Evaluation of antifungal activity, mechanisms of action and toxicological profile of the synthetic amide 2-chloro-N-phenylacetamide.

Aspergillus niger causes infections such as otitis and pulmonary aspergillosis in immunocompromised individuals. Treatment involves voriconazole or amphotericin B, and due to the increase in fungal resistance, the search for new compounds with antifungal activity has intensified. In the development of new drugs, cytotoxicity and genotoxicity assays are important, as they allow predicting possible damage that a molecule can cause, and in silico studies predict the pharmacokinetic properties. The aim of this study was to verify the antifungal activity and the mechanism of action of the synthetic amide 2-chloro-N-phenylacetamide against Aspergillus niger strains and toxicity. 2-Chloro-N-phenylacetamide showed antifungal activity against different strains of Aspergillus niger with minimum inhibitory concentrations between 32 and 256 µg/mL and minimum fungicides between 64 and 1024 µg/mL. The minimum inhibitory concentration of 2-chloro-N-phenylacetamide also inhibited conidia germination. When associated with amphotericin B or voriconazole, 2-chloro-N-phenylacetamide had antagonistic effects. Interaction with ergosterol in the plasma membrane is the probable mechanism of action.2-Chloro-N-phenylacetamide has favorable physicochemical parameters, good oral bioavailability and absorption in the gastrointestinal tract, crosses the blood-brain barrier and inhibits CYP1A2. At concentrations of 50 to 500 µg/mL, it has little hemolytic effect and a protective effect for type A and O red blood cells, and in the cells of the oral mucosa it promotes little genotoxic change. It is concluded that 2-chloro-N-phenylacetamide has promising antifungal potential, favorable pharmacokinetic profile for oral administration and low cytotoxic and genotoxic potential, being a promising candidate for in vivo toxicity studies.

Avaliação da citotoxicidade in vitro e genotoxicidade ex-vivo em compostos da Pavonia glazioviana Gürke (Malvaceae / Evaluation of in vitro cytotoxicity and ex-vivo genotoxicity in compounds from Pavonia glazioviana Gürke(Malvaceae)

Introdução: as terapias alternativas que utilizam plantas medicinais e fitoterápicos são bastante comuns no Brasil. Dentre várias espécies vegetais brasileiras utilizadas em terapias destacam-se as espécies da família Malvaceae. Objetivos: o presente estudo teve como objetivo avaliar a citotoxicidade in vitro e a genotoxicidade ex-vivo em compostos da Pavonia glazioviana Gürke espécie brasileira pertencente à família Malvaceae. Metodologia: métodos in vitro foram utilizados para verificar o potencial citotóxico por meio de ensaios hemolíticos e anti-hemolíticos e da análise genotóxica ex-vivo. O Extrato Etanólico Bruto (EEB) e Fração Clorofórmico (FC) foram obtidos na amostra vegetal utilizada neste estudo. Resultados: os produtos EEB-Pg e FC-Pg apresentaram baixo efeito citotóxico apenas nas concentrações de 50 e 100 µg / mL. As amostras expostas às concentrações de 500 e 1000 µg / mL apresentaram índice hemolítico alto a moderado com lise superior a 60%. Foi descrito efeito anti-hemolítico moderado em todas as amostras tratadas com 500 e 1000 µg / mL, com hemólise < 60%. Além disso, os compostos mostraram baixo efeito genotóxico ex-vivo, com um índice geral de células normais superior a 84% em todas as concentrações. Conclusões: os resultados sugerem um baixo perfil tóxico dos compostos obtidos da espécie Pavonia glazioviana, indicando limites seguros para o uso desses produtos naturais.

Introduction: alternative therapies using medicinal plants and herbal medicines are quite common in Brazil. Among several Brazilian plant species used in therapies, the species of the Malvaceae family stand out. Objetctives: the present study aimed to evaluate the in vitro cytotoxicity and ex-vivo genotoxicity in compounds of the Brazilian Pavonia glazioviana Gürke belonging to the Malvaceae family. Methodology: in vitro methods were used to verify the cytotoxic potential through hemolytic and antihemolytic assays and the ex-vivo genotoxic analysis. The Crude Etanolic Extract (CEE) and Cloroformic Fraction (CF) was obtained in vegetal sample used on this study. Results: the CEE-Pg and CF-Pg products only showed a low cytotoxic effect at the concentrations of 50 and 100 µg/mL. The exposure to the concentrations of 500 and 1000 µg/mL showed a high to moderate hemolytic index with lysis higher than 60%. A moderate anti-hemolytic effect was described in all samples treated with 500 and 1000 µg/mL, with hemolysis <60%. In addition, the compounds showed low ex-vivo genotoxic effect with a general index of normal cells greater than 84% at all concentrations. Conclusion: the results suggest a low toxic profile of the compounds obtained from the Pavonia glazioviana Gürke species belonging to the Malvaceae family, indicating safe limits for the use of these natural products.

Evaluation of Toxicity and Oxidative Stress of 2-Acetylpyridine-N(4)-orthochlorophenyl Thiosemicarbazone.

Thiosemicarbazones are well known for their broad spectrum of action, including antitumoral and antiparasitic activities. Thiosemicarbazones work as chelating binders, reacting with metal ions. The objective of this work was to investigate the in silico, in vitro, and in vivo toxicity and oxidative stress of 2-acetylpyridine-N(4)-orthochlorophenyl thiosemicarbazone (TSC01). The in silico prediction showed good absorption by biological membranes and no theoretical toxicity. Also, the compound did not show cytotoxicity against Hep-G2 and HT-29 cells. In the acute nonclinical toxicological test, the animals treated with TSC01 showed behavioral changes of stimulus of the central nervous system (CNS) at 300 mg/kg. One hour after administration, a dose of 2000 mg/kg caused depressive signs. All changes disappeared after 24 h, with no deaths, which suggest an estimated LD50 of 5000 mg/kg and GSH 5. The group treated with 2000 mg/kg had an increase of water consumption and weight gain in the second week. The biochemical parameters presented no toxicity relevance, and the analysis of oxidative stress in the liver found an increase of lipid peroxidation and nitric oxide. However, histopathological analysis showed organ integrity was maintained without any changes. In conclusion, the results show the low toxicological potential of thiosemicarbazone derivative, indicating future safe use.

