Cytotoxicity assessment of beta-lapachone in endothelial cells

The selective activity of an antineoplastic drug is related to its ability to promote cytotoxic action on tumor cells and preserve the integrity of non-neoplastic cells. Beta-lapachone is extracted from the sawdust of Ipe wood, a thick bark tree from the Ipe wood found in the Brazilian Cerrado biome. This study aimed to evaluate the cytotoxic action of beta-lapachone in an endothelial cell line. The EA.hy926 cells were seeded in two groups, G1 and G2, cultured and exposed to beta-lapachone at concentrations of 0.0, 0.01, 0.03, 0.1, 0.3, 1 and 3 & 956;M for 24 hours. G1 remained under normal cultivation conditions and G2 was subjected to oxidative stress through an ischemia and reperfusion assay, in a deoxygenated sealed chamber. The cytotoxicity assay was performed using the tetrazolium reduction method. In G1, the cytotoxicity ranged from 0.0 to 10.0%; and in G2 between 0.0 and 6.3%. No statistically significant difference was observed between the obtained values. Moreover, we found no cytotoxic action of beta-lapachone on endothelial cells, and the results point out that the drug might have preserved the cell’s integrity against oxidative stress under the conditions of this experiment. This promising result suggests the possibility of beta-lapachone as a chemotherapy drug with selective activity.

Identificación morfológica y comprobación de patogenicidad de agentes biológicos asociados Tabebuia rosea (Bertol) en etapa de vivero en Morelia (Risaralda) / Morphological identification of pathogenic agents associated with Tabebuia rosea (Bignoniaceae) in nursery stage in morelia (Risaralda)

Introducción. Las susceptibilidades de las plantaciones al ataque de organismos dañinos pueden ocasionar efectos nocivos para su desarrollo, cuando se considera que el nivel de daños ocasionado no se puede tolerar, es indispensable determinar acertadamente la naturaleza del agente causal, sea éste tipo biótico o abiótico; la acertada determinación del agente de un problema fitosanitario en un vivero o plantaciones forestale, se fundamenta en un análisis detallado de los factores que la pueden estar afectando. Tabebuia rosea o Guayacán rosado es una especie forestal nativa de amplia aceptación en el mercado, que presenta durante su etapa de vivero, limitantes en las fases de germinación, emergencia y sobrevivencia, por lo anterior el objetivo de esta investigación era la de Identificar morfológicamente los posibles agentes patógenos asociados a Tabebuia rosea en etapa de vivero y comprobar su patogenicidad. Metodología. Se tomaron plántulas de vivero, las cuales se les realizo un análisis de los signos y los síntomas para el aislamiento y siembra de zonas afectadas en agar papa dextrosa. En el cultivo mixto se identificó los posibles agentes patógenos, los cuales fueron sembrados para obtener cultivos puros, y utilizados en la prueba de patogenicidad, para la inoculación de las estructuras sanas (hojas, peciolos y tallos) y su respectivo control. Resultados. Se identificaron tres géneros de hongos Colletotrichum, Mucor, y Candida, y un género de nematodo denominado Meloidogyne. La prueba de patogenicidad para Colletotrichum y Candida mostraron relaciones significativas en el proceso de infección principalmente en estructuras foliares. Se concluye en este trabajo dos nuevos posibles géneros patógenos para Tabebuia rosea evidenciados en la prueba de patogenicidad. Y se corrobora que el género Meloidogyne es un patógeno severo en el guayacán rosado que ocasiona anomalías morfológicas en la raíz; cabe resaltar que es el primer reporte para el departamento de Risaralda

Introduction. The susceptibilities of plantations to attack by harmful organisms can cause harmful effects for their development, when it is considered that the level of damage caused cannot be tolerated, it is essential to correctly determine the nature of the causal agent, be it biotic or abiotic; The correct determination of the agent of a phytosanitary problem in a nursery or forest plantations is based on a detailed analysis of the factors that may be affecting it. Tabebuia rosea or pink Guayacán is a native forest species widely accepted in the market, which presents, during its nursery stage, limitations in the germination, emergence and survival phases, therefore the objective of this research was to morphologically identify the possible pathogens associated with Tabebuia rosea in the nursery stage and check its pathogenicity. Methodology. Nursery seedlings were taken, which were analyzed for signs and symptoms for the isolation and sowing of affected areas on potato dextrose agar. In the mixed culture, possible pathogens were identified, which were sown to obtain pure cultures, and used in the pathogenicity test, for the inoculation of healthy structures (leaves, petioles and stems) and their respective control. Results. Three fungal genera Colletotrichum, Mucor, and Candida, and a nematode genus named Meloidogyne were identified. The pathogenicity test for Colletotrichum and Candida showed significant relationships in the infection process mainly in leaf structures. Two new possible pathogenic genera for Tabebuia rosea evidenced in the pathogenicity test are concluded in this work. And it is corroborated that the genus Meloidogyne is a severe pathogen in the pink guayacán that causes morphological anomalies in the root; It should be noted that it is the first report for the department of Risaralda

Beta Lapachone blocks the cell cycle and induces apoptosis in canine osteosarcoma cells / Beta Lapachona bloqueia o ciclo celular e induz apoptose em células de osteossarcoma canino

Osteosarcoma is a malignant tumor of primitive bone cells with a high incidence in dogs and humans. The need for more effective drugs with less adverse consequences has pushed the development of chemotherapeutic agents from plants and other natural sources. The aim of this study was to verify the cytotoxic effects of beta-lapachone, a compound present in the sawdust of Tabebuia sp. (popularly known as ipê) wood, on canine osteosarcoma cells subcultured and treated in different concentrations (0.1µm, 0.3µm e 1.0µm) and exposure times (24h, 48h e 72h). Results were obtained through Trypan blue dye exclusion, tetrazolium reducing method, cell survival assay, Annexin V-FITC and Propidium Iodine labeling, JC-1 dye labeling and cell cycle kinetics e analysis. The group treated with 0.3µm beta-lapachone presented higher decrease in cell viability (80.27%, 24h, 47.41%, 48h and 35.19%, 72h) and greater progression of cytotoxicity (19.73%, 24h, 52.59%, 48h and 64.81%, 72h). The lower IC50 (0.180µm) was verified in the group treated for 72 hours. Cell growth after treatment decreased as concentration and time of exposure increased, with 0.50% survival fraction at the concentration of 1.0µm. Initial apoptosis was the most frequent type of cell death in all groups, reaching bottom in the 24-hour group treated with 0.1µm (4.26%) and peaking in the 72-hour group treated with 1.0µm (85.89%). Mitochondrial depolarization demonstrated a dose-dependent phenomenon, indicating the intrinsic apoptosis. Cell growth inhibition by blocking cell cycle in the G0/G1 phase related to the exposure the time. β-lapachone is cytotoxic for canine osteosarcoma cells, induces apoptosis and promotes cell cycle arrest in G0/G1 phase.(AU)

