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Id: lil-769514
Autor: Gadelha, Ellen Priscilla Nunes; Talhari, Sinésio; Guerra, Jorge Augusto de Oliveira; Neves, Leandro Ourives; Talhari, Carolina; Gontijo, Bernardo; Silva Junior, Roberto Moreira da; Talhari, Anette Chrusciak.
Título: Efficacy and safety of a single dose pentamidine (7mg/kg) for patients with cutaneous leishmaniasis caused by L. guyanensis: a pilot study
Fonte: An. bras. dermatol;90(6):807-813, Nov.-Dec. 2015. tab, graf.
Idioma: en.
Resumo: Abstract: BACKGROUND: There have been few studies on pentamidine in the Americas; and there is no consensus regarding the dose that should be applied. OBJECTIVES: To evaluate the use of pentamidine in a single dose to treat cutaneous leishmaniasis. METHODS: Clinical trial of phase II pilot study with 20 patients. Pentamidine was used at a dose of 7 mg/kg, in a single dose. Safety and adverse effects were also assessed. Patients were reviewed one, two, and six months after the end of treatments. RESULTS: there was no difference between the treatment groups in relation to gender, age, number or location of the lesions. Pentamidine, applied in a single dose, obtained an effectiveness of 55%. Mild adverse events were reported by 17 (85%) patients, mainly transient pain at the site of applications (85%), while nausea (5%), malaise (5%) and dizziness (5%) were reported in one patient. No patient had sterile abscess after taking medication at a single dose of 7mg/kg. CONCLUSIONS: Clinical studies with larger samples of patients would enable a better clinical response of pent amidine at a single dose of 7mg, allowing the application of more powerful statistical tests, thus providing more evidences of the decrease in the effectiveness of that medication. Hence, it is important to have larger studies with new diagrams and/or new medications.
Descritores: Antiprotozoários/administração & dosagem
Benzamidinas/administração & dosagem
Leishmania guyanensis
Leishmaniose Cutânea/tratamento farmacológico
Éteres Fenílicos/administração & dosagem
-Antiprotozoários/efeitos adversos
Benzamidinas/efeitos adversos
Glicemia/análise
Relação Dose-Resposta a Droga
Projetos Piloto
Éteres Fenílicos/efeitos adversos
Reprodutibilidade dos Testes
Fatores de Tempo
Resultado do Tratamento
Limites: Adolescente
Adulto
Feminino
Seres Humanos
Masculino
Meia-Idade
Adulto Jovem
Tipo de Publ: Ensaio Clínico Fase II
Responsável: BR1.1 - BIREME


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Id: lil-741217
Autor: Maekawa, Lilian Eiko; Rossoni, Rodnei Dennis; Barbosa, Júnia Oliveira; Jorge, Antonio Olavo Cardoso; Junqueira, Juliana Campos; Valera, Marcia Carneiro.
Título: Different Extracts of Zingiber officinale Decrease Enterococcus faecalis Infection in Galleria mellonella
Fonte: Braz. dent. j;26(2):105-109, Mar-Apr/2015. tab, graf.
Idioma: en.
Projeto: São Paulo Research Foundation (FAPESP).
Resumo: Dried, fresh and glycolic extracts of Zingiber officinale were obtained to evaluate the action against G. mellonella survival assay against Enterococcus faecalis infection. Eighty larvae were divided into: 1) E. faecalis suspension (control); 2) E. faecalis + fresh extract of Z. officinale (FEO); 3) E. faecalis + dried extract of Z. officinale (DEO); 4) E. faecalis + glycolic extract of Z. officinale (GEO); 5) Phosphate buffered saline (PBS). For control group, a 5 μL inoculum of standardized suspension (107 cells/mL) of E. faecalis (ATCC 29212) was injected into the last left proleg of each larva. For the treatment groups, after E. faecalis inoculation, the extracts were also injected, but into the last right proleg. The larvae were stored at 37 °C and the number of dead larvae was recorded daily for 168 h (7 days) to analyze the survival curve. The larvae were considered dead when they did not show any movement after touching. E. faecalis infection led to the death of 85% of the larvae after 168 h. Notwithstanding, in treatment groups with association of extracts, there was an increase in the survival rates of 50% (GEO), 61% (FEO) and 66% (DEO) of the larvae. In all treatment groups, the larvae exhibited a survival increase with statistically significant difference in relation to control group (p=0.0029). There were no statistically significant differences among treatment groups with different extracts (p=0.3859). It may be concluded that the tested extracts showed antimicrobial activity against E. faecalis infection by increasing the survival of Galleria mellonella larvae.