The prevalence of Listeria monocytogenes in meat products in Brazil: A systematic literature review and meta-analysis.

Listeria monocytogenes, a foodborne pathogen that causes human listeriosis, is commonly found in meat products. This study aimed to estimate the prevalence of L. monocytogenes in a variety of Brazilian meat products, using a meta-analysis of data from the literature. A total of 29 publications from five databases, published between January 1, 2009, and December 31, 2019, were included in the study. Estimated by the random-effects model, the combined prevalence of L. monocytogenes was 13%, ranging from 0 to 59%. The combined prevalence of L. monocytogenes was 14% and 11% for raw meat and ready-to-eat (RTE) meat, respectively. The prevalence of L. monocytogenes was higher in the swine species' meat products and the Southeast region of Brazil. Regarding the type of establishment, it was the retail market that presented the highest combined prevalence rate (19%). The most prevalent serotypes of L. monocytogenes were 4b, 1/2a, 1/2b, and 1/2c. The knowledge of differences in the prevalence levels of L. monocytogenes in different meat products can guide in its efficient control by the competent authorities and by industry.

Antibacterial effect of isoeugenol against Pseudomonas aeruginosa

Abatsract Pseudomonas aeruginosa is an important nosocomial pathogen and its clinical importance is mainly related to nosocomial infections. Increased rates of bacterial resistance in recent years has led WHO to publish a global priority list to guide research and discovery of new antibiotics, where P. aeruginosa is among the group of bacteria for which there is a critical level of priority for new drugs to be discovered. In this context, isoeugenol appears as an interesting alternative and the objective of this study was to investigate its action against P. aeruginosa. Isoeugenol presented significant antibacterial activity, with minimum inhibitory concentration (MIC) of 64µg/mL and minimum bactericidal concentration (MBC) of 128µg/mL, and was considered bactericidal against this species. Molecular docking revealed interactions that suggest that isoeugenol may bind to the enzyme Penicillin-Binding Protein 3 and interfere with the bacterial cell wall synthesis process. This study reinforces the antibacterial potential of this compound and emphasizes that more studies are needed in order to better investigate its mechanism of antibacterial action.

Avaliação in vitro da atividade fotoprotetora do extrato hexânicode Psidium araçá (Psidium guineense sw) / In vitro evaluation of photoprotective activity of hexanic extract of Psidium araçá (Psidium guineense sw) / Evaluación in vitro de la actividad fotoprotectiva del extracto hexanico de Psidium araçá (Psidium guineense sw)

A radiação ultravioleta (UV) é um potente carcinógeno, principalmente a UV-B, capaz de provocar danos ao DNA, relacionado a formação de radiação livres. A excessiva exposição solar e sem prevenção contra os raios UV representa um grande risco para o desenvolvimento de patologias com malignidade, dentre elas o câncer de pele. O emprego de extratos vegetais brasileiros com potencial fotoprotetor é sem dúvida um caminho inovador. O araçá ou araçá-do-campo por exemplo, da família Myrtaceae, espécie Psidium guineense Sw., possui grande potencial para exploração econômica e tem boa aceitação in natura, Dessa forma, o presente estudo tem por objetivo avaliar a atividade fotoprotetora do extrato hexânico do Psidium guineense Sw. Foram realizadas varreduras de 290 a 320nm (com intervalos de 5nm) em concentrações de 50, 100, 500 e 1000µg/mL em amostras de 2,0 mL. Os dados foram aplicados à equação de Mansur para aferir o FPS in vitro. Os resultados dessa pesquisa demonstraram que o extrato hexânico de Psidium guineense Sw. apresenta significativa atividade fotoprotetora nas concentrações de 500 e 1000 µg/mL mostrando-se superior ao FPS necessário. Assim, os resultados sugerem que possa ser utilizado como alternativa fitocosmética, tornando-se uma opção mais acessível(AU)

Ultraviolet radiation (UV) is a potent carcinogen, mainly UV-B, capable of causing damage to DNA, related to the formation of free radiation. Excessive sun exposure and without prevention against UV rays represents a great risk for the development of pathologies with malignancy, including skin cancer. The use of Brazilian plant extracts with photoprotective potential is undoubtedly an innovative path. The araçá or araçá-do-campo, for example, of the Myrtaceae family, Psidium guineense Sw., Has great potential for economic exploitation and has good acceptance in natura. Thus, the present study aims to evaluate the photoprotective activity of the hexane extract of Psidium guineense Sw. Scans of 290 to 320nm (with 5nm intervals) were performed in concentrationsof 50, 100, 500 and 1000µg / mL in samples of 2.0 mL. The data were applied to Mansur equation to measure SPF in vitro. The results of this research demonstrated that the hexanic extract of Psidium guineense Sw. Has significant photoprotective activity at concentrations of 500 and 1000 µg / mL, showing itself to be superior to the necessary SPF. Thus, the results suggest that it can be used as a phytocosmetic alternative, making it a more accessible option(AU)

