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Id: biblio-889115
Autor: Qiu, Zhenpeng; Zhou, Junxuan; Zhang, Cong; Cheng, Ye; Hu, Junjie; Zheng, Guohua.
Título: Antiproliferative effect of urolithin A, the ellagic acid-derived colonic metabolite, on hepatocellular carcinoma HepG2. 2. 15 cells by targeting Lin28a/let-7a axis
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;51(7):e7220, 2018. tab, graf.
Idioma: en.
Projeto: Hubei Provincial Department of Education.
Resumo: An abnormality in the Lin28/let-7a axis is relevant to the progression of hepatitis B virus (HBV)-positive hepatocellular carcinoma (HCC), which could be a novel therapeutic target for this malignant tumor. The present study aimed to investigate the antiproliferative and anti-invasive effects of urolithin A in a stable full-length HBV gene integrated cell line HepG2.2.15 using CCK-8 and transwell assays. The RNA and protein expressions of targets were assessed by quantitative PCR and western blot, respectively. Results revealed that urolithin A induced cytotoxicity in HepG2.2.15 cells, which was accompanied by the cleavage of caspase-3 protein and down-regulation of Bcl-2/Bax ratio. Moreover, urolithin A suppressed the protein expressions of Sp-1, Lin28a, and Zcchc11, and elevated the expression of microRNA let-7a. Importantly, urolithin A also regulated the Lin28a/let-7a axis in transient HBx-transfected HCC HepG2 cells. Furthermore, urolithin A decelerated the HepG2.2.15 cell invasion, which was involved in suppressing the let-7a downstream factors HMGA2 and K-ras. These findings indicated that urolithin A exerted the antiproliferative effect by regulating the Lin28a/let-7a axis and may be a potential supplement for HBV-infected HCC therapy.
Descritores: Proteínas de Ligação a RNA/efeitos dos fármacos
Carcinoma Hepatocelular/tratamento farmacológico
Cumarínicos/farmacologia
MicroRNAs/efeitos dos fármacos
Neoplasias Hepáticas/tratamento farmacológico
-Valores de Referência
Sincalida/análise
Fatores de Tempo
Replicação Viral/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Western Blotting
Reprodutibilidade dos Testes
Análise de Variância
Proteínas de Ligação a RNA/análise
Carcinoma Hepatocelular/genética
Carcinoma Hepatocelular/virologia
MicroRNAs/análise
Proliferação Celular/efeitos dos fármacos
Células Hep G2
Reação em Cadeia da Polimerase em Tempo Real
Neoplasias Hepáticas/genética
Neoplasias Hepáticas/virologia
Limites: Seres Humanos
Responsável: BR1.1 - BIREME


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Id: biblio-1001583
Autor: El-Sharkawy, Karam Ahmed; AlBratty, Mohammed Mofreh; Alhazmi, Hassan Ahmad.
Título: Synthesis of some novel pyrimidine, thiophene, coumarin, pyridine and pyrrole derivatives and their biological evaluation as analgesic, antipyretic and anti-inflammatory agents
Fonte: Braz. J. Pharm. Sci. (Online);54(4):e00153, 2018. tab, graf.
Idioma: en.