O osteossarcoma é o tumor maligno das células ósseas primitivas, com alta incidência em cães e humanos. A necessidade de medicamentos mais efetivos, com menor consequência adversa, tem gerado esforços para o desenvolvimento de agentes quimioterápicos compostos por plantas e outras fontes naturais. O objetivo deste estudo foi verificar os efeitos citotóxicos da beta lapachona, um composto presente na serragem da madeira do ipê, sobre células de osteossarcoma canino subcultivadas e submetidas ao tratamento, de acordo com as diferentes concentrações (0.1µm, 0.3µm e 1.0µm) e tempo de exposição (24h, 48h e 72h). Os resultados foram obtidos por meio dos métodos de exclusão do corante azul de Tripan e de redução do tetrazólio, além dos ensaios de sobrevivência celular, de dupla marcação com Anexina V-FITC e Iodeto de Propídio, de marcação com o corante JC-1 e pela análise da cinética do ciclo celular. O grupo tratado com 0.3µm de beta lapachona apresentou melhor regressão da viabilidade celular (80,27%, 24h; 47,41%, 48h e 35,19%, 72h) e maior progressão da citotoxicidade (19,73%, 24h; 52,59%, 48h e 64,81%, 72h). O menor IC50 (0.180µm) ocorreu no grupo tratado por 72 horas. O crescimento celular após o tratamento foi menor, de acordo com o aumento da concentração e tempo de exposição, apresentando 0,50% de fração de sobrevivência na concentração de 1.0µm. A apoptose inicial foi o tipo de morte celular mais frequente em todos os grupos, menor no grupo de 24 horas tratado com 0.1µm (4,26%) e maior no grupo de 72 horas tratado com 1.0µm (85,89%). A despolarização mitocondrial ocorreu de maneira dose dependente, indicando a ocorrência de apoptose intrínseca. A β lapachona possui efeitos citotóxicos em células de osteossarcoma canino, induz apoptose e promove o bloqueio do ciclo celular na fase G0/G1.(AU)

The Antinociceptive Effect of the Leaves and Flowers Ethanolic Extracts of Tabebuia aurea (Silva Manso) Benth & Hook. F. ex S. Moore

ABSTRACT In view of the traditional use of Tabebuia aurea for treating pain and inflammation, the antinociceptive pharmacological potential of T. aurea ethanolic extracts (TAEE) was investigated through in vivo experimental models. First, the MTT assay was conducted to determine the potential cytotoxicity of the TAEEs. Afterwards, the acetic acid-induced writhing test and the formalin-, and glutamate-induced nociception tests were performed on Swiss adult mice treated with TAEEs (100 and 200 mg/kg doses, p.o.), or saline solution (control groups, 10mL/kg, p.o.), or standard drugs: dipyrone 40 mg/kg (p.o.), and morphine 5,7 mg/kg (i.p). In the MTT assay, none of the tested concentrations demonstrated signals of cytotoxicity. In the in vivo experimental models of acetic acid-induced writhing and glutamate-induced nociception, all TAEEs doses were able to statistically reduce the nociceptive response. However, the TAEEs did not show significant decrease in the amount of time that the animals spent licking the stimulated paw in the neurogenic phase of formalin-induced nociception test, differently of what was observed in the inflammatory phase. The results showed that T. aurea species induce an antinociceptive effect in rodents, which encourages the study of new drugs and contributes to the research on natural products.

Evaluation of antipyretic, sedative and hypnotic activities of methanol extract of Tabebuia hypoleuca (C. Wright ex Sauvalle) Urb. stems / [Evaluación de la actividad antipirética, sedante e hipnótica del extracto metanólico de los tallos de Tabebuia hypoleuca (C. Wright ex Sauvalle) Urb

Species of the genus Tabebuia are used in traditional medicine and are reported in the literature for their properties against various diseases. The objective of this study was to evaluate the antipyretic, sedative and hypnotic activities of methanol extract of Tabebuia hypoleuca stems (THME) using the Brewer's yeast induced pyrexia, Open field and Sodium thiopental-induced sleeping time tests, respectively. In the Brewer's yeast induced pyrexia test, THME at 500 mg/kg produced a significant (p<0.001) decrease of the fever as from the first hour after administration and was sustained for 4 h. In the Open-field test, THME did not cause any significant change in the number of crossings, rearing, preening and defecation, and either in the time of immobility. Moreover, THME did not produce changes in neither the sleeping latency nor the sleeping time induced by sodium thiopental. These results showed that THME administered orally at 500 mg/kg exerts antipyretic activity, probably mediated by the inhibition of the enzyme cyclooxygenase-2. This study also showed that THME does not exert sedative and hypnotic effects at the doses tested.

Especies del género Tabebuia se utilizan en la medicina tradicional y se reportan en la literatura por sus propiedades contra diversas enfermedades. El objetivo de este estudio fue evaluar la actividad antipirética, sedante e hipnótica del extracto metanólico de los tallos de Tabebuia hypoleuca (THME) utilizando las pruebas de pirexia inducida por levadura de cerveza, campo abierto y tiempo de sueño inducido por tiopental sódico respectivamente. En el ensayo de pirexia inducida por levadura de cerveza, THME a 500 mg/kg produjo una reducción significativa (p<0.001) de la fiebre a partir de la primera hora después de la administración y se mantuvo durante cuatro horas. En el ensayo de campo abierto, THME no causó ningún cambio significativo en el número de cruces, levantamientos, acicalamientos y defecación, ni en el tiempo de inmovilidad. Además, THME no produjo cambios ni en la latencia de sueño, ni en el tiempo de sueño inducido por tiopental sódico. Estos resultados mostraron que THME administrado oralmente en dosis de 500 mg/kg posee actividad antipirética, mediado probablemente a la inhibición de la enzima ciclooxigenasa-2. Este estudio también demostró que THME no posee actividad sedante e hipnótica en las dosis ensayadas.