La radiación ultravioleta (UV) es un potente carcinógeno, principalmente UV-B, capaz de causar daño al ADN, relacionado con la formación de radiación libre. La exposición excesiva al sol y sin prevención contra los rayos UV representa un gran riesgo para el desarrollo de patologías con malignidad, incluido el cáncer de piel. El uso de extractos de plantas brasileñas con potencial fotoprotector es, sin duda, un camino innovador. El araçá o araçá-do-campo, por ejemplo, de la familia Myrtaceae, Psidiumguineense Sw., Tiene un gran potencial para la explotación económica y tiene una buena aceptación en la naturaleza. Por lo tanto, el presente estudio tiene como objetivo evaluar la actividad fotoprotectora del hexano de Psidium guineense Sw. Se realizaron exploraciones de 290 a 320 nm (con intervalos de 5 nm) en concentraciones de 50, 100, 500 y 1000 µg / ml en muestras de 2,0 ml. Los datos se aplicaron a la ecuación de Mansurpara medir SPF in vitro. Los resultados de esta investigación demostraron que el extracto hexánico de Psidium guineense Sw. Tiene una actividad fotoprotectora significativa a concentraciones de 500 y 1000 µg / ml, demostrando ser superior al SPF necesario. Por lo tanto, los resultados sugieren que puede usarse como una alternativa fitocosmética, por lo que es una opción más accesible(AU)

In silico, in vitro and ex-vivo Toxicological Profiling of 5,7,4'-Trihydroxyflavone-8-C-ß-Glucopyranoside - Vitexin

This study aimed to evaluate the in silico, in vitro, and ex-vivo toxicity of vitexin, the flavonoid 5,7,4'- trihydroxyflavone-8-C-ß-glucopyranoside from Waltheria viscosissima. The chemical structure and predicted bioactive properties were also in silico analyzed. The in vitro and ex-vivo assays were performed according to the Ethics Code of the World Medical Association and were approved by the Ethics Committee of University Center of Patos (protocol number: 3.621.284). In silico analysis suggested that the molecule presents good oral bioavailability and good absorption; penetrating biological membranes. The toxicity tests revealed the potential effectiveness of the molecule in cellular protection against free radicals, in addition to possible antimutagenic, anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic and apoptosis agonist activity. Hemolytic and genotoxic assessment detected low hemolysis rates in human red blood cells and no cellular toxicity against oral mucosa cells. The data suggest that vitexin is a safe molecule for possible therapeutic application and its toxicity profile indicates viability for future studies.

Estudo do potencial antifúngico e do mecanismo de ação do timol contra cepas de Candida parapsilosis resistentes ao fluconazol e a anfotericina B / Study of the antifungal potential and mechanism of action of thymol against strains of Candida parapsilosis resistant to fluconazole and amphotericin B

Objetivo: investigar a suscetibilidade de cepas fúngicas de Candida parapsilosis isoladas de sangue humano frente ao timol, bem como seu mecanismo de ação. Metodologia: foram utilizadas técnicas de microdiluição em placas de 96 poços para determinar a concentração inibitória mínima (CIM) e concentração fungicida mínima (CFM). Além disso, foram realizados testes com o sorbitol e o ergosterol para investigar a ação do timol na parede e na membrana celular fúngica respectivamente. Resultados: nos testes de CIM e CFM, foi observado que as cepas de C. parapsilosis são resistentes ao fluconazol e a anfotericina B, no entanto, o timol desempenhou efeito fungicida com razão CFM/CIM entre 1 e 2. Além disso, a CIM do timol não aumentou quando o sorbitol ou o ergosterol foi adicionado no meio, sugerindo fortemente que este monoterpeno não age na parede celular fúngica ou por ligação ao ergosterol na membrana plasmática. Conclusão: portanto, esses resultados contribuem para a elucidação do mecanismo de ação do timol, sugerindo outros possíveis alvos de interação fármaco-receptor. No entanto, mais investigações de caráter enzimático e molecular em modelos in vitro são necessários para que se possa elucidar completamente o modo de ação desse promissor monoterpeno.

Objective: to investigate the susceptibility of fungal strains of Candida parapsilosis isolated from human blood against thymol, as well as its mechanism of action. Methodology: microdilution techniques were used in 96-well plates to determine minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC). In addition, tests were performed with sorbitol and ergosterol to investigate the action of thymol on the wall and on the fungal cell membrane respectively. Results: in the CIM and CFM tests, it was observed that C. parapsilosis strains are resistant to fluconazole and amphotericin B, however, thymol had a fungicidal effect with MFC/MIC ratio between 1 and 2. In addition, thymol MIC did not increase when sorbitol or ergosterol was added in the medium, strongly suggesting that this monoterpene does not act on the fungal cell wall or by binding to ergosterol on the plasma membrane. Conclusion: therefore, these results contribute to the elucidation of the mechanism of action of thymol, suggesting other possible targets of drug-receptor interaction. However, further investigations of enzymatic and molecular character in in vitro models are necessary to fully elucidate the mode of action of this promising monoterpene.

Lavandula angustifolia Miller e sua utilização na Odontologia: uma breve revisão / Lavandula angustifolia Miller and its use in Dentistry: a brief review / Lavandula angustifolia Miller y su uso en la Odontología: una breve revisión