Extratos seco, fresco e glicólico de Zingiber officinale foram obtidos para avaliar suas ações por meio de ensaio de sobrevivência em G. mellonella contra infecção por Enterococcus faecalis. Oitenta larvas foram divididas em: 1) Suspensão de E. faecalis (controle); 2) E. faecalis + extrato fresco de Z. officinale (FEO); 3) E. faecalis + extrato seco de Z. officinale (DEO); 4) E. faecalis + extrato glicólico de Z. officinale (GEO); 5) Solução tampão fosfato salina (PBS). Para o grupo de controle, 5 µL de inóculo de suspensão padronizada (107 células/mL) de E. faecalis (ATCC 29212) foi injetado na última proleg esquerda de cada lagarta. Para os grupos com tratamento, após a injeção de E. faecalis, os extratos foram injetados na última proleg direita. Após as injeções, as lagartas foram armazenadas a 37 °C e o número de animais mortos foi registrado diariamente em 168 h (7 dias) para analisar a curva de sobrevivência. As lagartas foram consideradas mortas quando elas não mostraram qualquer movimento após o toque. A infecção por E. faecalis levou à morte de 85% das lagartas após 168 h. Não obstante, nos grupos de tratamento com associação dos extratos, houve um aumento nas taxas de sobrevivência de 50% (GEO), 61% (FEO) e 66% (DEO) das lagartas. Em todos os grupos com tratamento, as lagartas apresentaram um aumento na sobrevivência, com diferença estatisticamente significativa em relação ao grupo controle (p=0,0029). Não houve diferença estatisticamente significativa entre os tratamentos com os diferentes extratos (p=0,3859). Pode concluir-se que os extratos testados mostraram atividade antimicrobiana contra a infecção por E. faecalis, aumentando a sobrevivência das lagartas de G. mellonella.
Descritores: Receptores de GABA-A/química
-Sítios de Ligação
Benzamidinas/química
Benzamidinas/metabolismo
Benzamidinas/farmacologia
Sequência Conservada
Cristalografia por Raios X
Membrana Celular/química
Membrana Celular/metabolismo
Desenho de Drogas
Agonistas de Receptores de GABA-A/química
Agonistas de Receptores de GABA-A/metabolismo
Agonistas de Receptores de GABA-A/farmacologia
Predisposição Genética para Doença
Glicosilação
Modelos Moleculares
Mutação/genética
Estrutura Quaternária de Proteína
Estrutura Terciária de Proteína
Subunidades Proteicas
Polissacarídeos/química
Polissacarídeos/metabolismo
Receptores de GABA-A/genética
Transmissão Sináptica
Limites: Seres Humanos
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: BR1.1 - BIREME


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Id: lil-414713
Autor: Pereira, M. T; Silva-Alves, J. M; Martins-José, A; Lopes, J. C. D; Santoro, M. M.
Título: Thermodynamic evaluation and modeling of proton and water exchange associated with benzamidine and berenil binding to ß-trypsin
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;38(11):1593-1601, Nov. 2005.
Idioma: en.
Resumo: Serine-proteases are involved in vital processes in virtually all species. They are important targets for researchers studying the relationships between protein structure and activity, for the rational design of new pharmaceuticals. Trypsin was used as a model to assess a possible differential contribution of hydration water to the binding of two synthetic inhibitors. Thermodynamic parameters for the association of bovine ß-trypsin (homogeneous material, observed 23,294.4 ± 0.2 Da, theoretical 23,292.5 Da) with the inhibitors benzamidine and berenil at pH 8.0, 25°C and with 25 mM CaCl2, were determined using isothermal titration calorimetry and the osmotic stress method. The association constant for berenil was about 12 times higher compared to the one for benzamidine (binding constants are K = 596,599 ± 25,057 and 49,513 ± 2,732 M-1, respectively; the number of binding sites is the same for both ligands, N = 0.99 ± 0.05). Apparently the driving force responsible for this large difference of affinity is not due to hydrophobic interactions because the variation in heat capacity (DCp), a characteristic signature of these interactions, was similar in both systems tested (-464.7 ± 23.9 and -477.1 ± 86.8 J K-1 mol-1 for berenil and benzamidine, respectively). The results also indicated that the enzyme has a net gain of about 21 water molecules regardless of the inhibitor tested. It was shown that the difference in affinity could be due to a larger number of interactions between berenil and the enzyme based on computational modeling. The data support the view that pharmaceuticals derived from benzamidine that enable hydrogen bond formation outside the catalytic binding pocket of ß-trypsin may result in more effective inhibitors.
Descritores: Benzamidinas/química
Diminazena/análogos & derivados
Inibidores da Tripsina/química
Tripsina/química
-Água/química
Calorimetria
Diminazena/química
Concentração de Íons de Hidrogênio
Modelos Químicos
Estrutura Molecular
Pressão Osmótica
Ligação Proteica
Prótons
Termodinâmica
Limites: Animais
Bovinos
Responsável: BR1.1 - BIREME