Effects of changes in micro-weather conditions on structural features, total protein and carbohydrate content in leaves of the Atlantic rain forest tree golden trumpet (Tabebuia chrysotricha) / Efeito de alterações nas condições micro-climáticas sobre características estruturais, e proteína e carboidratos histoquimicamente marcados, de folhas da árvore da floresta Atlântica ipê amarelo

Abstract Golden trumpet, Tabebuia chrysotricha, is a native tree from the Brazilian Atlantic rain forest, with a broad latitudinal distribution. In this study, we investigated the potential effects of short-term changes in micro-weather conditions on structural features, and total protein and carbohydrate content of golden trumpet leaves, using structural and histochemical approaches. Leaves were harvested in four different micro-weather conditions: 1. Afternoon, after a hot, sunny day; 2. at dawn, after a previously hot, sunny day; 3. at noon, of a hot, sunny day; and 4. at noon, of a cold, cloudy day. Leaflets exposed to low light irradiance showed flattened chloroplasts, uniformly distributed within the cells, throughout the palisade parenchyma. Conversely, leaflets exposed to high light irradiance presented flattened and rounded chloroplasts, in the upper and lower palisade parenchyma cells, respectively. The strongest protein staining was found for leaves harvested at the coldest period, whereas the weakest protein staining was found for leaves harvested after a hot, sunny day. The largest and most numerous starch grains were found for leaves harvested in the afternoon, after a hot, sunny day. Conversely, the smallest and less numerous starch grains were found for leaves harvested at dawn. Analysis of the data reported herein suggests that the leaflet responses to transient changes in micro-weather conditions are likely to contribute to the golden trumpet successful establishment in the broad latitudinal distribution in which the species is found.

Resumo Ipê amarelo é uma árvore nativa da floresta Atlântica brasileira, encontrada em uma ampla distribuição latitudinal. Neste estudo, nós investigamos os efeitos potenciais de alterações de curto prazo nas condições micro-climáticas sobre características estruturais, proteína e carboidratos histoquimicamente marcados, de folhas de ipê amarelo, usando estratégias de análise estrutural e histoquímicas. As folhas foram marcadas em quatro condições microclimáticas distintas: 1. Tarde, após um dia quente e ensolarado; 2. Amanhecer, após um dia quente e ensolarado; 3. Ao meio-dia, de um dia quente e ensolarado; e 4. Ao meio-dia, de um dia frio e nublado. Folíolos expostos à baixa irradiância luminosa apresentaram cloroplastos achatados, uniformemente distribuídos no interior das células, por todo o parênquima paliçádico, enquanto que folíolos expostos à alta irradiância apresentaram cloroplastos achatados e arredondados, nas células superiores e inferiores do parênquima paliçádico, respectivamente. A marcação mais intensa para proteína foi observada para folhas coletadas no momento mais frio de coleta, enquanto que a marcação mais fraca foi observada para folhas coletadas após um dia quente e ensolarado. Os grãos de amido maiores e mais numerosos foram observados em folhas coletadas durante a tarde de dia quente e ensolarado, enquanto que os menores e menos numerosos grãos de amido foram observados em folhas coletadas ao amanhecer.

Germinación de semillas de cuatro especies arbóreas del bosque seco tropical del Valle del Cauca, Colombia / Seed germination of four tree species from the tropical dry forest of Valle del Cauca, Colombia

The ecological restoration strategies for highly threatened ecosystems such as the tropical dry forest, depend on the knowledge of limiting factors of biological processes for the different species. Some of these include aspects such as germination and seed longevity of typical species present in those forests. In this study, we evaluated the effect of light and temperature on seed germination of two Fabaceae (Samanea saman and Jacaranda caucana) and two Bignoniaceae (Pithecellobium dulce and Tabebuia rosea) species having potential use in restoration, and we analyzed the seed storage behavior of these species for a three months period. To study the light effect, four levels of light quality on seeds were used (photoperiod of 12 hours of white light, darkness and light enriched in red and far-red, both for an hour each day), and we combined them with three levels of alternated temperatures (20/25, 20/30 and 25/30°C-16/8h). For the storage behavior, two levels of seed moisture content particular for each species were used (low: 3.5-6.1% and high: 8.3-13.8%), with three storage temperatures (20, 5 and -20°C) and two storage times (one and three months). The criterion for germination was radicle emergence which was measured in four replicates per treatment, and was expressed as percentage of germination (PG). There were significant differences in germination of Samanea saman and Jacaranda caucana among light and temperature treatments, with the lowest value in darkness treatments, whereas germination of Pithecellobium dulce and Tabebuia rosea did not differ between treatments (PG>90%). The most suitable temperature regime to promote germination in all species was 25/30°C. These four species showed an orthodox seed storage behavior. We concluded that seeds of P. dulce, J. caucana and T. rosea did not have an apparent influence of all light conditions tested in their germination response, which might confer advantages in colonization and establishment processes, while S. saman did not germinate well in darkness. We suggest the use of seeds of P. dulce, J. caucana and T. rosea in ecological restoration processes, due to their tolerance and germination under a wide range of temperature and light conditions. Futhermore, seeds of S. saman might be used in open areas such as forest gaps.