O uso de medicamentos fitoterápicos vem crescendo mundialmente entre os programas preventivos e curativos, e tem estimulado a avaliação dos extratos de plantas para o uso na odontologia como controle do biofilme dental e outras desordens bucais. As plantas do gênero Lavandula, pertencem à família Lamiaceae, e têm sido utilizadas através dos anos para uma variedade de propósitos cosméticos e terapêuticos. Sua utilização na odontologia é, na grande maioria dos estudos, devido ao seu potencial ansiolítico. Entretanto, a Lavandula angustifólia demonstra outros potencias farmacológicos, como sua atividade antimicrobiana, antifúngica, anti-inflamatória e antinociceptiva. O presente estudo teve como objetivo integrar os conhecimentos já existentes sobre os aspectos das propriedades farmacológicas da Lavandula angustifolia Miller e sua aplicação na Odontologia. Trata-se de uma revisão bibliográfica no qual foi realizada uma seleção de artigos científicos a partir das bases de dados: Lilacs, MEDLINE, BVS e Scielo, além de monografias que atenderam aos requisitos do tema abordado, no período 2008 a 2018 com exceção de artigos clássicos que se apresentaram imprescindíveis ao presente estudo. Obteve-se um total de 1.532 artigos. Foram selecionados 38 artigos como amostra, que apresentaram a temática elencada para a pesquisa e que foram divididos por sessões: aspectos botânicos da planta; aspectos bioquímicos da planta; potencial antimicrobano; potencial anti-inflamatório; potencial ansiolítico e; potencial antinociceptivo. Pode-se concluir que a Lavandula angustifólia Miller apresenta-se como uma boa alternativa para utilização na odontologia. Entretanto, a falta de trabalhos que abordem sua utilidade na odontologia revela a necessidade de se intensificar as pesquisas sobre o assunto(AU)

The use of herbal medicines has been growing worldwide among preventive and curative programs and has stimulated the evaluation of plant extracts for use in dentistry as a control of dental biofilm and other oral disorders. Lavandula plants belong to the Lamiaceae family, and have been used over the years for a variety of cosmetic and therapeutic purposes. Its use in dentistry is, in the great majority of studies, due to its anxiolytic potential. However, Lavandula angustifolia shows other pharmacological potencies, such as its antimicrobial, antifungal, anti-inflammatory and antinociceptive activity. The aim of the present study was to integrate existing knowledge on aspects of the pharmacological properties of Lavandula angustifolia Miller and its application in dentistry. It is a bibliographic review in which a selection of scientific articles was carried out from the databases Lilacs, MEDLINE, BVS and Scielo, as well as monographs that met the requirements of the topic addressed, from 2008 to 2018, with the exception of classical articles that were essential to the present study. A total of 1,532 articles were obtained. A total of 38 articles were selected as the sample, which presented the theme for the research and were divided by sessions: botanical aspects of the plant; biochemical aspects of the plant; antimicrobial potential; anti-inflammatory potential; anxiolytic potential and; antinociceptive potential. It can be concluded that Lavandula angustifolia Miller presents itself as a good alternative for use in dentistry. However, the lack of studies that address its usefulness in dentistry reveals the need to intensify research on the subject(AU)

El uso de medicamentos fitoterápicos viene creciendo mundialmente entre los programas preventivos y curativos, y ha estimulado la evaluación de los extractos de plantas para el uso en la odontología como control del biopelículas dental y otros desórdenes bucales. Las plantas del género Lavandula, pertenecen a la familia Lamiaceae, y han sido utilizadas a través de los años para una variedad de propósitos cosméticos y terapéuticos. Su uso en la odontología es, en la gran mayoría de los estudios, debido a su potencial ansiolítico. Sin embargo, la Lavandula angustifolia demuestra otras potencias farmacológicas, como su actividad antimicrobiana, antifúngica, anti-inflamatoria y antinociceptiva. El presente estudio tuvo como objetivo integrar los conocimientos ya existentes sobre los aspectos de las propiedades farmacológicas de la Lavandula angustifolia Miller y su aplicación en la Odontología. Se trata de una revisión bibliográfica en la que se realizó una selección de artículos científicos a partir de las bases de datos: Lilacs, MEDLINE, BVS y Scielo, además de monografías que atendieron a los requisitos del tema abordado, en el período 2008 a 2018 con excepción de artículos clásicos que se presentaron imprescindibles para el presente estudio. Se obtuvo un total de 1.532 artículos. Se seleccionaron 38 artículos como muestra, que presentaron la temática elaborada para la investigación y que fueron divididos por sesiones: aspectos botánicos de la planta; aspectos bioquímicos de la planta; potencial antimicrobiano; potencial anti-inflamatorio; potencial ansiolítico y; potencial antinociceptivo. Se puede concluir que la Lavandula angustifolia Miller se presenta como una buena alternativa para su uso en la odontología. Sin embargo, la falta de trabajos que abordan su utilidad en la odontología revela la necesidad de intensificar las investigaciones sobre el tema(AU)

Malva Sylvestris, Vitis Vinífera e Punica Granatum: uma revisão sobre a contribuição para o tratamento de periodontite / Malva Sylvestris, Vitis Vinífera e Punica Granatum: a review of the contribution to the treatment periodontitis / Malva Sylvestris, Vitis Vinífera y Punica Granatum: una revisión sobre la contribución para el tratamiento de la periodontitis

As plantas medicinais têm demonstrado elevado poder de cura em estado natural, além disso, esse conhecimento tradicional sobre o uso das plantas e de suas propriedades terapêuticas no combate a doenças vêm sendo transmitida entre as gerações. A busca por novos produtos com maior atividade terapêutica, tem estimulado a realização de pesquisas com produtos naturais no meio odontológico para o tratamento de doença periodontal. Logo, objetivou-se apresentar uma revisão da literatura de espécies vegetais como Malva Sylvestris, Vitis Vinífera e Punica Granatum, comuns do cotidiano no tratamento da periodontite. A periodontite é uma doença inflamatória crônica decorrente da resposta imunológica do hospedeiro à presença de fatores microbianos, causando dano tecidual, resultando em formação de bolsas periodontais, reabsorção do osso alveolar, e perda de tecidos de sustentação. O estudo trata-se de uma revisão bibliográfica do tipo narrativa e foi realizada uma seleção de artigos científicos recuperados a partir das bases de dados: BVS Brasil (Biblioteca Virtual em Saúde), Scielo (Scientific Eletronic Library Online), Pubmed (National Center for Biotechnology Information) e Portal Periódico Capes no período de 05 a 28 de Fevereiro de 2018. Conclui-se que a Malva, Uva e Romã possuem ação terapêutica e estão entre os fitoterápicos com grande influência na cavidade bucal, que funcionam como auxiliares no tratamento de afecções orais sendo alternativas de fácil acesso, já que a atuação profissional frente à ação farmacológica dos vários medicamentos fitoterápicos e contraindicações tem sido importante nos últimos anos(AU)