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Id: lil-277054
Autor: Sousa, M. O; Miranda, T. L. S; Costa, E. B; Bittar, E. R; Santoro, M. M; Figueiredo, A. F. S.
Título: Linear competitive inhibition of human tissue kallikrein by 4-aminobenzamidine and benzamidine and linear mixed inhibition by 4-nitroaniline and aniline
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;34(1):35-44, Jan. 2001. tab, graf.
Idioma: en.
Conferência: Apresentado em: Annual Meeting of the Brazilian Society of Biochemistry and Molecular Biology, 28, Caxambu, May 22-25, 1999.
Projeto: FAPEMIG; . CNPq.
Resumo: Hydrolysis of D-valyl-L-leucyl-L-arginine p-nitroanilide (7.5-90.0 `M) by human tissue kallikrein (hK1) (4.58-5.27 nM) at pH 9.0 and 37ºC was studied in the absence and in the presence of increasing concentrations of 4-aminobenzamidine (96-576 `M), benzamidine (1.27-7.62 mM), 4-nitroaniline (16.5-66 `M) and aniline (20-50 mM). The kinetic parameters determined in the absence of inhibitors were: Km = 12.0 + or - 0.8 `M and k cat = 48.4 + or - 1.0 min-1. The data indicate that the inhibition of hK1 by 4-aminobenzamidine and benzamidine is linear competitive, while the inhibition by 4-nitroaniline and aniline is linear mixed, with the inhibitor being able to bind both to the free enzyme with a dissociation constant Ki yielding an EI complex, and to the ES complex with a dissociation constant Ki', yielding an ESI complex. The calculated Ki values for 4-aminobenzamidine, benzamidine, 4-nitroaniline and aniline were 146 + or - 10, 1,098 + or - 91, 38.6 + or - 5.2 and 37,340 + or - 5,400 `M, respectively. The calculated Ki' values for 4-nitroaniline and aniline were 289.3 + or - 92.8 and 310,500 + or - 38,600 `M, respectively. The fact that Ki'>Ki indicates that 4-nitroaniline and aniline bind to a second binding site in the enzyme with lower affinity than they bind to the active site. The data about the inhibition of hK1 by 4-aminobenzamidine and benzamidine help to explain previous observations that esters, anilides or chloromethyl ketone derivatives of Nalpha-substituted arginine are more sensitive substrates or inhibitors of hK1 than the corresponding lysine compounds
Descritores: Compostos de Anilina/farmacologia
Benzamidinas/farmacologia
Compostos Cromogênicos/metabolismo
Oligopeptídeos/metabolismo
Calicreínas Teciduais/antagonistas & inibidores
-Amidoidrolases/metabolismo
Sítios de Ligação
Hidrólise
Modelos Lineares
Calicreínas Teciduais/metabolismo
Inibidores da Tripsina/farmacologia
Limites: Seres Humanos
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: BR1.1 - BIREME


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Id: lil-113586
Autor: Junqueira, R. G; Silva, E; Mares-Guia, M.
Título: Competitive parabolic inhibition of bovine trypsin by benzamidines
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;25(9):873-87, 1992. ilus.
Idioma: en.
Resumo: Competitive parabolic inhibition, a rare type of inhibition of one-substrate enzymes, is described for alpha-and beta-trypsin. The enzymes were so inhibited by two bis-benzamidines 4-4' diazoamino-bis-benzamidine, Berenil (DABB) and its platinum complex, DABB-PtCl2, acting on acyl-amino acid-peptidyl nitroanilides (Nan) substrates, when inhibitor concentrations exceed 10 mM and approch the millimolar range. The type of nonlinear inhibition observed require4s ternary complex formation between one enzyme molecule and two inhibitor molecules (M. E. M), and also permits the formation of the mixed ternary complex (M. E. S.). Binding of the first DABB molecule to the active center of trypsin takes place with K1 values of ca. 1.50 uM for both alpha-and- beta-trypsin. The secondary binding site binds the inhibitor with dissociation constants K12 close to 0.25 mM for both forms of the enzyme, as determined with different substrates. The dissociation constants of the ternary mixed complexes (Ksi and Kis), however, depend on the structural features of the substrates, which are of negligible importance for Bz-Arg-Nan, but significant for Ac-Phe-Arg-Nan and D-Val-Leu-Arg-Nan, reflecting subsite interactions between S1-S3 and S'2. Pentamidine, a diamidino-4,4'-diphenoxy-alkane with a flexible chain, behaved as a strict competitive inhibitor. This implies that the triazene moiety of DABB is involved in the interaction between the inhibitor and the secondary binding site of the enzyme
Descritores: Benzamidinas
Bovinos
Inibidores Enzimáticos
Tripsina/antagonistas & inibidores
Responsável: BR26.1 - Biblioteca Central


