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Id: biblio-1151003
Autor: Monasterios Heydra, Melina C..
Título: Síntesis y evaluación preliminar de la posible actividad antimalárica y antineoplásica de derivados 7-cloroquinolina-4-sustituidos / Synthesis and preliminary evaluation of antimalarial and antineoplastic possible activity of 7-chloroquinoline-4-substituted derivatives.
Fonte: Caracas; s.n; feb, 2013. ilus.
Idioma: es.
Tese: Apresentada a Universidad Central de Venezuela. Facultad de Farmacia para obtenção do grau de Doctor.
Resumo: En el presente trabajo se describe la síntesis y la evaluación de la posible actividad Antimalárica y Antineoplásica de una serie de derivados 7-cloroquinolina-4-sustituidos. La estrategia empleada para la síntesis comienza con las obtención de los intermediarios clave 1-(3 ó 4-(7-cloroquinolin-4-ilamino)fenil)etanona (2 y 3) mediante una sustitución nucleofílica aromática entre la 4,7-dicloroquinolina y la 3 y/o 4-amino acetofenona. Los derivados (E)-1-(3 ó 4-(7-cloroquinolin-4-ilamino)fenil)-3-(fenilsustituido)prop-2-eno-1-ona (4 y 5), se sintetizaron a través de una condensación aldólica de Claisen-Schmidt entre los intermediarios clave y diferentes benzaldehídos sustituidos. Los derivados 7-cloro-N-(3 ó 4-(4,5-dihidro-5-(fenilsustituido)-1H-pirazol-3-il)fenil)quinolin-4-amina (6 y 7) y los 1-(3 ó 4-(7-cloroquinolin-4-ilamino)fenil)-3-(fenilsustituido)propano-1-ona (8 y 9) se diseñaron por modificación molecular de la cetona a,b-insaturada de los compuestos finales 4 y 5, (metodología clásica de la Química Medicinal) para obtener dichos derivados rígidos 6 y 7, mediante la formación de un anillo D2-pirazolina y flexibles 8 y 9, a través de su reducción. La síntesis de los derivados 6 y 7 se realizó mediante una reacción de ciclo-condensación con hidrazina monohidratada y los derivados 8 y 9, se obtuvieron a través de una hidrogenación catalítica. En la evaluación de la actividad Antimalárica in vitro se evidenció que los derivados 4, 5, 6 y 7, mostraron actividades inhibitorias la formación de la b hematina importantes (superior al 70 %), siendo los más activos: 4l, 5g, 5c, 5g y 6e, 6f con valores comparable al de la CQ. En la evaluación Antimalárica in vivo se encontró que el derivado 4e fue el más activo con 26,4 días de sobrevivencia post-infección (230 % de incremento) y una parasitemia de 2,4 % (96 % de reducción). Con respecto a los resultados obtenidos en el efecto de estos derivados sobre la viabilidad y proliferación de las líneas celulares neoplásicas Jurkat E6.1, HL60, MCF-7 y A549, los compuestos 4a, 4g, 4l, 4m y 6e mostraron la mayor actividad inhibitoria del crecimiento de las células leucémicas HL60 después de 24h de tratamiento con valores de CI50 de 1,19 µM, 1,08 µM, 0,59 µM, 0,43 µM y 0,94 µM (hasta 3 y 100 veces más activos que la doxorubicina y que la CQ, respectivamente). En lo referente a la evaluación de la actividad proapoptótica en las líneas celulares neoplásicas Jurkat E6.1, HL60, MCF-7 y A549, se evidenció que los derivados 4, 5 y 6, al igual que los controles, generaron un aumento en el porcentaje de células positivas para la Anexina V/FITC dependiente de la dosis (apoptosis temprana y tardía). Ninguno de estos derivados indujo el proceso de necrosis en estas células.