Medicinal plants have shown high healing power in the natural state, and this traditional knowledge about the use of plants and their therapeutic properties in the fight against diseases has been transmitted between the generations. The search for new products with greater therapeutic activity has stimulated research with natural products in the dental environment for the treatment of periodontal disease. Therefore, it was aimed to present a review of the literature of plant species such as Malva Sylvestris, Vitis Vinífera and Punica Granatum, common daily in the treatment of periodontitis. Periodontitis is a chronic inflammatory disease resulting from the host's immune response to the presence of microbial factors, causing tissue damage, resulting in formation of periodontal pockets, alveolar bone resorption, and loss of supporting tissues. The study is a bibliographical review of the narrative type and a selection of scientific articles retrieved from the databases: VHL Brasil (Virtual Health Library), Scielo (Scientific Electronic Library Online), Pubmed (National Center for Biotechnology Information) and Portal Periódico Capes from 05 to 28 February 2018. It is concluded that Malva, Grape and Pomegranate have therapeutic action and are among herbal medicines with great influence in the oral cavity, which function as auxiliaries in the treatment of oral diseases being alternatives of easy access, since the professional action against the pharmacological action of the various herbal medicines and contraindications has been important in recent years(AU)

Las plantas medicinales han demostrado un elevado poder de curación en estado natural, además, ese conocimiento tradicional sobre el uso de las plantas y de sus propiedades terapéuticas en el combate a enfermedades vienen siendo transmitidas entre las generaciones. La búsqueda de nuevos productos con mayor actividad terapéutica, ha estimulado la realización de investigaciones con productos naturales en el medio odontológico para el tratamiento de enfermedad periodontal. Por lo tanto, se objetivó presentar una revisión de la literatura de especies vegetales como Malva Sylvestris, Vitis Vinífera y Punica Granatum, comunes de lo cotidiano en el tratamiento de la periodontitis. La periodontitis es una enfermedad inflamatoria crónica derivada de la respuesta inmunológica del huésped a la presencia de factores microbianos, causando daño tisular, resultando en formación de bolsas periodontal, reabsorción del hueso alveolar, y pérdida de tejidos de sustentación. El estudio se trata de una revisión bibliográfica del tipo narrativa y se realizó una selección de artículos científicos recuperados a partir de las bases de datos: BVS Brasil (Biblioteca Virtual en Salud), Scielo (Scientific Eletronic Library Online), Pubmed (National Center for Y se encuentra entre los fitoterápicos con gran influencia en la cavidad bucal, que funcionan como auxiliares en el tratamiento de la enfermedad de Chagas, en el período de 5 a 28 de febrero de 2018. Se concluye que Malva, Uva y Román poseen acción terapéutica y están entre los fitoterápicos con gran influencia en la cavidad bucal, que funcionan como auxiliares en el tratamiento de afecciones orales siendo alternativas de fácil acceso, ya que la actuación profesional frente a la acción farmacológica de los diversos medicamentos fitoterápicos y contraindicaciones ha sido importante en los últimos años(AU)

Morus nigra L: revisão sistematizada das propriedades botânicas, fitoquímicas e farmacológicas / Morus nigra L: systematized review of botanical, phytochemical and pharmacological properties / Morus nigra L: revisión sistematizada de las propiedades botánicas, fitoquímicas y farmacológicas

Morus nigra é uma espécie vegetal popularmente conhecida por Amora negra. Esta espécie amplamente cultivada na Ásia e nas regiões sul e sudeste do Brasil, possui importância econômica devido a sua ampla utilização na alimentação e confeitaria, sendo também utilizada na medicina popular como anti-inflamatório, diurético, antitussígeno, anti-hemorrágico, para o tratamento do climatério e de doenças hepáticas e renais. Diversos estudos têm sido conduzidos a respeito das atividades farmacológicas da Morus nigra. Neste trabalho de revisão narrativa da literatura foram explorados estudos nas bases de dados acerca da atividade hipolipemiante e de outras atividades farmacológicas dos compostos fenólicos, estilbenos, flavonoide, isoprenilados, cumarinas, cromonas e xantonas da Morus nigra, para verificar sua capacidade de diminuição dos níveis de colesterol total, triglicerídeos, LDL e ainda, aumento dos níveis de HDL, como também outras propriedades antioxidantes, anticarcinogênica, antimutagênica. Desse modo, conclui-se a necessidade da realização de mais estudos com Morus nigra e principalmente mais ensaios clínicos que avaliem a segurança e eficácia na utilização desta planta(AU)

Morus nigra is a plant species popularly known as blackberry. This species, widely cultivated in Asia and in the south and southeast regions of Brazil, is economically important due to its wide use in food and confectionery. It is also used in folk medicine as anti-inflammatory, diuretic, antitussive, anti-hemorrhagic, for treatment climacteric and liver and kidney diseases. Several studies have been conducted regarding the pharmacological activities of Morus nigra. In this work of narrative review of the literature we explored studies in the databases on the lipid-lowering activity and other pharmacological activities of the phenolic, stilbenos, flavonoids, isoprenylates, coumarins, cromones and xanthones compounds of Morus nigra, to verify their capacity to decrease levels of total cholesterol, triglycerides, LDL and also, increased levels of HDL, as well as other antioxidant properties, anticarcinogenic, antimutagenic. Thus, it is concluded that further studies are needed with Morus nigra and, in particular, more clinical trials evaluating the safety and efficacy of this plant(AU)