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Id: lil-103648
Autor: Andrade, M. H. G; Silva, E; Guia, M. Mares.
Título: A plausible identification of secondary binding site in trypsin and trypsinogen
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;23(12):1223-31, 1990. tab.
Idioma: en.
Resumo: 1. The determination of the binding of 4,4'diazoamino-bis-benzamidine (DABB) to alfa-trypsin by equilibrium measurements in columns indicated a stoichiometry of 2 mol ligan/mol enzyme. One molecule binds to the secondy binding site, sith Ki2=mMat pH8,0, 25-C. 2. Bovine pancreatic trypsin inhibitor (BPTI) prevented binding of DABB to both sites, indicating that they are topographically close and within the interface of the trypsin-BPTI complex. 3. On the basis of data from the interface of the trypsin-BPTI complex, we concluded that the secondary binding site of trypsin is plausibly identified as the same site in trypsin that binds the Arg-17 reside of BPTI, i.e., Tyr-39 and Tyr-151 in bovine trypsin. This site would then correspond to subsite S'2 on the enzyme surface
Descritores: Benzamidinas/metabolismo
Tripsina/metabolismo
-Benzamidinas/química
Sítios de Ligação
Cromatografia de Afinidade
Matemática
Tripsinogênio/metabolismo
Responsável: BR1.1 - BIREME


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Rogana, E
Id: lil-83378
Autor: Rogana, E; Silva, N. Penha; Guia, M. Mares.
Título: The substituent effect on complex formation between alfa-trypsin and para-substituted benzamidinium ions: A thermodynamic study
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;22(10):1177-90, 1989. tab, ilus.
Idioma: en.
Resumo: Dissociation constants, Kj, were determined spectrophotometrically by measuring the absorbance at 410 nm, using N alfa-benzoyl-D,L-argomome-para-nitroanilide (Bz-D,L-Arg-Nan) as substrate. The Ki values for the complexes of alfa-trypsin with each of the para-derivatives of the benzamidinium ion -NH2, -CH3, -H, -F, -Cl, -Br, -COOEt, and -NO2 were measured at six temperatures (8,15,20,25, 29 and 33§C), in order to determine the thermodynamic parameters for complex formation. The standard enthalpy change was constant and all other parameters were also negative. The large negative values obtained for the standard heat capacity change suggest that the process occurs with a conformational adaptation in the enzyme structure. The apparent partial specife volumes of free alfa-trypsin and alfa-trypsin bound to benzamidinium ion indicated that there is a decrease of approximatelly 0.10 cm**3/g in the enzyme volume when the inhibitor binds. This contraction is consistent with the release of about 130 water molecules per enzyme molecule
Descritores: Benzamidinas/metabolismo
Espectrofotometria Atômica
Termodinâmica
Tripsina/metabolismo
-Conformação Proteica
Inibidores da Tripsina/metabolismo
Responsável: BR26.1 - Biblioteca Central


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Caovilla, Heloisa Helena
Id: lil-53607
Autor: Ganança, Maurício Malavasi; Caovilla, Heloisa Helena; Anadäo, Carlos Augusto; Nunes, Claudio Tobias Acatauassú.
Título: Estudo comparativo entre cloridrato de benzidamina versus hexamidina associada ao cloridrato de tetracaína no tratamento tópico das amegdalites / Benzydamine versus hexamydine associated with chloridrate of tetracaine in topic treatment of tonsillitis
Fonte: RBM rev. bras. med;45(3):66-8, mar. 1988. tab.
Idioma: pt.
Resumo: Sessenta e seis pacientes febris, com amigdalite aguda ou crônica reacutizada foram tratados por um período de 7 dias consecutivos com nebulizaçöes tópicas de benzidamina spray ou hexamidina + tetracaína aerosol.Ambas as medicaçöes experimentadas mostraram-se altamente efetivas, de boa tolerabilidade e palatabilidade. Observou-se tendência de melhora mais rápida com a utilizaçäo da benzidamina spray. Os resultados obtidos com o uso da benzidamina spray indicam que este potente antiinflamatório tópico deve ser incluído no arsenal terapêutico destinado ao combate das amigdalites, pelo valioso alívio sintomático que é capaz de proporcionar
Descritores: Benzamidinas/uso terapêutico
Benzidamina/uso terapêutico
Tetracaína/uso terapêutico
Tonsilite/tratamento farmacológico
-Administração Tópica
Limites: Adolescente
Adulto
Meia-Idade
Seres Humanos
Masculino
Feminino
Tipo de Publ: Estudo Comparativo
Responsável: BR1.1 - BIREME



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