The present investigation describes the synthesis and evaluation of the Antimalarial and Antineoplastic activity possible a series of derivatives of 7-substituted-4-chloro-quinoline. The strategy employed for the synthesis begins with preparation of the key intermediate 1-(3 or 4-(7-chloroquinolin-4-ylamino) phenyl)ethanone (2and 3) by a nucleophilic aromatic substitution between 4,7-dichloroquinoline and the 3 and/or4-amino acetophenone. The derivatives (E)-1-(3 or 4-(7-chloroquinolin-4-ylamino) phenyl)-3-(substitutedphenyl)prop-2-en-1-one (4and 5), were synthesized a through aldol condensation Claisen-Schmidt among different key intermediates and substituted benzaldehydes. The resulting 7-chloro-N-(3 or 4-(4,5-dihydro-5-(substitutedphenyl)-1H-pyrazol-3-yl)phenyl)quinolin-4-amine (6 and 7) and 7-chloro-4-[(3 or 4-(substituted phenyl)ethylcarbonyl)phenyl]aminoquinoline(8 and 9) were designed for the molecular modification , -unsaturated ketone of the final compounds 4and 5 (classic methodology Medicinal Chemistry) for said rigid derivatives 6and 7, through the formation of a 2-pyrazoline ring flexible and 8and 9, through its reduction. The synthesis of derivatives 6and 7were performed using a cycle-condensation reaction with hydrazine monohydrate and 8and 9derivatives were obtained via a catalytic hydrogenation. In the assessment of antimalarial activity in vitro was demonstrated that derivatives 4, 5, 6and 7showed inhibitory activities forming the major hematin (above 70%), being more active: 4l, 5g, 5c, 5g, 6eand 6f,with values comparable to that of CQ. In vivoantimalarial evaluation found that the derivative 4ewas most active with survival 26.4 dayspost-infection (230% increase) and a parasitemia of 2.4% (96% reduction). With regard to the results on the effect of these derivatives on the viability and proliferation of neoplastic cell lines Jurkat E6.1, HL60, MCF-7 and A549, compounds 4a, 4g, 4l,4mand 6eshow greater activity growth inhibitory HL60 leukemia cells after 24 h of treatment with IC50values of 1.19µM, 1.08µM, 0.59µM, 0.43µMand 0.94 M (to 3 and 100 times more active than doxorubicin and the CQ, respectively). Regarding the evaluation of pro-apoptotic activity on neoplastic cell lines Jurkat E6.1, HL60, MCF-7 and A549, was demonstrated that derivatives 4, 5and 6, like the controls, an increase in generated percentage of cells positive for Annexin V/FITC dose dependent (early andlate apoptosis). None of these derivatives induced necrosis process in these cells.
Descritores: Quinolinas/química
Cloroquina/química
Antimaláricos/química
Antineoplásicos/química
-Plasmodium berghei/efeitos dos fármacos
Quinolinas/síntese química
Quinolinas/farmacologia
Técnicas In Vitro/métodos
Linhagem Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Cloroquina/síntese química
Cloroquina/farmacologia
Apoptose/efeitos dos fármacos
Proliferação de Células/efeitos dos fármacos
Antimaláricos/síntese química
Antimaláricos/farmacologia
Antineoplásicos/síntese química
Antineoplásicos/farmacologia
Limites: Humanos
Animais
Masculino
Camundongos
Tipo de Publ: Estudo Clínico
Responsável: VE497.1 - Biblioteca Dr. Oswaldo Enríquez Isava
VE497.1; D-QM, M6


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Id: biblio-1041531
Autor: Wu, Wanting; Liang, Yuan; Wu, Guangchao; Su, Yinghang; Zhang, Hongying; Zhang, Zhenyan; Deng, Changsheng; Wang, Qi; Huang, Bo; Tan, Bo; Zhou, Chongjun; Song, Jianping.
Título: Effect of artemisinin-piperaquine treatment on the electrocardiogram of malaria patients
Fonte: Rev. Soc. Bras. Med. Trop;52:e20180453, 2019. tab, graf.
Idioma: en.
Projeto: Guangdong Provincial Chinese Medicine Bureau Project, Guangdong Traditional Chinese Medicine Letter; . Major projects of Guangdong Province; . Science and Technology Program of Guangzhou.