Resumo: Pyrimidine derivative 3 was afforded through the reaction of compound (1) with 5-ureidohydantion (2). Product 3 underwent a cyclization to produce fused pyrimidine derivative 7, although the latter product 7 was synthesized through one step via the reaction of compound (1) with 5-ureidohydantion (2) using another catalyst. Compound 3 was oriented to react with cyclic ketones 8a,b in the presence of elemental sulfur, salicylaldehyde (10), aryldiazonium chlorides 12a,b and ω-bromo-4-methoxy- acetophenone (14), which afforded, fused thiophene derivatives 9a,b, coumarin derivative 11, arylhdrazono derivatives 13a,b and 4-methoxyphenyl butenyl derivative 15, respectively. The latter product 15 was reacted with either potassium cyanide (16a) or potassium thiocyanide (16b) to form cyano and thiocyano derivatives 17a,b, respectively. Compound 17a underwent further cyclization to afford pyridopyrimidine derivative 19. Compound 15 was reacted with either hydrazine (20a) or phenylhydrazine (20b) to produce hydrazo derivatives 21a,b and these products were cyclize to produce pyrrole derivatives 23a,b. Finally, 5-ureidohydantion (2) was reacted with compounds 24a,b,c to afford pyrimidine derivatives 25a,b,c. The structures of the synthesized compounds were confirmed using IR, 1H NMR, 13C NMR and mass spectrometry techniques. Compounds 11 and 19 have promising as analgesic and antipyretic activities
Descritores: Piridinas/análise
Pirimidinas/agonistas
Pirróis
Tiofenos/análise
Cumarínicos/análise
-Antipiréticos
Analgésicos/classificação
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Simöes, Cláudia Maria Oliveira
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Id: biblio-839460
Autor: Cárdenas, Paola Andrea; Kratz, Jadel Müller; Hernández, Aura; Costa, Geison Modesti; Ospina, Luis Fernando; Baena, Yolima; Simões, Cláudia Maria Oliveira; Jimenez-Kairuz, Álvaro; Aragon, Marcela.
Título: In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats
Fonte: Braz. J. Pharm. Sci. (Online);53(1):e16081, 2017. tab, graf.
Idioma: en.
Projeto: CAPES.
Resumo: ABSTRACT 6-Methylcoumarin (6MC) is a semisynthetic coumarin with important in vitro and in vivo anti-inflammatory activity. In order to continue the pre-clinical characterization of this molecule, in vitro intestinal permeability, plasma profile and tissue distribution after oral administration in rats were studied. The permeability of 6MC was evaluated by the Caco-2 cellular model in both the apical-basal (A-B) and basal-apical (B-A) directions. The pharmacokinetics and biodistribution were evaluated in rats after oral and intraperitoneal administration at doses of 200 mg/kg. Transport experiments with Caco-2 cells showed that 6MC presented high permeability at all concentrations evaluated. This finding suggested that 6MC could be transported across the gut wall by passive diffusion. The plasma concentration-time curve showed that the maximum concentration (Cmax) was 17.13 ± 2.90 µg/mL at maximum time (Tmax) of 30 min for the oral route and Cmax 26.18 ± 2.47 µg/mL at 6.0 min for the intraperitoneal administration, with elimination constant of (Ke ) 0.0070 min-1 and a short life half time of (T1/2 ) lower that 120 min. The distribution study showed that 6MC has high accumulation in the liver, and widespread distribution in all the organs evaluated.
Descritores: Permeabilidade
Técnicas In Vitro/instrumentação
Administração Oral
Ratos Wistar/classificação
Cumarínicos/análise
-Farmacocinética
Absorção Peritoneal
Enteropatias/classificação
Limites: Animais
Masculino
Feminino
Ratos
Tipo de Publ: Técnicas In Vitro
Responsável: BR1.1 - BIREME


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Id: biblio-987181
Autor: García Zebadúa, Julio César; Reyes Chilpa, Ricardo.
Título: El árbol tropical Calophyllum brasiliense: una revisión botánica, química y farmacológica / The tropical tree Calophyllum brasiliense: a botanical, chemical and pharmacological review
Fonte: Vitae (Medellín);21(2):126-145, 2014. Ilustraciones.
Idioma: es.