Morus nigra es una especie vegetal popularmente conocida por Amora negra. Esta especie ampliamente cultivada en Asia y en las regiones sur y sudeste de Brasil, tiene una importancia económica debido a su amplia utilización en la alimentación y la confitería, siendo utilizada en la medicina popular como anti-inflamatorio, diurético, antitusígeno, anti-hemorrágico, para el tratamiento del climaterio y de las enfermedades hepáticas y renales. Se han realizado varios estudios sobre las actividades farmacológicas de Morus nigra. En este trabajo de revisión narrativa de la literatura se exploraron estudios en las bases de datos acerca de la actividad hipolipemiante y de otras actividades farmacológicas de los compuestos fenólicos, estilbenos, flavonoide, isoprenilados, cumarinas, cromonas y xantonas de Morus nigra, para verificar su capacidad de disminución de los niveles de colesterol total, triglicéridos, LDL y aún, aumento de los niveles de HDL, así como otras propiedades antioxidantes, anticarcinogénicas, antimutagénicas. De este modo, se concluye la necesidad de realizar más estudios con Morus nigra y principalmente más ensayos clínicos que evalúen la seguridad y eficacia en la utilización de esta planta(AU)

Atividade anti-Candida tropicalis dos enantiômeros (R)-(+) ­ & (S)-(-) ­ citronelal em associação com cetoconazol / Anti-Candida tropicalis activity of (R)-(+) ­ & (S)-(-) ­ citronellal enantiomers in combination with ketoconazole

Introdução: aproximadamente 75% das mulheres saudáveis experimentam pelo menos um episódio sintomático de candidíase vulvovaginal (CVV) durante sua vida. Objetivo: avaliar a atividade antifúngica contra cepas de C. tropicalis dos enantiômeros (R)-(+) ­ e (S)-(-)-citronelal [(R)-(+) ­ e (S)-(-)-CT] em associação com cetoconazol. Metodologia: o efeito antifúngico de ambos os enantiômeros foram quantificados e classificados como fungicida ou fungistático a partir dos resultados obtidos da microdiluição em meio líquido RPMI1640 para a obtenção da concentração inibitória mínima (CIM) e da concentração fungicida mínima (CFM). Foram realizados ensaios de associação do antifúngico padrão, cetoconazol com os fitoconstituintes por difusão em Agar e os resultados foram classificados como sinérgicos, antagônicos e indiferentes. Resultados: a CIM50 e a CFM50 dos compostos (R)-(+) ­ e (S)-(-)-citronelal foram respectivamente 16 e 64µg/mL e 2×CIM. Houve sinergismo para todas as cepas testadas com ambos os compostos, porém com maior efeito do enantiômero (S)-(-)-CT sobre as cepas LM 665 e LM 255 em relação ao enantiômero (R)-(+)-CT. Conclusão: os compostos naturais deste estudo mostraram efeito fungicida sobre as cepas testadas, bem como efeito sinérgico significativo quando associado ao cetoconazol

Isopropyl Caffeate: A Caffeic Acid Derivative-Antioxidant Potential and Toxicity.

Phenolic compounds, among them isopropyl caffeate, possess antioxidant potential, but not without toxicity and/or adverse effects. The present study aimed to evaluate the antioxidant activity and toxicity of isopropyl caffeate through in silico, in vitro and in vivo testing. The results showed that isopropyl caffeate presents no significant theoretical risk of toxicity, with likely moderate bioactivity: GPCR binding, ion channel modulation, nuclear receptor binding, and enzyme inhibition. Isopropyl caffeate induced hemolysis only at the concentrations of 500 and 1000 µg/ml. We observed types A and O erythrocyte protection from osmotic stress, no oxidation of erythrocytes, and even sequestrator and antioxidant behavior. However, moderate toxicity, according to the classification of GHS, was demonstrated through depressant effects on the central nervous system, though there was no influence on water and food consumption or on weight gain, and it did present possible hepatoprotection. We conclude that the effects induced by isopropyl caffeate are due to its antioxidant activity, capable of preventing production of free radicals and oxidative stress, a promising molecule with pharmacological potential.

In Silico Study and Bioprospection of the Antibacterial and Antioxidant Effects of Flavone and Its Hydroxylated Derivatives.

Flavonoid compounds are widely used as natural protective species, which can act as anti-inflammatory, antioxidant, anticoagulant, antihypertensive and antitumor agents. This study set out to investigate the probable pharmacological activities, along with the antibacterial and antioxidant effects, of flavone and its hydroxy derivatives: 3-hydroxyflavone, 5-hydroxyflavone and 6-hydroxyflavone. To do so, we investigated their pharmacological characteristics, using in silico tests that indicate likelihood of activity or inactivity, with the PASS online software, and the antimicrobial potential against Gram positive and Gram negative bacteria was also analyzed, including bacteria of clinical importance. We also tested for oxidant and antioxidant potential in these molecules in the presence of reactive oxygen species (ROS) and phenylhydrazine (Ph). The results revealed the following characteristics: pharmacological activities for the flavonoids as agonists of cell membrane integrity and as permeability inhibitors, as antagonists of anaphylatoxin receptors, as inhibitors of both kinase and peroxidase, and as having both antimutagenic capacity and vaso-protective potential. All of the flavonoids exhibited moderate antibacterial activity against Gram positive and Gram negative strains, with the flavones being bactericidal at 200 µg/mL for the strains of P. aeruginosa ATCC 8027, S. aureus ATCC 25619 and E. coli 104; the other flavonoids revealed bacteriostatic action. The substances did not promote erythrocyte oxidation and behaved as sequestrators and antioxidants of hydrogen peroxide (H2O2) and phenylhydrazine (Ph). It was concluded that the analyzed compounds have various pharmacological activities in accordance with the predictions of PASS online, as their antibacterial and antioxidant activities were confirmed. The study also helps to consolidate the use of computational chemistry in silico tools to guide new drug search and discovery protocols.