Resumo: Abstract INTRODUCTION: Concern regarding the cardiotoxicity of antimalarials has been renewed because of their potential to cause QT/QTc interval prolongation related to torsade de pointes (TdP). Artemisinin-piperaquine (AP) is considered an effective artemisinin-based combination therapy (ACT) for malaria. METHODS: This study involved a retrospective analysis of clinical data of 93 hospitalized malaria patients who had received AP orally. Electrocardiograms (ECGs) were obtained at specific time points in the original study. RESULTS: Some cases of QT prolongation were observed. However, no TdP was found. CONCLUSIONS: AP may cause QT interval prolongation in some malaria patients but may not lead to TdP.
Descritores: Quinolinas/efeitos adversos
Síndrome do QT Longo/induzido quimicamente
Malária Falciparum/tratamento farmacológico
Artemisininas/efeitos adversos
Antimaláricos/efeitos adversos
-Quinolinas/uso terapêutico
Síndrome do QT Longo/diagnóstico
Estudos Retrospectivos
Artemisininas/uso terapêutico
Quimioterapia Combinada
Eletrocardiografia
Pessoa de Meia-Idade
Antimaláricos/uso terapêutico
Limites: Humanos
Masculino
Feminino
Adulto
Responsável: BR1.1 - BIREME


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Id: biblio-1136875
Autor: Antinarelli, Luciana Maria Ribeiro; Souza, Marcus Vinicius Nora de; Coelho, Eduardo Antonio Ferraz; Lima, Wallace Pacienza; Coimbra, Elaine Soares.
Título: Efficacy of the 7-chloro-4-(3-hydroxy-benzilidenehydrazo)quinoline derivative against infection caused by Leishmania amazonensis
Fonte: Rev. Soc. Bras. Med. Trop;53:e20200091, 2020. graf.
Idioma: en.
Resumo: Abstract INTRODUCTION: The drugs currently available for leishmaniasis treatment have major limitations. METHODS: In vitro and in vivo studies were performed to evaluate the effect of a quinoline derivative, Hydraqui (7-chloro-4-(3-hydroxy-benzilidenehydrazo)quinoline, against Leishmania amazonensis. In silico analyses of absorption, distribution, metabolism, excretion, and toxicity (ADMET) parameters were performed. RESULTS: Hydraqui showed significant in vitro anti-amastigote activity. Also, Hydraqui-treated mice exhibited high efficacy in lesion size (48.3%) and parasitic load (93.8%) reduction, did not cause hepatic and renal toxicity, and showed appropriate ADMET properties. CONCLUSIONS: Hydraqui presents a set of satisfactory criteria for its application as an antileishmanial agent.
Descritores: Quinolinas/uso terapêutico
Leishmania mexicana/efeitos dos fármacos
Leishmaniose Cutânea/tratamento farmacológico
Antiprotozoários/uso terapêutico
-Quinolinas/química
Leishmaniose Cutânea/parasitologia
Modelos Animais de Doenças
Carga Parasitária
Camundongos
Camundongos Endogâmicos BALB C
Limites: Animais
Feminino
Responsável: BR1.1 - BIREME


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Id: biblio-1155593
Autor: Wu, Wanting; Lu, Chenguang; Liang, Yuan; Zhang, Hongying; Deng, Changsheng; Wang, Qi; Xu, Qin; Tan, Bo; Zhou, Chongjun; Song, Jianping.
Título: Electrocardiographic effect of artemisinin-piperaquine, dihydroartemisinin-piperaquine, and artemether-lumefantrine treatment in falciparum malaria patients
Fonte: Rev. Soc. Bras. Med. Trop;54:e05362020, 2021. tab, graf.
Idioma: en.
Projeto: Traditional Chinese Medicine Bureau of Guangdong Province; . Ministry of Science and Technology of the People's Republic of China; . Guangdong province of the People's Republic of China.