Resumo: Antecedentes: Calophyllum brasiliense Cambess. Es un árbol de la familia Calophyllaceae, separada recientemente de Clusiaceae (Guttiferae). Se distribuye ampliamente en selvas tropicales lluviosas del continente americano, desde Brasil hasta México. Esta especie sintetiza diversos metabolitos secundarios en hojas, flores, frutos, corteza y raíz, tales como cumarinas, cromanonas, xantonas, terpenos, flavonoides y compuestos fenólicos, los cuales presentan múltiples propiedades biológicas. Objetivos: Ofrecer una visión general de las características botánicas, químicas y farmacológicas de C. brasiliense, así como evidencias químicas, anatómicas y genéticas que sugieren la existencia de quimiotipos (fenotipos químicos) en la especie. Métodos: Se revisó la información disponible en las bases de datos NCBI y SciFinder®, se seleccionaron investigaciones relevantes que permitieron conocer los compuestos químicos aislados y su actividad biológica. Resultados: Entre los compuestos sintetizados por C. brasiliense destacan calanólidos e inofilums, especialmente el (+)-calanólido A, como inhibidores potentes de la enzima transcriptasa reversa del virus de inmunodeficiencia humana tipo 1 (VIH-1) y baja toxicidad a linfocitos humanos. El (+)-calanólido A, una dipiranocumarina tetracíclica, podría ser el primer fármaco de origen natural aprobado por la FDA (EUA) en el tratamiento del VIH/SIDA. Otros compuestos, tales como cumarinas tipo mammea, cromanonas, xantonas y triterpenos, mostraron actividad contra protozoarios, células tumorales humanas, como bactericidas y antiespasmódicos. La actividad más importante de cumarinas tipo mammea es contra protozoarios como Leishmania y Trypanosoma. En relación a L. amazonensis, destacó (-)-mammea A/BB presentando buena actividad y selectividad contra amastigotes y promastigotes, y baja toxicidad en macrófagos humanos. La (-)-mammea A/BA, y las xantonas preniladas mostraron alta citotoxicidad sobre líneas celulares tumorales humanas y T. cruzi. Las evidencias químicas, anatómicas y genéticas indican que existen quimiotipos en C. brasiliense, sugiriendo un proceso de especiación en curso en el taxón. Las secuencias ribosomales (ITS) discriminaron al quimiotipo 1 (produce coumarinas tipo mammea) de los quimiotipos 2 y 3 (biosintetizan calanólidos e inofilums), siendo útiles como posibles códigos de barras. Conclusiones: El adecuado manejo de C. brasiliense mediante técnicas silvícolas y biotecnológicas, así como el conocimiento científico y tecnológico, podrían aportar soluciones a países en desarrollo, por ejemplo mediante producción de fitomedicamentos, a enfermedades como el VIH/ SIDA, Leshmaniasis y la Enfermedad de Chagas.

Rationale: Calophyllum brasiliense Cambess. Is a tree belonging to Calophyllaceae family, recently separated from Clusiaceae (= Guttiferae). This species is widely distributed in the Tropical Rain Forests of the American continent, from Brazil to Mexico. It synthesizes a wide variety of secondary metabolites isolated from leaves, flowers, fruits, bark and roots, such as coumarins, chromanones, xanthones, terpenes,flavonoids and phenolic compounds, which exhibit multiple biological properites. Objective: To provide a comprehensive view of the botanical, chemical and pharmacological characteristics of C. brasiliense, and to present chemical, anatomical and genetic evidences supporting the notion of chemotypes (chemical phenotypes) in this species. Methods: Information available in the databases NCBI and SciFinder® was reviewed, and relevant investigations were selected regarding to chemical compounds isolated and their biological activity. Results: Among compounds synthesized by C. brasiliense, calanolides and inophyllums stand out, specially (+)-calanolide A, since these can inhibit reverse transcriptase of human immunodeficiency virus type 1 (HIV-1). (+)-Calanolide A, a tetracyclic dipyranocoumarin, could be the first drug of natural origin approved by the FDA (US) in the treatment of HIV/AIDS. Other compounds, such as mammea type-coumarins, chromanones, xanthones, and triterpenes showed antitumor, antiparasitic, antibacterial and antispasmodic activity. Most important activity of mammea type-coumarins is against protozoa, such as Leishmania, and Trypanosoma. Regarding to L. amazonensis, (-)-mammea A/BB stands out, being highly potent and selective against amastigotes, and promastigotes, but poorly toxic to human macrophages. (-)-Mammea A/BA as well as prenylated xanthones showed high citotoxicity against human tumor cell lines and T. cruzi. The chemical, anatomical and genetical evidences supported the idea of chemotypes in C. brasiliense, suggesting a current process of speciation in this taxon. The ribosomal ITS sequences discriminate chemotype 1 (produces mammea type coumarins) from chemotypes 2 and 3(synthesize calanolides and inophyllums) being useful like possible barcodes. Conclusions: The proper management of Calophyllum brasiliense with forestry and biotechnological methods, as well as scientific and technological knowledge, could provide solutions to developing countries, for instance through the production of phytomedicines against HIV/AIDS, and illnesses caused by protozoa such as Leshmaniasis and Chaga's Disease.
