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1.
J Enzyme Inhib Med Chem ; 34(1): 333-342, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30734600

RESUMO

Leishmaniasis is considered as one of the major neglected tropical diseases due to its magnitude and wide geographic distribution. Leishmania braziliensis, responsible for cutaneous leishmaniasis, is the most prevalent species in Brazil. Superoxide dismutase (SOD) belongs to the antioxidant pathway of the parasites and human host. Despite the differences between SOD of Leishmania braziliensis and human make this enzyme a promising target for drug development efforts. No medicinal chemistry effort has been made to identify LbSOD inhibitors. Herein, we show that thermal shift assays (TSA) and fluorescent protein-labeled assays (FPLA) can be employed as primary and secondary screens to achieve this goal. Moreover, we show that thiazole derivatives bind to LbSOD with micromolar affinity.


Assuntos
Inibidores Enzimáticos/farmacologia , Leishmania braziliensis/enzimologia , Superóxido Dismutase/antagonistas & inibidores , Tiazóis/farmacologia , Brasil , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , Superóxido Dismutase/metabolismo , Tiazóis/síntese química , Tiazóis/química
2.
Mol Biotechnol ; 60(8): 595-600, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29951736

RESUMO

Leishmaniasis is one of the most important neglected tropical diseases, with a broad spectrum of clinical manifestations. Among the clinical manifestations of the disease, cutaneous leishmaniasis, caused by species of Leishmania braziliensis, presents wide distribution in Brazil. In this work, we performed the cloning, expression, and purification of the enzyme superoxide dismutase of Leishmania braziliensis (LbSOD-B2) considered a promising target for the search of new compounds against leishmaniasis. In vitro assays based on pyrogallol oxidation showed that LbSOD-B2 is most active around pH 8 and hydrogen peroxide is a LbSOD-B2 inhibitor at low millimolar range (IC50 = 1 mM).


Assuntos
Leishmania braziliensis/genética , Superóxido Dismutase/genética , Brasil , Clonagem Molecular/métodos , Humanos , Peróxido de Hidrogênio/farmacologia , Leishmania braziliensis/efeitos dos fármacos , Leishmaniose Cutânea/tratamento farmacológico , Leishmaniose Cutânea/parasitologia
3.
J. pediatr. (Rio J.) ; 89(6): 601-607, nov.-dez. 2013. tab
Artigo em Português | LILACS | ID: lil-697136

RESUMO

OBJETIVOS: realizar diagnóstico situacional do bullying e autoestima em unidades municipais de ensino, por meio de estimativa da prevalência do bullying, segundo o sexo, faixa etária e situação do ator; identificar o nível de autoestima dos escolares segundo sexo e situação do ator e correlacionar com o envolvimento em situações de bullying. MÉTODOS: estudo transversal, realizado com 237 alunos, do 9º ano do ensino fundamental, em escolas públicas municipais do Programa Saúde na Escola de Olinda (PE). Foi utilizado um questionário dividido em três blocos, um sociodemográfico, outro sobre bullying, validado por Freire, Veiga e Ferreira, e um para avaliar a autoestima, de Rosenberg. RESULTADOS: a prevalência de bullying foi de 67.5%. A população do estudo foi composta por adolescentes do sexo feminino (56,4%), na faixa etária de 15-19 anos (51,3%), de raça/cor preta (69,1%). Grande parte mora com quatro ou mais pessoas (79,7%), em casa própria (83,8%) e com cinco ou mais cômodos na residência (79,1%). Presenciar ou sofrer bullying foram às situações mais registradas (59,9% e 48,9%, respectivamente); Quando se associou os papéis de bullying e autoestima em relação ao sexo verificou-se que no grupo de vítimas/agressores e agressores (p = 0,006 e 0,044; respectivamente), o sexo masculino apresentou escores de autoestima superiores estatisticamente significativos em relação aos do sexo feminino. CONCLUSÃO: os achados apontam para um número grande de alunos envolvidos nos diversos papéis do bullying, identificando-se associação entre estas características e o sexo/gênero e autoestima dos envolvidos. Identifica-se a necessidade de estudos adicionais sobre a natureza do evento.