Las estrategias de restauración ecológica en ecosistemas altamente amenazados como el bosque seco tropical, dependen del conocimiento de factores limitantes de procesos biológicos, como la germinación y la longevidad de semillas de especies típicas de los mismos. En este estudio se evaluó el efecto de la luz y la temperatura en la germinación de semillas de dos especies de Fabaceae y dos de Bignoniaceae potencialmente útiles para restauración, y se determinó su comportamiento en el almacenamiento. Para el primer objetivo, se utilizaron cuatro niveles de calidad lumínica (fotoperiodo con 12 horas de luz, oscuridad y estímulos de luz enriquecida en rojo y luz enriquecida en rojo lejano, ambas por una hora), combinados con tres niveles de temperaturas alternadas (20/25, 20/30 y 25/30°C - 16/8h). Para el segundo objetivo, se utilizaron dos niveles de contenido de humedad de las semillas, con tres niveles de temperatura de almacenamiento (20, 5 y -20°C) y dos tiempos de almacenamiento (1 y 3 meses). La variable de respuesta para ambos experimentos fue el número de semillas germinadas, expresado en porcentaje (PG). Samanea saman y Jacaranda caucana presentaron un PG significativamente diferente entre los tratamientos lumínicos, con el valor menor en la oscuridad, mientras Pithecellobium dulce y Tabebuia rosea no presentaron diferencias significativas entre tratamientos (PG>90%). La respuesta a la temperatura mostró que 25/30°C es el régimen más adecuado para promover la germinación de la mayoría de las especies. Las semillas de las cuatro especies evaluadas presentaron un comportamiento ortodoxo en el almacenamiento. Se concluye que las semillas de P. dulce, J. caucana y T. rosea son indiferentes a las condiciones de luz y temperatura probadas, confiriéndoles ciertas ventajas en procesos de colonización y establecimiento frente a S. saman, cuya germinación no se ve favorecida en la oscuridad. Se sugiere el uso de semillas de P. dulce, J. caucana y T. rosea en proyectos de restauración ecológica del bosque seco Tropical, debido a su tolerancia y germinación en condiciones ambientales con intervalos amplios de temperatura y luminosidad. Mientras que, semillas de S. saman podrían ser usadas en sitios abiertos como claros de bosques.

Avaliação do potencial biológico da Tabebuia aurea (Silva Manso) como fonte de moléculas bioativas para atividade antimicrobiana, antiedematogênica e antirradicalar / Biological potential assessment of Tabebuiaaurea (Silva Manso) as a source of bioactive molecules for antimicrobial, antiedematogenic and antiradical activity

RESUMO As espécies da família Bignoniaceae e do gênero Tabebuia são amplamente utilizadas na medicina tradicional e possuem um forte potencial terapêutico. Diante disso, objetivou-se avaliar o potencial biológico da Tabebuia aurea, determinando a atividade antimicrobiana; por meio do método da microdiluição em caldo, para a determinação da Concentração Inibitória Mínima (CIM); antiedematogênica, pelo ensaio de edema de orelha induzido por capsaicina; e antirradicalar, frente ao radical DPPH. Os extratos etanólicos de T. aurea não evidenciaram citotoxicidade, exceto o extrato etanólico da flor nas concentrações > 0,5 mg mL-1. O extrato etanólico da flor foi ativo com ação bactericida frente a S. epidermidis (CIM de 0,06 mg mL-1) enquanto o extrato etanólico da folha foi moderadamente ativo frente a S. epidermidis (CIM: 0,25 mg mL-1) e S. aureus (CIM: 0,50 mg mL-1) sugerindo ação bacteriostática para ambas as linhagens. Os dois extratos apresentaram ação antiedematogênica, com inibição do edema de 40,50% pelo extrato etanólico da flor e de 41,73% pelo extrato da folha. T. aurea não apresentou atividade antirradicalar. Os resultados comprovam o perfil antibacteriano e antiedematogênico com ausência de citotoxidade pela T. aurea. Sugere-se a continuação dos testes com frações e substâncias isoladas das flores e folhas da referida espécie vegetal, bem como de experimentos in vivo, como forma de agregar evidências visando à busca de novos fitoterápicos.

ABSTRACT The species of Bignoniaceae family and genus Tabebuia are widely used in the traditional medicine and have a great therapeutic potential. The aim of the current research was to evaluate the biological potential of the Tabebuia aurea, determining its antimicrobial activity by the microdilution broth method, to predict the anti-edematogenic Minimum Inhibitory Concentration (MIC) by ear edema assay induced by capsaicin; and the antiradical one, towards DPPH. The ethanol extracts of T. aureashowed no cytotoxicity, except for the flower ethanol extract in concentrations above > 0.5 mg mL-1. The ethanol extract of the flower was active, with bactericidal action, against S. epidermidis (MIC 0.06 mg ml-1) and the ethanol extract of moderately active recto S. epidermidis (CIM: 0.25 mg mL-1) and S. aureus (MIC: 0.50 mg mL-1) were bacteriostatic for both strains. Both extracts had antiedematogenic action on the inhibition of edema of 40.50% by the ethanol extract of the flower and 41.73% by leaf extract. T. aurea did not show antiradical activity. The results indicate the antibacterial and antiedematogenic profile with no cytotoxicity by the T. aurea. It suggests the continuation of tests with isolated fractions and substances of flowers and leaves of that plant species as well as in vivo trials, in order to enhance the evidences targeted on finding new herbal medicines.

Antibacterial activity of ifve Peruvian medicinal plants against Pseudomonas aeruginosa

Objective:To evaluate the susceptibility of Pseudomonas aeruginosa (P. aeruginosa) in vitro to the ethanolic extracts obtained from five different Peruvian medicinal plants. Methods:The plants were chopped and soaked in absolute ethanol (1:2, w/v). The antibacterial activity of compounds against P. aeruginosa was evaluated using the cup-plate agar diffusion method. Results:The extracts from Maytenus macrocarpa (“Chuchuhuasi”), Dracontium loretense Krause (“Jergon Sacha”), Tabebuia impetiginosa (“Tahuari”), Eucalyptus camaldulensis Dehn (eucalyptus), Uncaria tomentosa (“U?a de gato”) exhibited favorable antibacterial activity against P. aeruginosa. The inhibitory effect of the extracts on the strains of P. aeruginosa tested demonstrated that Tabebuia impetiginosa and Maytenus macrocarpa possess higher antibacterial activity. Conclusions:The results of the present study scientifically validate the inhibitory capacity of the five medicinal plants attributed by their common use in folk medicine and contribute towards the development of new treatment options based on natural products.

Antibacterial activity of five Peruvian medicinal plants against Pseudomonas aeruginosa

Objective: To evaluate the susceptibility of Pseudomonas aeruginosa (. P. aeruginosa) in vitro to the ethanolic extracts obtained from five different Peruvian medicinal plants. Methods: The plants were chopped and soaked in absolute ethanol (1:2, w/v). The antibacterial activity of compounds against P. aeruginosa was evaluated using the cup-plate agar diffusion method. Results: The extracts from Maytenus macrocarpa ("Chuchuhuasi"), Dracontium loretense Krause ("Jergon Sacha"), Tabebuia impetiginosa ("Tahuari"), Eucalyptus camaldulensis Dehn (eucalyptus), Uncaria tomentosa ("Uña de gato") exhibited favorable antibacterial activity against P. aeruginosa. The inhibitory effect of the extracts on the strains of P. aeruginosa tested demonstrated that Tabebuia impetiginosa and Maytenus macrocarpa possess higher antibacterial activity. Conclusions: The results of the present study scientifically validate the inhibitory capacity of the five medicinal plants attributed by their common use in folk medicine and contribute towards the development of new treatment options based on natural products.