Descritores: HIV
-Botânica
Leishmaniose
Cumarínicos
Xantonas
Limites: Seres Humanos
Tipo de Publ: Artigo Clássico
Responsável: CO56.3 - Biblioteca


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Texto completo SciELO Chile
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Id: biblio-899662
Autor: Nazar J, Claudio; Cárdenas C, Antonia; Coloma D, Roberto; Contreras C, José Ignacio; Molina, Ian; Miranda H, Pablo; Fuentes H, Ricardo.
Título: Manejo perioperatorio de pacientes con tratamiento anticoagulante crónico / Perioperative management of patients with chronic anticoagulant therapy
Fonte: Rev. chil. cir;70(1):84-91, 2018. tab, ilus.
Idioma: es.
Resumo: Resumen La terapia anticoagulante es ampliamente utilizada en la práctica clínica, como profilaxis en pacientes con riesgo de presentar fenómenos tromboembólicos o como tratamiento en aquellos que han presentado algún evento trombótico. Cada vez es más frecuente enfrentarse a pacientes en tratamiento anticoagulante crónico que serán intervenidos mediante procedimientos quirúrgicos, por lo que es importante y necesario conocer el manejo perioperatorio de los diferentes fármacos anticoagulantes, para disminuir los riesgos y complicaciones asociados a la suspensión o mantención de estos en el período perioperatorio. Para lograr este objetivo se debe evaluar y balancear el riesgo de sangrado versus el riesgo de eventos tromboembólicos, considerando la condición médica de cada paciente y el tipo de procedimiento quirúrgico que recibirá. La recomendación para fármacos anticoagulantes orales antagonistas de vitamina K es mantenerlos en cirugías con bajo riesgo de sangrado y suspenderlos 5 días antes de procedimientos quirúrgicos con riesgo hemorrágico moderado y alto, controlando el international normalized ratio el día previo a la cirugía. Los nuevos anticoagulantes orales no requieren monitorización de rutina, recomendándose suspenderlos a las 24-96 h previas al procedimiento quirúrgico, dependiendo del riesgo hemorrágico de cada cirugía y de la función renal. En relación con los anticoagulantes parenterales, la heparina no fraccionada en infusión intravenosa se recomienda suspenderla 4-5 h antes de la cirugía, mientras que la utilizada vía subcutánea, 12 h previas a la intervención quirúrgica. Las heparinas de bajo peso molecular en dosis de tratamiento se sugiere descontinuarlas 24 h previas a la cirugía, mientras que las usadas en dosis profilácticas, solo 12 h antes.

