Enhancement of the antibiotic activity by quercetin against Staphylococcus aureus efflux pumps.

The objective of this work was to evaluate the inhibitory effect of quercetin on S. aureus Efflux Pumps. The MIC of Quercetin was evaluated through the broth microdilution method, as well as the Efflux Pump inhibition assay through the method of reducing the antibiotic minimum inhibitory concentration as well as that of ethidium bromide. The in silico approach through bioinformatics was performed to demonstrate the molecular mechanism of interaction of the substrate and the binding cavity. The Quercetin inhibition concentration was not clinically relevant. With respect to the reversal of bacterial resistance effect by efflux pump inhibition, this effect was observed with the strains carrying the TetK and NorA pumps. Regarding the interaction between the Quercetin complex and the NorA pump, the extra stability was provided by hydrogen bonds produced by the hydroxyl group.

Cytotoxicity of Essential Oil Cordia verbenaceae against Leishmania brasiliensis and Trypanosoma cruzi.

The species Cordia verbenacea DC (Boraginaceae), known as the whaling herb and camaradinha, is a perennial shrub species native to the Atlantic Forest. Its leaves are used in folk medicine as an anti-inflammatory, analgesic, antiulcerogenic and curative agent, in the form of teas or infusions for internal or topical use. The present study aimed to verify the cytotoxicity of the essential oil and the leishmanicidal and trypanocidal potential of C. verbenacea. The essential oil was characterized by GC-MS. The in vitro biological activity was determined by anti-Leishmania and anti-Trypanosoma assays. The cytotoxixity was determined using mammalian fibroblasts. The C. verbenacea species presented α-pinene (45.71%), ß-caryophyllene (18.77%), tricyclo[2,2,1-(2.6)]heptane (12.56%) as their main compounds. The essential oil exhibited strong cytotoxicity at concentrations below 250 µg/mL (LC50 138.1 µg/mL) in mammalian fibroblasts. The potent anti-trypanosome and anti-promastigote activities occurred from the concentration of 62.5 µg/mL and was considered clinically relevant. The results also demonstrate that at low concentrations (<62.5 µg/mL), the essential oil of C. verbenacea managed to be lethal for these activities. This can be considered an indication of the power used in daily human consumption. Therefore, it can be concluded that the essential oil of C. verbenacea contains a compound with remarkable antiparasitic activities and requires further research.

Cytotoxic and anti-kinetoplastid potential of the essential oil of Alpinia speciosa K. Schum.

Alpinia speciosa K. Schum, known as colônia (colony), is native to tropical Asia and found in parts of tropical America. Its leaves are used to wrap food, rhizomes for food preparation and seeds for health maintenance, and have been widely used by the population as a diuretic, antihypertensive, antiulcerogenic and sedative. The present study aimed to verify the leishmanicidal and trypanocidal potential, as well as the cytotoxicity, of the A. speciosa essential oil, in vitro. A. speciosa presented 1,8-cineole (28.46%), camphor (17.10%) and sabinene (9.95%) as major constituents. The cytotoxic activity of the essential oil presented a low value, while the antipromastigote and antiepimastigote activity presented values considered clinically relevant, since it had an action below 500 µg/mL. In relation to this study, it can be concluded that this is a pioneer in the potential of the A. speciosa essential oil and in the use against the parasites Trypanosoma cruzi Chagas and Leishmania brasiliensis Vianna, having its importance also rooted in this fact. Still in accordance with the results, A. speciosa was effective because it presented values of clinical relevance and low toxicity. It was also observed that the chemical constitution of the above identified compounds with remarkable antiparasitic activities.

Comparative research performance of top universities from the northeastern Brazil on three pharmacological disciplines as seen in scopus database.

OBJECTIVES: Postgraduate programmes around the world are periodically subjected to research performance evaluation through bibliometric indicators. In this research, we characterized and compared the research performance of 15 universities from Northeastern Brazil, in which 13 were among the top Universities of the Latin America. METHODS: Specifically, total documents, citations and the h-index of each university were retrieved from the Elsevier Scopus database and were analysed not only for historical scientific achievement but also across the period of the past 6 years (2010-2015). Using these bibliometric indicators, we also investigated the performance of programmes at these Universities that have their papers indexed in the Scopus database under the category of "Pharmacology, Toxicology and Pharmaceuticals" for the same period. RESULTS: We found that the Federal University of Pernambuco (UFPE) and the Federal University of Ceará (UFC) were the most productive institutions, producing 17847 and 15048 documents, respectively. The number of papers published by each of these universities in the past six years represented more than 50% of their entire productivity. With regards to their scientific output in "Pharmacology, Toxicology and Pharmaceutics", UFC showed the highest number of published documents followed by UFPE and the Federal University of Paraíba (UFPB). UFC received the highest h-index (with and without self-citations) and number of citations and shared their most cited papers with foreign institutions from the USA and Germany. However, papers from UFC were published in journals with lower impact factors (2.322). CONCLUSIONS: The present study shows where each of these universities stands and can be helpful in identifying potential collaborators in these areas of knowledge.