Aspidosperma subincanum I. characterisation, extraction of an uleine-enriched fraction and potential health hazard due to the contaminant ellipticine

The bark of the Brazilian tree Aspidosperma subincanum Mart. ex A. DC., Apocynaceae, has been characterised, and its constituents concentrated to obtain an uleine-enriched extract with the aim to produce food supplements. The concentration of the contaminant alkaloid ellipticine was assessed, and its potential to elicit toxic effects on consumers evaluated. It was found that this alkaloid posited no danger.

Nitric oxide inhibitory activity of hydrogenated synthetic analogues of furanonaphthoquinones isolated from Tabebuia spp

Objective: to describe the synthesis of analogues of furanonaphthoquinones isolated from Tabebuia genus and their inhibitory effect on nitric oxide production. Methods: a series of six derivatives were prepared through cycloaddition reactions and the products characterized by spectroscopy methods. The biological activity was evaluated measuring their effect on the pro-inflammatory mediator production in macrophages RAW 264.7 induced with lipopolysaccharides. To prevent compounds from interfering with cellular viability, their cytotoxic effect was determined using methyl tetrazolium assay. Additionally, scavenging effect was in vitro measured. Results: FNQ1, FNQ2, and FNQ5 derivatives showed potent concentration-depending inhibitory effect on nitric oxide production, with an IC50 value lower than 2 µM concentration at which they did not have toxic or scavenging effects. FNQ5 was the most active and selective derivative. Conclusions: this is the first paper concerning the anti-inflammatory potential of tested synthetic compounds. Our results indicated that FNQ5 might be considered as useful potential anti-inflammatory molecule to treat inflammatory diseases related with nitric oxide overproduction(AU)

Objetivo: describir la síntesis de análogos de furanonaftoquinonas aisladas del género Tabebuia y su efecto inhibidor en la producción de óxido nítrico. Métodos: se obtuvo una serie de seis derivados a través de reacciones de cicloadición y se caracterizaron los productos por métodos espectroscópicos. Se evaluó la actividad biológica por su efecto en la producción del mediador proinflamatorio en macrófagos RAW 264.7 activados con lipopolisacárido. Para asegurar que los compuestos no interfirieran con la viabilidad celular, se evaluó su efecto citotóxico empleando el ensayo de metiltetrazolio. Adicionalmente, se evaluó el efecto captador del radical in vitro. Resultados: los derivados FNQ1, FNQ2 y FNQ5 demostraron potente efecto inhibitorio en la producción de óxido nítrico de manera concentración-dependiente, con un valor de CI50 menor que 2 µM, concentración a la que no ejercieron efectos tóxicos o captadores de radicales. FNQ5 resultó el compuesto más activo y selectivo. Conclusiones: este trabajo es el primero que evalúa el potencial antinflamatorio de los compuestos sintetizados. Los resultados indican que FNQ5 puede ser considerada como una molécula de uso potencial para el tratamiento de enfermedades inflamatorias que cursen con sobreproducción de óxido nítrico(AU)

Anti-infectious activity in plants of the genus Tabebuia / Actividad anti-infecciosa en plantas del género Tabebuia / Atividade anti-infecciosa em plantas do género Tabebuia

Infectious diseases are a worldwide public health problem. There is growing research in the field of new plant-based drugs for treating such diseases. Our objective was to perform a systematic literature review to evaluate the anti-infectious activity (antibacterial, antifungal, antiviral and antiparasitic) attributed to plants of the Tabebuia (Bignoniaceae) genus. We conducted a search for the period of 2000-2013 in ScienceDirect, Scopus, PubMed, Embase, Napralert and SciELO databases using the following MeSH terms: Tabebuia, biological activity, bioactive compounds, chemical compounds, diseases, traditional medicine, tropical infections, infections and treatment. We found ethnobotanical and experimental (in vitro) evidence supporting the use of Tabebuia species for treating infectious diseases. In addition, the compounds responsible for their antimicrobial activity have been isolated, and their structures have been elucidated, emphasizing among them naphthoquinones such as lapachol. Natural products isolated from Tabebuia plants may be an alternative for developing new anti-infectious agents.

Dada la importancia de las enfermedades infecciosas como problema de salud pública a nivel mundial y la búsqueda de nuevos medicamentos basados en plantas para tratar dichas enfermedades; se realizó una revisión sistemática de literatura con el fin de evaluar la actividad anti-infecciosa (antibacteriana, antifúngica, antiviral y antiparasitaria) reportada en plantas pertenecientes al género Tabebuia (Bignoniaceae). Las bases de datos fueron: ScienceDirect, Scopus, Pubmed, Embase y Napralert, SciELO, durante 2000 - 2013. Se utilizaron términos en MeSH como: Tabebuia, biological activity, bioactive compounds, chemical compounds, diseases, traditional medicine, tropical infections, infections and treatment. Existe evidencia tanto etnobotánica como experimental (in vitro) que soporta el uso de especies del género Tabebuia en el tratamiento de enfermedades infecciosas. Adicionalmente, se encontró reportado y se esclareció estructuralmente los compuestos responsables de la actividad antimicrobiana, donde se destacan naftoquinonas como el lapachol. Se concluye a partir de la revisión que los productos naturales aislados de las plantas del género Tabebuia podrían considerarse alternativas para el desarrollo de nuevos agentes anti-infecciosos.