Resumo: Abstract INTRODUCTION: Artemisinin-based combination therapy (ACT), such as artemisinin-piperaquine (AP), dihydroartemisinin-piperaquine (DP), and artemether-lumefantrine (AL), is the first-line treatment for malaria in many malaria-endemic areas. However, we lack a detailed evaluation of the cardiotoxicity of these ACTs. This study aimed to analyze the electrocardiographic effects of these three ACTs in malaria patients. METHODS: We analyzed the clinical data of 89 hospitalized patients with falciparum malaria who had received oral doses of three different ACTs. According to the ACTs administered, these patients were divided into three treatment groups: 27 treated with AP (Artequick), 31 with DP (Artekin), and 31 with AL (Coartem). Electrocardiograms and other indicators were recorded before and after the treatment. The QT interval was calculated using Fridericia's formula (QTcF) and Bazett's formula (QTcB). RESULTS: Both QTcF and QTcB interval prolongation occurred in all three groups. The incidence of such prolongation between the three groups was not significantly different. The incidence of both moderate and severe prolongation was not significantly different between the three groups. The ΔQTcF and ΔQTcB of the three groups were not significantly different. The intra-group comparison showed significant prolongation of QTcF after AL treatment. CONCLUSIONS: Clinically recommended doses of DP, AL, and AP may cause QT prolongation in some malaria patients but do not cause torsades de pointes ventricular tachycardia or other arrhythmias.
Descritores: Malária Falciparum/tratamento farmacológico
Artemisininas/efeitos adversos
Malária/tratamento farmacológico
Antimaláricos/efeitos adversos
-Quinolinas
Combinação de Medicamentos
Eletrocardiografia
Artemeter/uso terapêutico
Combinação Arteméter e Lumefantrina/uso terapêutico
Limites: Humanos
Responsável: BR1.1 - BIREME


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Id: biblio-1150907
Autor: Lorenzo Sarmiento, Maria Angelita.
Título: Diseño, síntesis y evaluación biológica de un grupo de pirazinoisoquinolinas y quinolinas con posible actividad esquistosomicida y leishmanicida respectivamente / Design, synthesis and biological evaluation of a group of pyrazinoisoquinolines and quinolines with possible schistosomicidal and leishmanicidal activity respectively.
Fonte: Caracas; s.n; nov. 2012. 419 p. ilus, tab, graf.
Idioma: es.
Tese: Apresentada a Universidad Central de Venezuela. Facultad de Farmacia para obtenção do grau de Doctor.
Resumo: La esquistosomiasis y la leishmaniasis son dos parasitosis con una alta incidencia en el mundo y con la menor cantidad de medicamentos disponibles para sus tratamientos. Para la esquistosomiasis, el praziquantel (PZQ) es la única droga que existe en los actuales momentos contra la enfermedad, mientras que, en el caso de la leishmaniasis, los antimoniales pentavalentes, empleados como drogas de primera línea, son altamente tóxicos o presentan problemas de resistencia. Por ello, esta tesis describe el diseño, la síntesis y los estudios de actividad biológica de un grupo de pirazinoisoquinolinas y quinolinas sustituidas con posible actividad esquistosomicida y leishmanicida respectivamente. Luego de ensayar diversas vías, se logró la síntesis del PZQ y compuestos relacionados (quince compuestos) mediante una secuencia de cinco pasos, con rendimientos entre el 20% y el 60%. El PZQ se obtuvo en un 33%, con un exceso del enantiómero levo, mostrando ser más activo que el PZQ comercial (mezcla racémica). Los compuestos obtenidos, evaluados en cepas de S. mansoni, no mostraron ser más activos que el PZQ, a las dos concentraciones evaluadas. También, se cuantificó la relación entre la estructura química y la actividad biológica (QSAR) de derivados de PZQ reportados en la literatura. En cuanto a los compuestos con posible actividad leishmanicida, también se ensayaron varios métodos de síntesis hasta lograr obtener veintidós quinolínas de los tipos 2-metil, 2-propil, 4-metil-2-propil y 2-alquildiamino con rendimientos entre un 10 y un 70%. Los compuestos evaluados que mostraron una actividad prometedora en promastigotes de L. mexicanafueron la 2-metilquinolina y 6,7-metilendioxi-2-propil-quinolina. En cuanto a los estudios QSAR, no fue posible encontrar una ecuación representativa que relacionara la actividad biológica con la estructura química.

