1+DMBA, and with S9 between Trp-P-1+MX and MX+DMBA. It observed an increase dose dependent in tail length. Half the cultures showed genotoxic damage and increased cell damage. For each mixture, minimum concentrations were determined at which adverse effects are observed; for some only the maximum concentration was determined at which no adverse effects are observed. Conclusion. The processes between mutagens present in a mixture have become better understood, and the results validated an analytical model that determined which component had an effect on another. The results also showed that the type of compounds in the mixture determined whether or not a risk threshold was present.
Descritores: Ensaio Cometa
Técnicas In Vitro
Linfócitos/efeitos dos fármacos
-/administração & dosagem
Benzo(a)pireno/administração & dosagem
Sobrevivência Celular
Carbolinas/administração & dosagem
Células Cultivadas/efeitos dos fármacos
Células Cultivadas/ultraestrutura
Dano ao DNA
Interações Medicamentosas
Furanos/administração & dosagem
Microssomos Hepáticos/metabolismo
Mutagênicos/administração & dosagem
Limites: Adulto
Tipo de Publ: Estudo Comparativo
Research Support, Non-U.S. Gov't
Responsável: CO332 - Facultad de Medicina

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Texto completo SciELO Cuba
Texto completo
Id: lil-628453
Autor: Iraizoz Barrios, Antonio; Bataille, Bernard; Castanedo Cancio, Nilo; Iraizoz Colarte, Antonio; Lidwine, Grosmaire; Barrios Álvarez, María Aurora; Baylac, Giles.
Título: Incremento de disolución de un derivado del furano mediante la técnica de secado por atomización / Improvement of Furane derivate dissolution rate using spray drying technique
Fonte: Rev. cuba. farm;46(2):150-161, abr.-jun. 2012.
Idioma: es.
Resumo: Objetivo: incrementar la solubilidad en agua del 2-bromo-5-(2-bromo-2-nitrovinyl)-furano (G1), un ingrediente farmacéuticamente activo sintetizado por el Centro de Bioactivos Químicos de la Universidad Central de Las Villas, con potente acción bactericida y fungicida, mediante la elaboración de macropartículas de dispersiones sólidas utilizando un proceso de secado por atomización. Métodos: se realizó un ensayo preliminar de secado por atomización de la suspensión de G1, compuesta por: 10 g de G1, 1 g de Aerosil (Aerosil®, Degusa, Bélgica), 1 g de laurilsulfato de sodio y 100 mL de agua. La atomización se efectuó en un equipo de laboratorio (Buchi Mini Dryer spray) a 90 ºC. La dispersión sólida obtenida fue caracterizada físico-químicamente mediante difracción de rayos X, granulometría láser por el método de difracción angular, calorimetría diferencial de barrido, microscopia electrónica de barrido y espectrofotometría de absorción infraroja. Resultados: las partículas obtenidas presentaron un pequeño tamaño, forma esférica y un incremento de la cristalinidad del G-1; no se encontraron interacciones entre los componentes de la dispersión ni presencia de productos de degradación, y la solubilidad del G-1 en agua resultó notablemente incrementada. Conclusiones: el producto obtenido por la técnica de secado por atomización incrementó apreciablemente la solubilidad del G1 sin afectar los grupos funcionales, responsables de la actividad terapéutica que se le reportan al ingrediente activo estudiado. Estos alentadores resultados sugieren la necesidad de continuar estudios para la optimización del proceso y realizar al producto obtenido ensayos de estabilidad con el objetivo de su futura inclusión en formas farmacéuticas de dosificación.

Objective: to increase the solubility of 2-bromium-5(2-bromium-2-nitrovinyl)-furane (G1), one pharmaceutically active ingredient with potent bactericidal and fungicidal action, synthesized through the preparation of solid dispersion macroparticles based on spray-drying process in the Center of Chemical Bioactives of the Central University in Las Villas province. Methods: a preliminary spray-drying test of GI suspension made up of 10 g of G1, 1g of Aerosil (Aerosil®, Degusa, Bélgica), 1g of sodium laurylsulphate and 100 ml of water was made. A piece of lab equipment known as Buchi Mini Dryer spray served for the spraying at 90 ºC. The solid dispersion was characterized from the physical and chemical viewpoints through X-ray diffraction, laser granulometry based on angular diffraction method, differential scanning calorimetry, electronic scanning microscopy and infrared spectrophotometry. Results: the obtained particles were small, spherical and had increased G1 crystallinity. No interactions were found in the dispersion components; there were no degradation products, and G1 solubility was significantly increased. Conclusions: the product obtained from spray-drying technique substantially raised the solubility of G1 without affecting the functional groups, which are responsible for the reported therapeutic action of the studied active ingredient. These encouraging results endorse the need for further studies to optimizing the process and carrying out stability tests for the product to be included in the pharmaceutical forms of dosing in the future.
Descritores: Dissolução
Responsável: CU1.1 - Biblioteca Médica Nacional

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