Dada a importância das doenças infecciosas como problema de saúde pública a nível mundial e a procura crescente de novos medicamentos baseados em plantas para tratar tais doenças, realiza se uma pesquisa sistematizada da literatura com o fim de avaliar a atividade anti-infecciosa (antibacteriana, antifúngica, antiviral y antiparasitária) reportada em plantas pertenecientes ao género Tabebuia (Bignoniaceae). Foi realizada uma pesquisa nas bases de dados ScienceDirect, Scopus, Pubmed, Embase y Napralert, assim como em SciELO, durante o período 2000 - 2013, empregando os términos MeSH: Tabebuia, biological activity, bioactive compounds, chemical compounds, diseases, traditional medicine, tropical infections, infections and treatment. Existe evidencia tanto etnobotánica como experimental (in vitro) que suporta o uso das espécies do género Tabebuia no tratamento das doenças infecciosas e adicionalmente, há sido isolado e identificado estruturalmente os compostos responsáveis da sua atividade antimicrobiana, donde se destacam as naftoquinonas como o lapachol. Os produtos naturais isolados de plantas do género Tabebuia poderiam considerar se como uma alternativa para o desarrolho de novos agentes anti-infecciosos.

Actividad antiinflamatoria, antioxidante y antibacteriana de dos especies del género Tabebuia / Antiinflammatory, antioxidant and antibacterial activity of two species of Tabebuia genus

Introducción: Tabebuia rosea (Bertol.) A. DC. y Tabebuia ochracea (Cham.) Standl., que pertenecen a la familia Bignoniaceae, son utilizadas en la medicina popular por su potencial farmacológico como antiinflamatorio y antibacteriano, lo que ha motivado su estudio químico y biológico. Objetivos: determinar la actividad antiinflamatoria, antioxidante y antibacteriana de extractos totales etanólicos y fracciones en éter, diclorometano, acetato de etilo y etanol, obtenidas a partir de la corteza interna de Tabebuia rosea y Tabebuia ochracea. Métodos: el material vegetal se extrajo por maceración con etanol y se fraccionó mediante procedimientos de partición líquido/líquido. La actividad antiinflamatoria se evaluó utilizando el modelo murino in vivo de edema auricular inducido por 13-acetato de 12-orto-tetradecanoilforbol, mientras que la actividad antioxidante y antibacteriana se determinó in vitro, utilizando el método de captación del radical 2,2-difenil-1-picrilhidrazilo y métodos de difusión en agar, respectivamente.Resultados: los extractos etanólicos de la corteza de Tabebuia rosea y Tabebuia ochracea, así como algunas de sus fracciones, mostraron significativa actividad antiinflamatoria y antioxidante; en términos generales Tabebuia rosea resultó más activa como antiinflamatoria, mientras que en cuanto a la actividad antioxidante Tabebuia ochracea mostró ser más potente. Ambas especies de Tabebuia presentaron importante actividad antibacteriana frente a Staphylococcus aureus ATCC25923. Conclusiones: se demostró actividad antiinflamatoria, captadora de radicales libres 2,2-difenil-1-picrilhidrazilo y antibacteriana, en extractos totales y fracciones obtenidas de Tabebuia rosea y Tabebuia ochracea. Este constituye el primer reporte que valida el uso popular dado a estas especies como antiinflamatorio y antibacteriano, en la costa norte colombiana.

Introduction: Tabebuia rosea (Bertol.) A. DC. and Tabebuia ochracea (Cham.) Standl., belonging to the Bignoniaceae family, are widely used in folk medicine because of their antiinflammatory and antibacterial potentialities, all of which has prompted the chemical and biological study of these species. Objectives: to evaluate the antiinflammatory, antioxidant and antibacterial activity of the total ethanolic extracts and fractions obtained from the inner bark of Tabebuia rosea and Tabebuia ochracea by using ether, dichloromethane, ethyl acetate and ethanol. Methods: plant material was extracted through maceration with ethanol and fractionated through liquid-liquid partition method. The evaluation of antiinflammatory action used the 12-O-tetradecanoylphorbol-13-acetate induced ear edema in mice, whereas the antioxidant and antibacterial activities were determined in vitro, using the 2,22 -diphenyl-1-picrylhydrazyl radical scavenging method and agar well diffusion method, respectively. Results: ethanol extracts from Tabebuia rosea and Tabebuia ochracea inner bark, as well as some of their fractions showed significant antiinflammatory and antioxidant activity, being generally Tabebuia rosea more active as antiinflammatory. Regarding the antioxidant activity Tabebuia ochracea proved to be more potent. Both Tabebuia species revealed significant antibacterial activity against Staphylococcus aureus ATCC 25923. Conclusions: it was proven that total extracts and fractions obtained from Tabebuia rosea and Tabebuia ochracea had antiinflammatory, free radical DPPH scavenging capacity, and antibacterial activity. This is the first report which validates the popular use of these species as antiinflammatory and antibacterial agents in the north coast of Colombia.

In vitro antimalarial activity of fractions and constituents isolated from Tabebuia billbergii / Actividad antimalárica in vitro de fracciones y constituyentes aislados de Tabebuia billbergii

Introduction: in vitro antimalarial activity of naphthoquinones (1-5), isolated from Tabebuia billbergii (Bureau & K. Schum.) Standl., was investigated. Tabebuia billbergii, commonly known as guayacán, is a plant traditionally used in the Amazon in numerous conditions like bacterial and fungal infections, fever, syphilis, malaria, trypanosomiasis, as well as stomach and bladder disorders, and tumours. Objective: to study the dichloromethane extracts of both the trunk and the inner bark of Tabebuia billbergii and to demonstrate the antimalarial activity of some of its bioactive components. Methods: some bioactive components were evaluated for the antimalarial activity against Plasmodium berghei, by using the inhibition of the differentiation cycle of the parasite measure by the ³H-hypoxanthine incorporation and compared to that obtained for chloroquine. Results: conventional chromatographic techniques and bioassay-guided fractionation (Artemia salina) allowed isolating from the active fractions one naphthoquinone (lapachol) and four naphtho-furan-4,9-diones. These compounds proved to have an important antiplasmodial effect, with very encouraging IC50's, especially when compared to the results shown by Chloroquine in the same experiment. In addition, two triterpenes, β-sitosterol and stigmasterol, were obtained from the bark. Conclusions: the activity-guided fractionation (A. salina) of dichloromethane extracts of the trunk and the inner bark of Tabebuia billbergii led to the isolation and the identification of five quinonoid compounds with antiplasmodial effect. The significant inhibitory activity in vitro against Plasmodium berghei observed for compound 2-acetyl-naphtho-[2,3b]-furan-4,9-dione allow us to present them as a potential antimalarial compound.