Anticoagulant therapy is widely used in clinical practice, as prophylaxis in patients at risk of presenting thromboembolic phenomena or as treatment in those who have presented a thrombotic event. It is increasingly the number of patients on chronic anticoagulant therapy to undergo surgical procedures, so it is important and necessary to know the perioperative management of the different anticoagulant drugs to reduce the risks and complications associated with suspension or maintenance of these in the perioperative period. To achieve this goal, the risk of bleeding should be evaluated and balanced against the risk of thromboembolic events, considering the medical condition of each patient and the type of surgical procedure to which they have undergone. The recommendation for vitamin K antagonist oral anticoagulant drugs is to maintain them for surgeries at low risk of bleeding and to suspend them 5 days before surgical procedures with moderate and high bleeding risk, controlling 'International Normalized Ratio' the day before surgery. The new oral anticoagulants do not require routine monitoring, recommending suspending them 24-96 h prior to the surgical procedure, depending on the hemorrhagic risk of each surgery and renal function of patient. In relation to parenteral anticoagulants, unfractionated heparin in intravenous infusion is recommended to be discontinued 4-5 h prior to surgery, while the subcutaneous route, 12 h prior to surgery. Low-molecular-weight heparins in treatment doses should be suspended 24 h prior to surgery, while in prophylactic doses, only 12 h earlier.
Descritores: Assistência Perioperatória/métodos
Anticoagulantes/administração & dosagem
-Complicações Pós-Operatórias/prevenção & controle
Vitamina K/antagonistas & inibidores
Heparina/administração & dosagem
Administração Oral
Medição de Risco
Cumarínicos/administração & dosagem
Inibidores do Fator Xa/administração & dosagem
Hemorragia/prevenção & controle
Limites: Seres Humanos
Tipo de Publ: Revisão
Responsável: CL61.1 - Biblioteca Central Campus Sur


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Id: biblio-995573
Autor: Moreno, Laura M; Cuca, Luis E; Guerrero, Mario F.
Título: Serotonergic-like profile of 4-propyl-2hbenzo[h]-chromen-2-one (FCS-304) in mice and rats / Perfil de tipo serotoninérgico de 4-propil-2h-benzo[h]-cromen-2-ona (FCS-304) en ratones y ratas
Fonte: Vitae (Medellín);26(1):17-22, 2019. Ilustraciones.
Idioma: en.
Resumo: Background: 4-propil-2H-benzo[h]-cromen-2-ona (FCS-304) is a semisynthetic coumarin with MAO-A inhibitory activity and positive results in forced swimming and tail suspension test in mice, but until now, it has not been studied in other screening antidepressant models in mice and rats. Objectives: The aim of this work was to assess the serotonin like effect of FCS-304 in the 5-hydroxytryptophan (5-HTP) test in mice, in the behavioral despair test in rats, and in the reserpine test in rats. Methods: Potentiation of 5-HTP (100 mg/kg, i.p.), induced head twitches were assessed in mice, previously treated with FCS-304 (50-75-150 mg/kg, p.o.). The behavioral despair test was performed in rats treated with FCS-304, recording the immobility time attained by the animals subjected to forced swimming. Antagonism of reserpine-induced ptosis was examined in rats, assessing the level of palpebral closure. Imipramine (30 mg/kg, p.o.) and vehicle (canola oil) served as positive and negative controls, respectively. Results: FCS-304 significantly potentiated 5-HTP induced head twitches in mice, in a dose dependent manner. In rats, FCS-304 significantly decreased the immobility time in the behavioral despair test and antagonized reserpine induced ptosis. Conclusions: These results add support to propose that FCS-304 could elicit antidepressant effects related to MAO-A inhibitory activity.