Schistosomiasis and leishmaniasis are two parasitic diseaseswell spread in the world, and at the same time both have very few medications for their treatment. For schistosomiasis, praziquantel (PZQ) is the drug of choice for its treatment, while in the case of leishmaniasis, the pentavalent antimonials used as first line drugs are highly toxic or present resistance problems. This work describes the design, synthesis and biological activity studies of a group of pirazinoisoquinolines and substituted quinolines with a possible schistosomicidal and leishmanicidal activities, respectively. After several intents, it was possible to synthesize PZQ and some related compounds (fifteen) through a sequence of five steps, with yields between 20 and 60%. PZQ was obtained with a yield of 33%, with a levoenantiomeric excess, and showed a better activity than the commercial compound. The related compounds obtained, evaluated against S. mansonistrains did not have an activity comparable to that of PZQ, at the concentrations evaluated. Quantitative structure­activity relationships (QSAR)studieswere also performed with PZQ derivatives reported in the literature.Several ways of synthesis were also probed for the possible leishmanicidal compounds proposed, until it was possible to obtain twenty two quinoline derivatives (of the type 2-methyl-, 2-propyl-, 4-methyl-2-propyl-and 2-alquildiamino-), with yields between10 and 70%. Of the compounds evaluated, two showed promising activity against L. mexicana promastigotes, 2-iimethylquinoline and 6,7-methylendioxi-2-propyl-quinoline. QSAR studies with these compounds did not yield a representative model for the set.
Descritores: Doenças Parasitárias
Doenças Parasitárias/prevenção & controle
Infecções por Protozoários/parasitologia
Quinolinas/síntese química
Esquistossomose/fisiopatologia
Leishmaniose/fisiopatologia
-Doenças Parasitárias/tratamento farmacológico
Praziquantel/uso terapêutico
Praziquantel/química
Schistosoma mansoni/parasitologia
Leishmania mexicana/parasitologia
Relação Quantitativa Estrutura-Atividade
Limites: Humanos
Tipo de Publ: Protocolo de Ensaio Clínico
Responsável: VE497.1 - Biblioteca Dr. Oswaldo Enríquez Isava
VE497.1; D-QM, L6


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Id: biblio-950900
Autor: Niu, Xiao-Ling; Hou, Jian-Feng; Li, Jing-Xiang.
Título: The NK1 receptor antagonist NKP608 inhibits proliferation of human colorectal cancer cells via Wnt signaling pathway
Fonte: Biol. Res;51:14, 2018. graf.
Idioma: en.
Projeto: Shanghai Pudong New Area Zhoupu Hospital College; . Shanghai Pudong New Area Health System.
Resumo: BACKGROUND: Neurokinin1 (NK1) receptor has played a vital role in the development of tumor. However, NKP608 as a NK1 receptor antagonist whether has the effect of the resistance of colorectal cancer is still unclear. Thereby, in this study, we investigated the role of NKP608 on human colorectal cancer and explored the underlying mechanism. METHODS: The cell proliferation of colorectal cancer cells was detected by cell counting kit-8 (CCK8) assay, cell migration and invasion were assessed by transwell assay, the apoptotic ratio of cells was assessed by Annexin V-fluorescein isothiocyanate/propidium iodide stained and flow cytometry. The involvement of molecular mechanisms was examined by western blot. RESULTS: In this study, we found that NKP608 inhibited the proliferation, migration/invasion of HCT116 cells. In addition, NKP608 reduced expressions of Wnt-3a, ß-catenin, Cyclin D1, and (vascular endothelial growth factor) VEGF while induced expression of E-Cadherin. Furthermore, flow cytometry analyzed that NKP608 induced apoptosis of HCT116 cells, consistently, western blotting detecting of apoptosis-related proteins revealed that NKP608 downregulated Bcl-2 while upregulated Bax and Active-Caspase-3. CONCLUSIONS: Taken together, our results demonstrated that NKP608 inhibited colorectal cancer cell proliferation, migration and invasion via suppressing the Wnt/ß-catenin signaling pathway. Therefore, NKP608 might represent a promising therapeutic agent in the treatment of colorectal cancer.