Estudo químico-biológico do óleo essencial de Lantana montevidensis (chumbinho) (Spreng.) Briq. (Verbenaceae) contra Drosophila melanogaster / Estudio químico-biológico del aceite esencial de Lantana montevidensis (Chumbinho) (Spreng.) Briq. (Verbenaceae) contra Drosophila melanogaster / Chemical-biological study of the essential oil of Lantana montevidensis (chumbinho) (Spreng.) Briq. (Verbenaceae) against Drosophila melanogaster

Introdução: O uso de plantas como inseticidas podem substituir muitos produtos sintéticos por apresentarem baixa toxicidade para os animais e biodegradação no ambiente. A espécie Lantana montevidensis (Spreng.) Briq. (Verbenaceae), chumbinho, é um vegetal subarbustivo rico de compostos secundários para a sua defesa. O modelo experimental com Drosophila melanogaster tem sido usada para estudos, por apresentar vantagens, pois tem fácil manuseio e rápida taxa de reprodução. Objetivo: Avaliar a composição química e efeito inseticida do óleo essencial (OE) de L. montevidensis contra D. melanogaster. Metodos: O OE das folhas secas provenientes do Crato-CE, Brasil, foi extraído por hidrodestilação e foi analisado por CG/EMS para identificação dos constituintes. No ensaio foi avaliada a mortalidade e geotaxia negativa das moscas, em que elas foram expostas a diferentes concentrações do OE (3-30,5 µg/mL do óleo essencial/ar). Um total de vinte moscas adultas foram submetidas à diapausa por meio de resfriamento e em seguidas foram colocadas em frascos de 300 mL, cuja parte inferior havia papel filtro impregnado com 1 mL de sacarose a 20 por cento em água destilada. Na parte superior (tampa) foi afixado um papel filtro para a aplicação do produto a ser testado, nesse caso o OELM. As leituras foram realizadas a cada 3, 6, 12 e 24 h. Resultados: Os resultados mostraram que o OE apresentou o ß-Cariofileno (34,96 por cento), o Germacreno D (25,49 por cento) e o Biciclogermacreno (9, 78 por cento) como componentes majoritários, no ensaio inseticida houve uma CL50 na concentração de 15,14 µg/mL em 3 h de exposição, e houve um efeito significativo nos danos do aparelho locomotor das moscas.mConclusão: Este estudo fornece evidências que esse OE apresenta-se como um potencial bioinseticida(AU)

Introducción: el uso de plantas como insecticidas puede sustituir muchos productos sintéticos porque tienen baja toxicidad para los animales y son fácilmente biodegradables en el medio ambiente. La especie Lantana montevidensis (Spreng.) Briq. (Verbenaceae), Chumbinho, es una planta sub-arbustiva rica en metabolitos secundarios para su defensa. El modelo experimental en Drosophila melanogaster se ha utilizado para varios tipos de estudios, presenta algunas ventajas como: fácil manejo y tasa de reproducción rápida. Objetivo: evaluar la composición química y el efecto insecticida de aceite esencial (OE) de L. montevidensis contra las D. melanogaster. Métodos: el OE de hojas secas del Crato-CE, Brasil, se extrajo por hidrodestilación y se analizó por GC/EMS para identificar los constituyentes. En el test se evaluó la mortalidad y geotaxia negativas de las moscas, donde fueron expuestos a diferentes concentraciones de OE (3-30,5 µg/mL de aceite esencial/aire). Un total de veinte moscas adultas se sometieron a diapausa por enfriamiento y seguido se colocaron en botellas de 300 mL, la parte inferior contenido papel de filtro impregnado con 1 mL de 20 por ciento de sacarosa en agua destilada. En la parte superior (tapa) se haya colocado un papel de filtro para la aplicación del producto a ensayar, la OELM. Las lecturas se realizaron cada 3, 6, 12 y 24 h. Resultados: Los resultados mostraron que el OE presenta la ß-cariofileno (34,96 por ciento), el germacreno D (25,49 por ciento) y bicyclogermacrene (9,78 por ciento) como componentes principales en el ensayo insecticida había una CL50 de la concentración de 15,14 µg/mL en 3 h de exposición, y había un un efecto significativo en el daño del aparato locomotor de las moscas. Conclusión: este estudio proporciona evidencia de que este OE o se presenta como un biopesticida potencial(AU

Introduction: The use of plants as insecticides may be an alternative to many synthetic products because their toxicity to animals is low and they are easily biodegradable in the environment. The species Lantana montevidensis (Spreng.) Briq. (Verbenaceae), chumbinho, is a subshrub rich in secondary metabolites it uses for its own defence. The experimental model for Drosophila melanogaster has been used in several types of studies. Some of its advantages are its easy management and its fast rate of reproduction. Objective: Evaluate the chemical composition and insecticidal effect of the essential oil (EO) of L. montevidensis against D. melanogaster. Method: EO of dry leaves from Crato-CE, Brazil, was extracted by hydrodistillation and analyzed by GC/EMS to identify its constituents. As part of the test, evaluation was conducted or the mortality and negative geotaxis of the flies, to attain which they were exposed to different concentrations of the EO (3-30.5 µg/mL essential oil/air). A total 20 adult flies were subjected to cold diapause and placed in 300 mL bottles with filter paper in their lower section impregnated with 1 mL of 20 percent saccharose in distilled water. Filter paper was also attached to the upper section (lid) to apply the test product OELM. Readings were taken every 3, 6, 12 and 24 h. Results: Results showed that the principal components of the EO are ?-caryophyllene (34.96 percent), germacrene D (25.49 percent) and bicyclogermacrene (9.78 percent). In the insecticide test there was a CL50 for the concentration of 15.14 µg/ml in 3 h exposure, and significant damage to the locomotor system of the flies. Conclusion: The study provides evidence that the EO analyzed is a potential biopesticide(AU)