Study of the antifungal potential of (r)-(+)-citronellal and its association with therapeutic agents used in the treatment of vulvovaginal candidiasis / Estudo do potencial antifúngico do (r)-(+)-citronelal e sua associação com agentes terapêuticos utilizados no tratamento da candidíase vulvovaginal

Vulvovaginal candidiasis (VVC) is a common fungal infection that affects healthy women of all ages. At least 75% of women will develop one or more infections once during their lifetime, with 6 to 9% of those individuals developing recurrent infections. In view of this context, this study sought to evaluate the antifungal potential of the isolated (R)-(+)-citronellal [(R)-(+)-CT] and associated to therapeutic agents of clinical importance. The enantiomer was solubilized in tween 80 and dimethylsulfoxide (DMSO). Posteriorly diluted in sterile distilled water up to the concentration of 2048µg/mL. The minimum inhibitory concentration (MIC) of the product was determined by microdilution in RPMI-1640 obtaining dilutions of 1024-4µg/mL. The minimum fungicidal concentration (MFC) was determined by the Sabouraud dextrose agar (SDA) depletion technique from aliquots of 1µL of the MIC, MIC × 2 and MIC × 4. The MIC and the MFC values of (R)-(+)-CT for 90% of the C. albicans strains were 16 and 32µg/mL respectively. In the susceptibility test, C. albicans presented a high resistance to fluconazole and to itraconazole, 12 (92.30%) of the strains. However, for ketoconazole and miconazole the resistance was of 4 (30.76%) and 3 (23.07%) of the strains respectively. In the combination testing of the (R)-(+)-CT with ketoconazole and miconazole, the resistance was completely reverted. For fluconazole and itraconazole, the resistance was reverted in 9 (75%) and 7 (58.33%) of the strains respectively. The (R)-(+)-CT presented fungicide activity with MFC of MIC × 2. When in combination with ketoconazole, fluconazole, itraconazole and miconazole increased the inhibition zones of these antifungal drugs, reducing the resistance against C. albicans.

Candidíase vulvovaginal (CVV) é uma infecção fúngica comum que afeta mulheres saudáveis de todas as idades. Pelo menos 75% das mulheres irão desenvolver uma ou mais infecções uma vez durante a vida, com 6 a 9% dos indivíduos desenvolvendo infecções recorrentes. Diante deste contexto, buscou-se avaliar neste estudo o potencial antifúngico do (R)-(+)-citronelal [(R)-(+)-CT] isolado e associado a agentes terapêuticos de importância clínica. O enantiômero foi solubilizado em tween 80 e dimetilsulfóxido (DMSO). Posteriormente diluiu-se em água destilada estéril até a concentração de 2048µg/mL. A concentração inibitória mínima (CIM) do produto foi determinada por microdiluição em meio RPMI-1640 obtendo diluições de 4-1024µg/mL. A concentração fungicida mínima (CFM) foi determinada pela técnica de esgotamento em agar Sabouraud dextrose (ASD) a partir de alíquotas de 1mL da CIM, CIM × 2 e CIM × 4. A CIM e a CFM do (R)-(+)-CT para 90% das cepas de C. albicans foram 16 e 32µg/mL respectivamente. No ensaio de suscetibilidade, C. albicans apresentou alta resistência ao fluconazol e ao itraconazol, 12 (92.30%) das cepas. No em tanto, para o cetoconazol e o miconazol a resistência foi de 4 (30.76%) e 3 (23.07%) das cepas respectivamente. No ensaio de combinação do (R)-(+)-CT com cetoconazol e miconazol, a resistência foi completamente revertida. Para o fluconazol e o itraconazol, a resistências foi revertida em 9 (75%) e 7 (58.33%) das cepas respectivamente. O (R)-(+)-CT apresentou atividade fungicida com CFM igual à CIM × 2. Quando em combinação com cetoconazol, fluconazol, itraconazol e miconazol ampliou as zonas de inibição desses antifúngicos, diminuindo a resistência contra C. albicans.

Antifungal effect of 7-hydroxycitronellal against C. Tropicalis strains: an in vitro approach / Efeito antifúngico do 7-hidroxicitronelal contra cepas de C. Tropicalis: uma abordagem in vitro

The fungi of the genus Candida play a relevant role in the emergence of oral infections and are increasingly more frequent the cases of infections by non-albicans strains. In light of this context and the need for new alternatives to the antimicrobial therapy, the monoterpene [7-hidroxicitronelal] (7-HO) was evaluated for its antifungal effects. For the obtainment of the MIC and MFC values the broth microdilution method was used. The MIC and the MFC of this monoterpene for 60% of the tested strains was of 256µg/mL and 512µg/mL respectively. Furthermore, the standard antifungal nystatin (100UI/mL) was used as positive control for the inhibition of fungal growth. Therefore, were used 4 clinical strains of the species tropicalis (LM 06, LM 14, LM 31 and LM 36) and a standard strain (C. tropicalis ATCC 13803), originated from the Mycology collection of the Mycology Laboratory (LM) of the Health Sciences Center (CCS) of the Federal University of Paraiba (UFPB). The results obtained in this study showed fungicide activity of the compound (7-OH) against the strains of C. tropicalis.