Descritores: Piperidinas/farmacologia
Quinolinas/farmacologia
Neoplasias Colorretais/patologia
Movimento Celular/efeitos dos fármacos
Proliferação de Células/efeitos dos fármacos
Via de Sinalização Wnt/efeitos dos fármacos
Antagonistas dos Receptores de Neurocinina-1/farmacologia
-Regulação para Baixo/efeitos dos fármacos
Western Blotting
Linhagem Celular Tumoral
Células HCT116
Citometria de Fluxo
Limites: Humanos
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-1089372
Autor: Shen, Congxiang; Chen, Fang; Wang, Huigang; Zhang, Xinyu; Li, Guanxue; Wen, Zhong.
Título: Individualized treatment for allergic rhinitis based on key nasal clinical manifestations combined with histamine and leukotriene D4 levels / Tratamento individualizado para a rinite alérgica baseado nas principais manifestações clínicas nasais e dos níveis de histamina e leucotrieno D4
Fonte: Braz. j. otorhinolaryngol. (Impr.);86(1):63-73, Jan.-Feb. 2020. tab, graf.
Idioma: en.
Projeto: Science and Technology Program Project of Guangdong Province.
Resumo: Abstract Introduction The types of allergic rhinitis are roughly classified based on the causative antigens, disease types, predilection time, and symptom severity. Objective To examine the clinical typing and individualized treatment approach for allergic rhinitis and to determine the optimal treatment method for this disease using various drug combination therapies. Methods A total of 108 participants with allergic rhinitis were divided into three groups based on symptoms. Subsequently, each group was further categorized into four subgroups based on the medications received. The efficacy of the treatments was evaluated using the visual analog scale VAS scores of the total and individual nasal symptoms, decline index of the symptom score, histamine and leukotriene levels, and mRNA and protein expression levels of histamine 1 and cysteinyl leukotriene 1 receptors. Results Loratadine + mometasone furoate and loratadine + mometasone furoate + montelukast significantly improved the sneezing symptom and reduced the histamine levels compared with the other combination therapies (p < 0.05). Meanwhile, montelukast + mometasone furoate and montelukast + mometasone furoate + loratadine considerably improved the nasal obstruction symptom and decreased the leukotriene D4 levels compared with the other combination therapies (p < 0.05). Conclusion Clinical symptom evaluation combined with experimental detection of histamine and leukotriene levels can be an objective and accurate method to clinically classify the allergic rhinitis types. Furthermore, individualized treatment based on allergic rhinitis classification can result in a good treatment efficacy.

Resumo Introdução A rinite alérgica é basicamente classificada de acordo com os antígenos causadores, tipos de doença, peridiocidade e gravidade dos sintomas. Objetivo Avaliar os tipos clínicos e a abordagem terapêutica individualizada para cada tipo de rinite alérgica e determinar o método de tratamento ideal utilizando várias terapias de combinação de fármacos. Método Um total de 108 participantes com rinite alérgica foram divididos em três grupos com base nos sintomas. Posteriormente, cada grupo foi subsequentemente categorizado em quatro subgrupos com base nos medicamentos recebidos. A eficácia dos tratamentos foi avaliada utilizando os escores da escala visual analógica EVA dos sintomas nasais totais e individualmente, índice de declínio do escore de sintomas, níveis de histamina e leucotrienos e níveis de expressão de mRNA e proteína dos receptores de histamina 1 e cisteinil-leucotrieno 1. Resultados As associações entre loratadina + furoato de mometasona, assim como a de loratadina + furoato de mometasona + montelucaste melhoraram significativamente o sintoma de espirros e reduziram os níveis de histamina em comparação às outras terapias combinadas (p < 0,05). Por outro lado, a associação montelucaste + furoato de mometasona, assim como a associação montelucaste + furoato de mometasone + loratadina melhoraram consideravelmente o sintoma de obstrução nasal e diminuíram os níveis de leucotrieno D4 em comparação com as outras combinações (p < 0,05). Conclusão A avaliação clínica dos sintomas combinada com a detecção experimental dos níveis de histamina e leucotrieno pode ser um método objetivo e preciso para classificar clinicamente os tipos de rinite alérgica. Além disso, o tratamento individualizado baseado na classificação da rinite alérgica pode resultar no aumento da eficácia do tratamento.