Antecedentes: 4-propil-2H-benzo[h]-cromen-2-ona (FCS-304) es una cumarina semisintética inhibidora de MAO-A con efectos positivos en las pruebas de nado forzado y suspensión por la cola en ratones, sin embargo, hasta ahora no se había estudiado en otros modelos de tamizado antidepresivo en ratones y ratas. Objetivos: el objetivo de este trabajo fue evaluar el efecto de tipo serotoninérgico de FCS-304 en la prueba de potenciación de 5-hidroxitriptofano (5-HTP) en ratones, y su respuesta en la prueba de desesperanza conductual en ratas y en la prueba de reserpina en ratas. Métodos: se evaluó la potenciación de las sacudidas de cabeza inducidas por 5-HTP (100 mg/kg, i.p.), en ratones tratados con FCS-304 (50-75-150 mg/Kg, v.o.). La prueba de desesperanza conductual se realizó en ratas tratadas con FCS-304, expuestas a nado forzado. El antagonismo de la ptosis palpebral inducida por reserpina se examinó en ratas determinando el grado de apertura ocular. Imipramina (30 mg/kg, v.o.) y el vehículo (aceite de canola, 0,1 mL/10 g), sirvieron como controles positivo y negativo, respectivamente. Resultados: FCS-304 incrementó significativamente el recuento de sacudidas de cabeza inducidas por 5-HTP en ratones, en función de la dosis. En ratas, FCS-304 fue efectiva para disminuir el tiempo de inmovilidad en la prueba de desesperanza inducida por nado forzado y el grado de ptosis palpebral inducido por reserpina. Conclusiones: estos resultados dan soporte para proponer que FCS-304 ejercería efectos de tipo antidepresivo relacionados con la inhibición de MAO-A.
Descritores: Ratos
Serotoninérgicos
-5-Hidroxitriptofano
Cumarínicos
Antidepressivos
Limites: Seres Humanos
Tipo de Publ: Artigo Clássico
Responsável: CO56.3 - Biblioteca


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Texto completo SciELO Cuba
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Id: lil-740921
Autor: Rodríguez Chanfrau, Jorge Enrique; Rodríguez Ferrada, Carlos.
Título: Harvest time influences on coumarin and umbelliferone contents in extracts of Justicia pectoralis Jacq. (tilo) / Influencia del tiempo de cosecha sobre el contenido de cumarina y de umbeliferon hallado en los extractos de Justicia pectoralis Jacq. (tilo)
Fonte: Rev. cuba. farm;48(3):477-485, jul.-set. 2014. tab, Ilus.
Idioma: en.
Resumo: INTRODUCTION: Justicia pectoralis Jacq. (Acanthaceae) is medicinal plant species commonly used in Cuba for the treatment of nervous disorders because of its sedative effect. Coumarin is one of its main active phytochemicals present in the extracts obtained from this plant and used as analytic marker in quality control. On the other hand, this compound contributes to the sedative effect attributed to this plant. OBJECTIVE: to evaluate the influence of harvest time on the coumarin and umbelliferone (7-hydroxycoumarin) in Justicia pectoralis extracts. METHODS: the experiment lasted two years. The harvest was performed at 4, 6 and 8 months after planting. Aqueous and hydroalcohol extracts were produced and the coumarin and umbelliferone contents were determined by high resolution liquid chromatography. RESULTS: the achieved results showed the presence of coumarin and umbelliferone in both extracts. Both methods can be used for the extraction of these components from the plant, although in the case of umbelliferone, the best extraction results were achieved by using aqueous extract. In both cases, the recovery percentages were more than 98 %. This study confirmed that the harvest time significantly influences on the coumarin and umbelliferone contents. CONCLUSIONS: the best results are observed in the first two harvests (4 and 6 months at summer time), which indicates that the industry should process the vegetal material in these two periods of the year.