Os fungos do gênero Candida tem um papel relevante no aparecimento de infecções orais e são cada vez mais frequentes os casos de infecções por cepas não-albicans. Diante deste contexto e da necessidade de novas alternativas para a terapia antimicrobiana, o monoterpeno [7-hidroxicitronelal] (7-HO) foi avaliado pelos seus efeitos antifúngicos. Para a obtenção dos valores da CIM e da CFM foi utilizado o método da microdiluição em caldo. A CIM e a CFM deste monoterpeno para 60% das cepas testadas foram de 256µg/mL e 512µg/mL respectivamente. Além disso, o antifúngico padrão nistatina (100UI/mL) foi utilizado como controle positivo para inibir o crescimento fúngico. Por tanto, foram utilizadas 4 cepas clínicas da espécie tropicalis (LM 06, LM 14, LM 31 e LM 36) e uma cepa padrão (C. tropicalis ATCC 13803), oriundas da Micoteca do Laboratório de Micologia (LM) do Centro de Ciências da Saúde (CCS) da Universidade Federal da Paraíba (UFPB). Os resultados obtidos neste estudo mostraram atividade fungicida do composto (7-OH) contra as cepas de C. tropicalis.

Involvement of Potassium Channels in Vasorelaxant Effect Induced by Valeriana prionophylla Standl. in Rat Mesenteric Artery.

Assays in vitro and in vivo were performed on extract from roots and leaves from the Valeriana prionophylla Standl. (VPR and VPF, resp.). In phenylephrine (1 µ M) precontracted rings, VPR (0.01-300 µ g/mL) induced a concentration-dependent relaxation (maximum response (MR) = 75.4 ± 4.0%, EC50 = 5.97 (3.8-9.3) µ g/mL, n = 6]); this effect was significantly modified after removal of the endothelium (EC50 = 39.6 (27.2-57.6) µ g/mL, P < 0.05). However, VPF-induced vasorelaxation was less effective compared to VPR. When rings were preincubated with L-NAME (100 µ M) or indomethacin (10 µ M), the endothelium-dependent relaxation induced by VPR was significantly attenuated (MR = 20.9 ± 2.3%, 34.2 ± 2.9%, resp., P < 0.001). In rings denuded endothelium, precontracted with KCl (80 mM), or in preparations pretreated with KCl (20 mM) or tetraethylammonium (1 or 3 mM), the vasorelaxant activity of VPR was significantly attenuated (MR = 40.0 ± 8.2, n = 5; 50.5 ± 6.0%; 49.3 ± 6.4%; 46.8 ± 6.2%; resp., P < 0.01). In contrast, neither glibenclamide (10 µ M), barium chloride (30 µ M), nor 4-aminopyridine (1 mM) affected VPR-induced relaxation. Taken together, these results demonstrate that hypotension induced by VPR seems to involve, at least in part, a vascular component. Furthermore, endothelium-independent relaxation induced by VPR involves K(+) channels activation, most likely due to BKCa channels, in the rat superior mesenteric artery.

Perfil enteroparasitológico dos habitantes de uma cidade do Nordeste do Brasil / Enteroparasitological profile of inhabitants from a city of Northeast Brazil

JUSTIFICATIVA E OBJETIVOS: A elevada prevalência de parasitoses em países subdesenvolvidos e em desenvolvimento, é responsável por quadros clínicos variáveis, os quais, frequentemente, encontram-se associados à diarreia crônica e à desnutrição.O objetivo deste estudo foi traçar o perfil enteroparasitológico dos habitantes de um município do nordeste do Brasil. MÉTODO: Estudo retrospectivo, com dados secundários, realizado no período de janeiro de 2009 a janeiro de 2010. Todas as informações foram obtidas por meio dos laudos dos exames coproparasitológicos.Para a análise estatística, utilizou-se os testes Qui-quadrado e Exato de Fisher, com o auxílio do programa estatístico R. O nível de significância adotado foi de 5% (p < 0,05).RESULTADOS: Observou-se que 42,07% da amostra analisada possuíam pelo menos uma espécie de parasita intestinal, além disso, que o helminto Ascaris lumbricóides e o protozoário Endolimaxnana foram os parasitas mais frequentes nesses exames positivos,com porcentagem de 6,93% e 13,59%, respectivamente. Constatou-se também que os parasitas ancilostomídeos e Giardia lamblia estiveram mais frequentes nos homens e o parasita Endolimax nana nas mulheres, e que o parasita Giardia lamblia foi o mais frequente nos pacientes menores de cinco anos de idade.CONCLUSÃO: Verificou-se ser alta a frequência de indivíduos parasitados, bem como que espécies de parasitas com potencial patogênico fazem parte do perfil parasitológico da referida população.

BACKGROUND AND OBJECTIVES: The high prevalence of parasitic diseases in underdeveloped and developing countries is responsible for variables clinical symptoms, which often are associated with chronic diarrhea and malnutrition. The objective of this study was to obtain the enteroparasitological profile of inhabitants from a city of Northeast Brazil. METHOD: A retrospective study using secondary data was carried out, from January 2009 to January 2010. All information was obtained through the results of coproparasitological samples. The data were processed and analyzed using the Chi-square and Fisher Exact test, of the statistical software R. The level of significance was 5 % (p < 0.05).RESULTS: It was observed that 42.07% of the sample had at least one species of intestinal parasite, the helminth Ascaris lumbricoides and protozoa Endolimax nana were the most frequently positive in these tests, with a percentage of 6.93% and 13.59% respectively. It was also found that the parasites Giardia lamblia and hookworms were the most frequent in males and Endolimax nana was the most frequent in females. The parasite Giardia lamblia was the most frequent in patients under five years old. CONCLUSION: We found high frequency of infected individuals and the parasite species with potential pathogenic are presentat the profile of this population.