RESUMO
Resumen En el presente trabajo utilizamos la minería de texto como herramienta de tratamiento de una gran base de datos científica, con el objetivo de obtener nueva información de todas las publicaciones firmadas por autores argentinos e indexadas hasta 2019 en el área de las ciencias de la vida. Se analizaron más de 75 000 artículos, publicados en alrededor de 5000 medios, firmados por cerca de 186 000 autores con lugar de trabajo en la Argentina o en colaboraciones con laboratorios argentinos. Mediante herramientas automatizadas, que fueron desarrolladas ad hoc, se analizó el texto de alrededor de 70 800 resúmenes y se buscaron, mediante detección digital no supervisada, los principales temas abordados, su relación con problemáticas de salud en la Argentina y su tratamiento. Se presentan, además, resultados del número de publicaciones por año, las revistas que las publicaron, y sobre sus autores y colaboraciones. Estos resultados, junto con las predicciones que se obtuvieron, podrían constituirse en una herramienta útil para optimizar el manejo de recursos dedicados a la investigación básica y clínica.
Abstract In the present work we use text mining as a treatment tool for a large scientific database, with the aim of obtaining new information about all the publications signed by Argentine authors and indexed until 2019, in the area of life sciences. More than 75 000 articles were analysed, published in around 5000 media, signed by about 186 000 authors with a workplace in Argentina or in collaborations with Argentine laboratories. Using automated tools that were developed ad hoc, the text of around 70 800 abstracts was analysed, seeking, through non-supervised digital detection, the main topics addressed by the authors, and the relationship with health problems in Argentina and their treat ment. Results are also presented regarding the number of publications per year, the journals that have published them, and their authors and collaborations. These results, together with the predictions that were obtained, could become a useful tool to optimize the management of resources dedicated to basic and clinical research.
Assuntos
Humanos , Mineração de Dados , ArgentinaRESUMO
In the present work we use text mining as a treatment tool for a large scientific database, with the aim of obtaining new information about all the publications signed by Argentine authors and indexed until 2019, in the area of life sciences. More than 75 000 articles were analysed, published in around 5000 media, signed by about 186 000 authors with a workplace in Argentina or in collaborations with Argentine laboratories. Using automated tools that were developed ad hoc, the text of around 70 800 abstracts was analysed, seeking, through non-supervised digital detection, the main topics addressed by the authors, and the relationship with health problems in Argentina and their treatment. Results are also presented regarding the number of publications per year, the journals that have published them, and their authors and collaborations. These results, together with the predictions that were obtained, could become a useful tool to optimize the management of resources dedicated to basic and clinical research.
En el presente trabajo utilizamos la minería de texto como herramienta de tratamiento de una gran base de datos científica, con el objetivo de obtener nueva información de todas las publicaciones firmadas por autores argentinos e indexadas hasta 2019 en el área de las ciencias de la vida. Se analizaron más de 75 000 artículos, publicados en alrededor de 5000 medios, firmados por cerca de 186 000 autores con lugar de trabajo en la Argentina o en colaboraciones con laboratorios argentinos. Mediante herramientas automatizadas, que fueron desarrolladas ad hoc, se analizó el texto de alrededor de 70 800 resúmenes y se buscaron, mediante detección digital no supervisada, los principales temas abordados, su relación con problemáticas de salud en la Argentina y su tratamiento. Se presentan, además, resultados del número de publicaciones por año, las revistas que las publicaron, y sobre sus autores y colaboraciones. Estos resultados, junto con las predicciones que se obtuvieron, podrían constituirse en una herramienta útil para optimizar el manejo de recursos dedicados a la investigación básica y clínica.
Assuntos
Mineração de Dados , Argentina , HumanosRESUMO
A series of related thalidomide derivatives (2-9) were synthesized by microwave irradiation and evaluated for anti-inflammatory activity. Such activity was assessed in vivo and ex vivo. Compounds 2, 8 and 9 showed the highest levels of inhibition of TNF-α production. On rat paw edema and hyperalgesia assays, compound 9, (1,4-phthalazinedione) demonstrated the highest in vivo anti-inflammatory activity. Thus, compound 9 can be considered as a promising compound to be subjected to further modification to obtain new agents for the treatment of inflammatory diseases.
Assuntos
Anti-Inflamatórios , Talidomida , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Animais , Anti-Inflamatórios/síntese química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Líquido da Lavagem Broncoalveolar/imunologia , Carragenina , Edema/induzido quimicamente , Edema/tratamento farmacológico , Edema/metabolismo , Pé/patologia , Hiperalgesia/induzido quimicamente , Hiperalgesia/tratamento farmacológico , Lipopolissacarídeos , Masculino , Camundongos Endogâmicos BALB C , Peroxidase/metabolismo , Ratos Sprague-Dawley , Talidomida/análogos & derivados , Talidomida/farmacologia , Talidomida/uso terapêutico , Fator de Necrose Tumoral alfa/imunologiaRESUMO
A series of novel benzoimidazo and N-aryl-5-oxo-imidazo[1,2-b]isoquinoline-10-carbothioamides was developed. All the compounds were evaluated for their in vitro action against the epimastigote form of Trypanosoma cruzi. Four of them showed higher activity than Nifurtimox. Their unspecific cytotoxicity was evaluated using HeLa and L6 cells, being non-toxic at concentrations at least 15 and 200 times higher than that of T. cruzi IC(50.) To gain insight into the mechanism of action, their DNA binding properties and reactivity with glutathione were studied, and QSAR study was performed.
Assuntos
DNA de Protozoário/metabolismo , Imidazóis/química , Imidazóis/farmacologia , Isoquinolinas/química , Isoquinolinas/farmacologia , Tripanossomicidas/síntese química , Trypanosoma cruzi/efeitos dos fármacos , Animais , Doença de Chagas/tratamento farmacológico , Relação Dose-Resposta a Droga , Glutationa/química , Glutationa/metabolismo , Células HeLa , Humanos , Imidazóis/metabolismo , Imidazóis/toxicidade , Isoquinolinas/metabolismo , Isoquinolinas/toxicidade , Modelos Moleculares , Oxirredução/efeitos dos fármacos , Relação Quantitativa Estrutura-Atividade , Tripanossomicidas/metabolismo , Tripanossomicidas/farmacologia , Tripanossomicidas/toxicidadeRESUMO
A new series of bis-aminomethylnaphthalenes were synthesized in satisfactory overall yield, through a simple synthetic strategy using reductive amination. The DNA binding properties of these compounds have been examined and compared to those of reference drugs using an UV spectroscopy method. The compounds were evaluated for their in vitro anticancer activity and some of them were studied in vivo. Compound 15 exhibited remarkable antitumor activity and represents a novel template for anticancer chemotherapy and can serve as a new lead compound.