INTRODUCCIÓN: Justicia pectoralis Jacq. (Acanthaceae) es una planta medicinal comúnmente usada en Cuba para el tratamiento de enfermedades nerviosas por su efecto sedante. La cumarina es uno de los fitocomponentes mayoritarios en los extractos obtenidos con esta planta y empleado como marcador analítico en los controles de calidad. Por otro lado, este componente contribuye con el efecto sedante atribuido a esta planta. OBJETIVO: evaluar la influencia del tiempo de cosecha sobre el contenido de cumarina y umbelliferona (7 hidroxicumarina) en extractos de Justicia pectoralis. MÉTODOS: se desarrolló el experimento durante 2 años. Se realizaron las cosechas a los 4, 6 y 8 meses de plantada. Se elaboraron extractos acuosos e hidroalcohólicos y se determinó el contenido de cumarina y umbelliferone por cromatografía líquida de alta resolución. RESULTADOS: se mostró la presencia de cumarina y umbelliferona en ambos extractos. Además, en el caso de la umbelliferona, los mejores resultados se alcanzaron al aplicar extracción acuosa. En ambos casos, los por cientos de recobrados fueron superiores al 98 % Se confirmó que el tiempo de cosecha influyó significativamente sobre el contenido de cumarina y umbelliferona. CONCLUSIONES: los mejores resultados se obtienen en la primeras dos cosechas (4 y 6 meses que coincide con el verano), lo que sugiere que el material de la planta debe procesarse por la industria en esos periodos del año.
Descritores: Umbeliferonas/farmacologia
Cromatografia Líquida de Alta Pressão/métodos
Cumarínicos/farmacologia
Responsável: CU1.1 - Biblioteca Médica Nacional


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Id: biblio-911729
Autor: Garibello Rubiano, Carlos Felipe.
Título: Estudio de hojas de Pentacalia vaccinioides (Kunth) cuatr como nueva fuente natural de sustancias esteroidales y cumarinas / Study of leaves of Pentacalia vaccinioides (Kunth) cuatr as a new natural source of steroidal substances and coumarins.
Fonte: Bogotá; s.n; 2010. [89] p. graf.
Idioma: es.
Tese: Apresentada a Pontificia Universidad Javeriana para obtenção do grau de Maestría.
Resumo: Objetivo. Reconocer la especie Pentacalia vaccinioides (Kunth) Cuatr como una nueva fuente natural de sustancias esteroidales y cumarinas, contribuir al estudio quimiotaxonómico del genero Pentacalia. Materiales y métodos. El material vegetal (hojas) se colecto en el páramo de Cruz Verde-Cundinamarca (Colombia). Se prepararon dos extractos uno en éter de petróleo y el otro en etanol (EtOH), al extracto etanólico se le realizaron dos fraccionamiento liquido-liquido (FL/L) uno con éter de petróleo y el otro con diclorometano (CH2Cl2), extractos y fracciones fueron trabajados con diferentes técnicas cromatograficas, los metabolitos aislados fueron identificados con base en sus propiedades físicas (punto de fusión y valor de Rf) reacciones químicas cualitativas y técnicas como Cromatografía de Gases acoplada a Masas (CG-MS), y Resonancia Magnética Nuclear de 1H y 13C en una dimensión, dependiendo de la complejidad de cada una. Resultados. Del extracto éter de petróleo se aislaron dos cumarinas y dos mezclas de esteroles, las cumarinas 2-H-1-Benzopiren-2-ona (Cumarina) y 7-Hidroxi-6-metoxi-2-H-1-benzopiren-2-ona (Escopoletina) y las mezclas de esteroles Estigmasterol-7,16-dien-3-ol-Estigmasterol-Gamma sitosterol y Estigmasterol-Gamma sitosterol, de la fracción CH2Cl2 del extracto EtOH se aisló la Cumarina 6,7-dimetoxi-2-H-1-benzopiren-2-ona (Escoporona). Conclusiones. Se identificaron dos sustancias la Cumarina y el 7,16-dien-3-ol-Estigmasterol de las cuales no existen reportes de su presencia en la especie Pentacalia. De acuerdo con los resultados obtenidos se puede catalogar a la especie Pentacalia vaccinioides como una nueva fuente natural de cumarinas y sustancias esteroidales. Estos resultados aportan información que enriquecen los criterios quimiotaxonómicos del género Pentacalia
Descritores: Asteraceae
Cumarínicos
Plantas Medicinais
-Cromatografia
Colômbia
Compostos Fitoquímicos
Responsável: BR1.1 - BIREME


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Id: biblio-889247
Autor: Guerra, Felipe QS; Araújo, Rodrigo SA; Sousa, Janiere P; Silva, Viviane A; Pereira, Fillipe O; Mendonça-Junior, Francisco JB; Barbosa-Filho, José M; Pereira, Julio Abrantes; Lima, Edeltrudes O.