Introducción: se evaluó la actividad antimalárica in vitro de una serie de naftoquinonas (1-5), aisladas de Tabebuia billbergii (Bureau & K. Schum.) Standl., que es conocida comúnmente como guayacán, una planta utilizada tradicionalmente en la Amazonía en numerosos problemas de salud como infecciones bacterianas y fúngicas, fiebre, sífilis, paludismo, tripanosomiasis, así como en problemas estomacales, tumores y trastornos de la vejiga. Objetivo: estudiar los extractos en diclorometano tanto del tronco como la corteza interna de Tabebuia billbergii y evaluar la actividad antimalárica de algunos de sus componentes bioactivos. Métodos: la actividad antimalárica contra Plasmodium berghei se evaluó en algunos componentes bioactivos, por la inhibición del ciclo de la diferenciación de la medida de los parásitos mediante la incorporación de 3H-hipoxantina y se comparó con la obtenida para la cloroquina. Resultados: a través de técnicas cromatográficas convencionales y el fraccionamiento guiado por bioensayo (Artemia salina) se aislaron de las fracciones activas, una naftoquinona (lapachol) y 4 nafto-furan-4,9-dionas. Estos compuestos presentaron un efecto antiplasmodial importante, con buenos valores de IC50, especialmente cuando se compara con los resultados mostrados por la cloroquina en el mismo experimento. Además, se obtuvieron de la corteza 2 triterpenos, β-sitosterol y estigmasterol. Conclusiones: el fraccionamiento guiado por Artemia salina de los extractos en diclorometano del tronco y la corteza interna de Tabebuia billbergii, condujo al aislamiento y la identificación de 5 compuestos de naturaleza quinoidal con efecto antiplasmódicol. La actividad in vitro contra Plasmodium berghei observada para el compuesto 2-acetil-nafto-[2,3 b]-furan-4,9-diona, permite proponerlo como un potencial compuesto antimalárico.

Antifungigrama para comprovar o potencial de ação dos extratos vegetais hidroglicólicos sobre Candida sp. (Berkhout) / Etest to confirm the action potential of plant hydroglycol extracts on Candida sp. (Berkhout)

A candidíase vaginal é uma doença causada, na maioria das vezes, pelo fungo do gênero Candida sp, que habita o trato gastrintestinal e geniturinário da espécie humana e pode tornar-se patogênico sob determinadas condições. A maioria dos indivíduos desenvolve defesas imunológicas que impedem a proliferação e desenvolvimento de candidíase localizada ou disseminada. Embora a causa exata do aumento de espécies não-albicans seja desconhecida, há evidências de que a própria terapia antifúngica possa estar contribuindo para o processo. Linhagens de C. glabrata são mais resistentes aos imidazólicos do que a C. albicans, sendo necessária uma concentração 10 vezes superior de miconazol para eliminar a C. glabrata quando comparada a C. albicans. Foi realizado um antifungigrama testando o potencial de ação de produtos vegetais sobre o fungo Candida sp. Foi observado que, ocorreu inibição do fungo no contato com os extratos hidroglicólicos das plantas Arctium lappa L., Calendula officinalis L., Stryphnodendron adstringens (Mart.) Coville e Tabebuia avellanedae Lorentz ex Griseb. A importância deste trabalho reside na possibilidade de desenvolvimento de tratamento complementar, menos agressivo, de menor custo e sem toxidade, o que possibilitaria melhor qualidade de vida para portadoras de candidíase vaginal recorrente ou não.

Vaginal candidiasis is a disease caused, in most cases, by the fungus of the genus Candida sp., which inhabits the gastrointestinal and genitourinary tracts of the human species and can become pathogenic under certain conditions. Most individuals develop immune defenses that prevent the proliferation and the development of localized or disseminated candidiasis. Although the exact cause of the increase in non-albicans species is unknown, there is evidence that antifungal therapy itself may have contributed to it. Strains of C. glabrata are more resistant to imidazole than C. albicans, and a 10-fold higher concentration of miconazole is required to eliminate C. glabrata compared to C. albicans. Etest was performed by testing the action potential of plant products on the fungus Candida sp. Inhibition of the fungus occurred when it was in contact with the hydroglycol extracts of plants Arctium lappa L., Calendula officinalis L., Stryphnodendron adstringens (Mart.) Coville and Tabebuia avellanedae Lorentz ex Griseb. The importance of this study lies in the possibility of developing a complementary treatment, less aggressive, of lower cost and without toxicity, which would allow better life quality for women with vaginal candidiases that are recurrent or not.

Estudo da ação antineoplásica da Tabebuia avellanedae (Ipê-Roxo) na carcinogênese induzida pelo azoximetano em camundongos / Study of the antineoplastic action of Tabebuia avellanedae in carcinogenesis induced by azoxymethane in mice

PURPOSE: To study the antitumor action of Tabebuia avellanedae in experimentally induced colon carcinogenesis by azoxymethane in mice. METHODS: Fifty (n=50) mice were divided into five groups: in group I azoxymethane (AOM) was administered, in Group II - β-lapachone, in group III - vehicle (diluent) and in group IV - vehicle + AOM and finally in group V - β-lapachone + AOM. RESULTS: It was observed the presence of aberrant crypt foci in all animals of groups I and IV, 50 percent in group II and 90 percent in group V. CONCLUSION: The β-lapachone extracted from the Tabebuia avellanedae showed no protective effect of lesions induced by azoxymethane in colon of mice.

OBJETIVO: Estudar a ação antitumoral da Tabebuia avellanedae (Ipê-Roxo) na carcinogênese colônica induzida experimentalmente pelo azoximetano em camundongos. MÉTODOS: Foram utilizados 50 camundongos divididos em 5 grupos: grupo I administrado Azoximetano (AOM); grupo II - β-lapachona; grupo III - veículo (diluente); grupo IV - veículo + AOM; e grupo V - β-lapachona + AOM. RESULTADOS: Observou-se presença de focos de criptas aberrantes em todos os animais dos grupos I e IV, 50 por cento no grupo II e 90 por cento no grupo V. CONCLUSÃO: A β-lapachona extraída da Tabebuia avellanedae não apresentou efeito protetor das lesões induzidas pelo azoximetano em cólon de camundongos.