OBJECTIVES: to perform a situational analysis of bullying and self-esteem in municipal school units, by estimating the prevalence of bullying, according to gender, age, and role in bullying situations; and to identify the level of self-esteem of students by gender and role in bullying situations and correlate with the involvement in bullying situations. METHODS: this was a cross-sectional study with 237 students in the ninth grade of middle school from public schools participating in the School Health Program in the city of Olinda (PE). The questionnaire used in the study was divided into three blocks: a sociodemographic block; a block on bullying, validated by Freire, Simão, and Ferreira (2006); and a block to assess self-esteem, by Rosenberg (1989). RESULTS: the prevalence of bullying was 67.5%. The study population consisted of adolescents, mostly female (56.4%), aged 15-19 years (51.3%), of black ethnicity (69.1%). Most students lived with four or more people (79.7%) in their family-owned homes (83.8%), which had five or more rooms (79.1%). Observing bullying or being bullied were the most often reported situations (59.9% and 48.9%, respectively); when the roles of bullying are associated with self-esteem in relation to gender, it was observed that in the group of victims/aggressors and aggressors (p = 0.006 and 0.044, respectively), males had higher statistically significant self-esteem scores when compared to females. CONCLUSION: the findings indicate a large number of students involved in the several roles of bullying, identifying an association between these characteristics and sex/gender and self-esteem of those involved. The present study has identified the need for further studies on the nature of the event.


Assuntos
Adolescente , Feminino , Humanos , Masculino , Adulto Jovem , Bullying/psicologia , Setor Público , Autoimagem , Estudantes , Instituições Acadêmicas/estatística & dados numéricos , Violência/estatística & dados numéricos , Brasil , Estudos Transversais , Programas Nacionais de Saúde , Fatores Sexuais , Fatores Socioeconômicos
4.
J Pediatr (Rio J) ; 89(6): 601-7, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24029549

RESUMO

OBJECTIVES: To perform a situational analysis of bullying and self-esteem in municipal school units, by estimating the prevalence of bullying, according to gender, age, and role in bullying situations; and to identify the level of self-esteem of students by gender and role in bullying situations and correlate with the involvement in bullying situations. METHODS: This was a cross-sectional study with 237 students in the ninth grade of middle school from public schools participating in the School Health Program in the city of Olinda (PE). The questionnaire used in the study was divided into three blocks: a sociodemographic block; a block on bullying, validated by Freire, Simão, and Ferreira (2006); and a block to assess self-esteem, by Rosenberg (1989). RESULTS: The prevalence of bullying was 67.5%. The study population consisted of adolescents, mostly female (56.4%), aged 15-19 years (51.3%), of black ethnicity (69.1%). Most students lived with four or more people (79.7%) in their family-owned homes (83.8%), which had five or more rooms (79.1%). Observing bullying or being bullied were the most often reported situations (59.9% and 48.9%, respectively); when the roles of bullying are associated with self-esteem in relation to gender, it was observed that in the group of victims/aggressors and aggressors (p = 0.006 and 0.044, respectively), males had higher statistically significant self-esteem scores when compared to females. CONCLUSION: The findings indicate a large number of students involved in the several roles of bullying, identifying an association between these characteristics and sex/gender and self-esteem of those involved. The present study has identified the need for further studies on the nature of the event.


Assuntos
Bullying/psicologia , Setor Público , Instituições Acadêmicas/estatística & dados numéricos , Autoimagem , Estudantes , Violência/estatística & dados numéricos , Adolescente , Brasil , Estudos Transversais , Feminino , Humanos , Masculino , Programas Nacionais de Saúde , Fatores Sexuais , Fatores Socioeconômicos , Adulto Jovem
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