Descritores: Histamina/sangue
Leucotrieno D4/sangue
Quimioterapia Combinada/métodos
Medicina de Precisão/métodos
Rinite Alérgica/sangue
-Quinolinas/uso terapêutico
Espirro
RNA Mensageiro/genética
Receptores Histamínicos H1/genética
Obstrução Nasal/tratamento farmacológico
Resultado do Tratamento
Loratadina/uso terapêutico
Receptores de Leucotrienos/genética
Antialérgicos/uso terapêutico
Rinite Alérgica/diagnóstico
Rinite Alérgica/tratamento farmacológico
Furoato de Mometasona/uso terapêutico
Acetatos/uso terapêutico
Mucosa Nasal
Limites: Humanos
Masculino
Feminino
Adolescente
Adulto
Pessoa de Meia-Idade
Idoso
Adulto Jovem
Tipo de Publ: Ensaio Clínico Controlado
Responsável: BR1.1 - BIREME


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Id: biblio-983805
Autor: Pitoia, Fabián; Schmidt, Angélica; Bueno, Fernanda; Abelleira, Erika; Jerkovich, Fernando.
Título: Rare complications of multikinase inhibitor treatment
Fonte: Arch. endocrinol. metab. (Online);62(6):636-640, Dec. 2018. tab, graf.
Idioma: en.
Resumo: ABSTRACT Objective: The advent of multikinase inhibitor (MKI) therapy has led to a radical change in the treatment of patients with advanced thyroid carcinoma. The aim of this manuscript is to communicate rare adverse events that occurred in less than 5% of patients in clinical trials in a subset of patients treated in our hospital. Subjects and methods: Out of 760 patients with thyroid cancer followed up with in our Division of Endocrinology, 29 (3.8%) received treatment with MKIs. The median age at diagnosis of these patients was 53 years (range 20-70), and 75.9% of them were women. Sorafenib was prescribed as first-line treatment to 23 patients with differentiated thyroid cancer and as second-line treatment to one patient with advanced medullary thyroid cancer (MTC). Vandetanib was indicated as first-line treatment in 6 patients with MTC and lenvatinib as second-line treatment in two patients with progressive disease under sorafenib treatment. Results: During the follow-up of treatment (mean 13.7 ± 7 months, median 12 months, range 6-32), 5/29 (17.2%) patients presented rare adverse events. These rare adverse effects were: heart failure, thrombocytopenia, and squamous cell carcinoma during sorafenib therapy and squamous cell carcinoma and oophoritis with intestinal perforation during vandetanib treatment. Conclusions: About 3 to 5 years after the approval of MKI therapy, we learned that MKIs usually lead to adverse effects in the majority of patients. Although most of them are manageable, we still need to be aware of potentially serious and rare or unreported adverse effects that can be life-threatening.
Descritores: Piperidinas/efeitos adversos
Quinazolinas/efeitos adversos
Carcinoma/tratamento farmacológico
Carcinoma Medular/tratamento farmacológico
Inibidores de Proteínas Quinases/efeitos adversos
Antineoplásicos/efeitos adversos
-Ooforite/induzido quimicamente
Compostos de Fenilureia/efeitos adversos
Quinolinas/efeitos adversos
Trombocitopenia/induzido quimicamente
Fatores de Tempo
Neoplasias da Glândula Tireoide/tratamento farmacológico
Estudos Retrospectivos
Fatores de Risco
Seguimentos
Estimativa de Kaplan-Meier
Sorafenibe/efeitos adversos
Insuficiência Cardíaca/induzido quimicamente
Perfuração Intestinal/induzido quimicamente
Limites: Humanos
Masculino
Feminino
Adulto
Pessoa de Meia-Idade
Idoso
Adulto Jovem
Responsável: BR1.1 - BIREME


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Id: biblio-886663
Autor: WILHELM, ETHEL A; FERREIRA, ANA TERESINHA; PINZ, MIKAELA P; REIS, ANGÉLICA S DOS; VOGT, ANE G; STEIN, ANDRE L; ZENI, GILSON; LUCHESE, CRISTIANE.