Clinical Safety Test of the Long Term Intake of Tabebuia Avellanedae (Taheebo) in Cancer Patients / 日本補完代替医療学会誌

60 cancer patients between the ages of 20 and 80 who had completed a main treatment were randomly administered Tabebuia Avellanedae (Taheebo) extract 2.0 g/day (usual dosage), 4.0 g/day (2 times dosage), or 6.0 g/day (3 times dosage) for 6 months. A blood biochemical exam, urinalysis, adverse effects, several immunological parameters, urine 8-OHdG and QOLsurvey were evaluated. Five patients dropped out, but there was no direct cause and effect between the extract and dropout. Although several items of the blood biochemical exam revealed slight variation within the normal limits, distinct abnormities were not detected. Furthermore, side effects like allergic symptoms were not found. Immune parameters and urine 8-OHdG did not change significantly. CRP, which is a sensitive marker of inflammation, was significantly improved, and this may suggest the possibility of this extract helping to prevent hardening of blood vessels due to arteriosclerosis. In Japan, long-term food safety tests have rarely been done, therefore we recommend that more of these exams be carried out.<br>

Ausência de mutagenicidade e antimutagenicidade do extrato obtido das flores do ipê roxo [Tabebuia impetiginosa (Mart. ex DC.) Standl.] / Absence of mutagenicity and antimutagenicity of the extract obtained from the flowers of "ipê roxo" Tabebuia impetiginosa (Mart. ex DC.) Standl

A Tabebuia impetiginosa, conhecida popularmente como ipê-roxo, é uma planta nativa das florestas tropicais chuvosas da América do Sul e Central. Componentes químicos obtidos da casca têm mostrado efeito terapêutico, como antiinflamatório, antifúngico e antibacteriano. Porém, pela falta de dados na literatura, pouco se sabe sobre os efeitos do extrato das flores. Assim, o objetivo do presente trabalho foi avaliar o potencial mutagênico e antimutagênico do extrato obtido das flores da T. impetiginosa, em três diferentes concentrações (100, 300 e 500 mg kg-1 p.c.) pelo teste do micronúcleo. Para o teste de mutagenicidade, a doxorrubicina (DXR, 90 mg kg-1 p.c.) foi utilizada como indutor de danos no DNA e para o teste de antimutagenicidade, os tratamentos com o extrato foram realizados simultaneamente com este agente químico. O sangue periférico dos animais foi coletado 24 horas após os tratamentos. A comparação da frequência de eritrócitos policromáticos (PCEs) em 400 eritrócitos/animal entre os diferentes grupos não demonstrou qualquer citotoxicidade do extrato. Em relação às frequências de micronúcleos em PCEs (PCEMNs), não foram observadas diferenças significativas entre os grupos tratados com as diferentes concentrações de extrato e o controle negativo. Da mesma forma, todos os grupos de animais que receberam os tratamentos simultâneo do extrato (100, 300 ou 500 mg kg-1 p.c.) com a DXR, apresentaram valores de PCEMNs muito próximos quando comparados com os dados observados no grupo de animais que recebeu somente a DXR. Esses resultados apresentados indicam ausência de efeito mutagênico e antimutagênico do extrato obtido das flores da T. impetiginosa em sistema teste in vivo.

T. impetiginosa, known as "ipê-roxo", is a plant native to tropical rain forests of Central and South Americas. Chemical compounds obtained from its bark have shown anti-inflammatory, antifungal and antibacterial therapeutic effect. However, due to the lack of data in the literature, little is known about the effects of its flower extract. Thus, the aim of this study was to evaluate the mutagenic and antimutagenic potential of the extract obtained from T. impetiginosa flowers at three different concentrations (100, 300 and 500 mg kg-1 p.c.) by the micronucleus test. For the mutagenicity test, doxorubicin (DXR, 90 mg kg-1 p.c.) was used as DNA-damage inducer, while for the antimutagenicity test, treatments with the extract were performed simultaneously with this chemical agent. The peripheral blood of animals was collected 24 hours after the treatments. The frequency of polychromatic erythrocytes (PCEs) in 400 erythrocytes/animal was compared among the different groups and showed no extract cytotoxicity. As regards the frequency of micronuclei in PCEs (PCEMNs), there were no significant differences between the groups treated with different concentrations of extract and the negative control. Similarly, all groups of animals that received the simultaneous extract treatments (100, 300 or 500 mg kg-1 p.c.) with DXR showed very similar values of PCEMNs when compared with the data observed for the group of animals that received DXR alone. These results indicate no mutagenic and antimutagenic effect of the extract obtained from T. impetiginosa flowers in the testing system in vivo.

Produção de biomassa e estrutura do pasto de capim-andropogon em sistema silvipastoril e monocultura / Biomass production and pasture structure of Andropogon grass in a silvopastoral system and in monoculture

A produção de biomassa e as características estruturais do capim-andropogon foram avaliadas nas idades de rebrota de 35, 49 e 63 dias, em três ambientes de um sistema silvipastoril: sob a copa de pau-d'arco, sob a copa de jatobá, em área aberta; local fora da copa de qualquer árvore e em sistema de monocultura. O delineamento experimental foi o de parcelas subdivididas com cinco repetições. As parcelas foram representadas pelos ambientes e as subparcelas, pelas idades de rebrota. A luminosidade sob pau-d'arco, sob jatobá e em área aberta foi de 74, 62 por cento e 82 por cento, respectivamente, das áreas a pleno sol. Houve interação ambiente versus idade de rebrota. O sombreamento sob a copa de pau-d'arco e de jatobá não afetou a produção de matéria seca do capim-andropogon, contudo reduziu a altura do pasto aos 63 dias de rebrota. O percentual de folhas da forragem aos 35 dias de rebrota foi mais elevado na monocultura. Nas outras idades de rebrota, os quatro ambientes não diferiram entre si.

The biomass production and pasture structure of Andropogon grass were evaluated at 35, 49, and 63 days of regrowth, in three silvopastoral environments: under Pau-d'Arco and Jatobá trees, in open field and in monoculture system. The experiment was designed in split plot with five replications, the plots were the environments and the split plots were the regrowth ages. The luminosities under Pau-d'Arco, Jatobá, and open field were: 74, 62, and 82 percent, respectively, relative to the areas under full sun. There was interaction among environments and ages of regrowth. The shading under the canopy of Pau-d'Arco and Jatobá did not affect the production of dry matter of Andropogon grass; however, reduced the height of the grass at 63 days of regrowth. The percentage of leaves of forage at 35 days of regrowth was higher in monoculture. At other ages of regrowth, the four environments did not differ among themselves.