Título: A new coumarin derivative, 4-acetatecoumarin, with antifungal activity and association study against Aspergillus spp
Fonte: Braz. j. microbiol;49(2):407-413, Apr.-June 2018. tab, graf.
Idioma: en.
Resumo: Abstract Fungal infections have become a concern for health professionals, and the emergence of resistant strains has been reported for all known classes of antifungal drugs. Among the fungi causing disease, we highlight those that belong to the genus Aspergillus. For these reasons, the search for new antifungals is important. This study examines the effects of a coumarin derivative, 4-acetatecoumarin (Cou-UMB16) both alone and together with antifungal drugs, and its mode of action against Aspergillus spp. Cou-UMB16 was tested to evaluate its effects on mycelia growth, and germination of Aspergillus spp. fungal conidia. We investigated its possible action on cell walls, on the cell membrane, and also the capacity of this coumarin derivative to enhance the activity of antifungal drugs. Our results suggest that Cou-UMB16 inhibits Aspergillus spp. virulence factors (mycelia growth and germination of conidia) and affects the structure of the fungal cell wall. When applying Cou-UMB16 in combination with azoles, both synergistic and additive effects were observed. This study concludes that Cou-UMB16 inhibits mycelial growth and spore germination, and that the activity is due to its action on the fungal cell wall, and that Cou-UMB16 could act as an antifungal modifier.
Descritores: Antifúngicos/isolamento & purificação
Antifúngicos/farmacologia
Aspergillus/efeitos dos fármacos
Cumarínicos/isolamento & purificação
Cumarínicos/farmacologia
Sinergismo Farmacológico
-Aspergillus/crescimento & desenvolvimento
Azóis/farmacologia
Membrana Celular/efeitos dos fármacos
Parede Celular/efeitos dos fármacos
Hifas/efeitos dos fármacos
Hifas/crescimento & desenvolvimento
Esporos Fúngicos/efeitos dos fármacos
Esporos Fúngicos/crescimento & desenvolvimento
Responsável: BR1.1 - BIREME


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Id: biblio-888957
Autor: Weng, KG; Yuan, YL.
Título: Synthesis and evaluation of coumarin derivatives against human lung cancer cell lines
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;50(11):e6455, 2017. tab, graf.
Idioma: en.
Resumo: Series of novel coumarin derivatives [I (a-d) and II (a-d)] were successfully synthesized and their structures were determined based on infrared 1H-nuclear magnetic resonance (NMR), HRMS, and single crystal X-ray crystallography. Additionally, the new synthesized compounds were evaluated to identify the molecular characteristics that contribute to their cytotoxicity, which was tested against SK-LU-1, SPC-A-1 and 95D human lung cancer cell lines, using the MTT assay. The results of this study showed that compounds Ic, Id, IIc, and IId exhibited an efficient percentage of inhibition of cell proliferation.
Descritores: Antineoplásicos/farmacologia
Cumarínicos/farmacologia
Neoplasias Pulmonares/tratamento farmacológico
-Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Corantes
Cumarínicos/síntese química
Cumarínicos/química
Cristalografia por Raios X/métodos
Ensaios de Seleção de Medicamentos Antitumorais
Neoplasias Pulmonares/patologia
Espectroscopia de Ressonância Magnética/métodos
Valores de Referência
Reprodutibilidade dos Testes
Sais de Tetrazólio
Tiazóis
Limites: Seres Humanos
Tipo de Publ: Estudos de Avaliação
Responsável: BR1.1 - BIREME



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