Título: Antioxidant effect of quinoline derivatives containing or not selenium: Relationship with antinociceptive action quinolines are antioxidant and antinociceptive
Fonte: An. acad. bras. ciênc;89(1,supl):457-467, May. 2017. graf.
Idioma: en.
Projeto: Universidade Federal de Pelotas, Universidade Federal de Santa Maria, Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) and Fundação de Amparo à Pesquisa do Estado do Rio Grande do Sul (FAPERGS)/CNPq (PRONEX).
Resumo: ABSTRACT The present study investigated the antioxidant effect of a new class of quinoline derivatives (a-d) on assays in vitro. Lipid peroxidation, thiol peroxidase-like and free radical scavenging activities were determined to evaluate antioxidant activity of compounds. Thiol oxidase-like and δ-aminolevulinate dehydratase activities were performed as a toxicological parameter. A second objective of this study was to evaluate the in vivo antinociceptive effect of the compound with better antioxidant effect and without toxic effects in a model of nociception induced by formalin in mice. In liver, at 100 µM, compound a reduced the lipid peroxidation to the control levels, while compounds c and d partially reduced it. In brain, only compound d partially reduced the lipid peroxidation at 50 and 100 µM. Compound b did not have an effect on the lipid peroxidation. Thiol peroxidase-like and free radical scavenging activities are not involved in the antioxidant mechanisms of these compounds. Compounds did not present thiol oxidase-like activity and effect on the δ-aminolevulinate dehydratase. In vivo experiments showed that compound a caused an inhibition of licking time in the first and second phases, and edema formation induced by formalin. In conclusion, quinoline derivative without selenium presented better in vitro antioxidant effect and in vivo antinociceptive activity.
Descritores: Quinolinas/farmacologia
Selênio/farmacologia
Estresse Oxidativo/efeitos dos fármacos
Analgésicos/farmacologia
Antioxidantes/farmacologia
-Oxirredução
Quinolinas/química
Medição da Dor
Sequestradores de Radicais Livres
Modelos Animais de Doenças
Oxirredutases atuantes sobre Doadores de Grupo Enxofre/farmacologia
Sintase do Porfobilinogênio/farmacologia
Limites: Animais
Masculino
Ratos
Responsável: BR1.1 - BIREME


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Id: lil-792413
Autor: Melekoglu, Rauf; Ciftci, Osman; Cetin, Aslı; Basak, Nese; Celik, Ebru.
Título: The beneficial effects of Montelukast against 2 3 7 8 tetrachlorodibenzo dioxin toxicity in female reproductive system in rats
Fonte: Acta cir. bras;31(8):557-563, Aug. 2016. tab, graf.
Idioma: en.
Resumo: ABSTRACT PURPOSE: To determine the toxic effect of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) on reproductive system and the beneficial effects of Montelukast (ML) with histological and biochemical analysis. METHODS: Rats were randomly divided into four equal groups (control, TCDD, ML and TCDD+ML). Tissue samples were collected on day 60 and oxidative status and histological alterations were analyzed. RESULTS: The results showed a significant increase in oxidative and histological damage on uterine and ovarian tissues. Otherwise, the oxidative and histological damages caused by TCDD were prevented with ML treatment. CONCLUSION: The toxic effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin on female reproductive system were reversed with Montelukast treatment. Therefore, we claimed that ML treatment might be useful for TCDD toxicity.
Descritores: Ovário/efeitos dos fármacos
Quinolinas/farmacologia
Estresse Oxidativo/efeitos dos fármacos
Dibenzodioxinas Policloradas/toxicidade
Acetatos/farmacologia
Antioxidantes/farmacologia
-Ovário/patologia
Superóxido Dismutase/metabolismo
Útero/patologia
Catalase/metabolismo
Distribuição Aleatória
Ratos Wistar
Glutationa/metabolismo
Folículo Ovariano/efeitos dos fármacos
Limites: Animais
Feminino
Ratos
Responsável: BR1.1 - BIREME



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