Mammea B/BA Isolated From the Seeds of Mammea americana L. (Calophyllaceae) is a Potent Inhibitor of Methicillin-Resistant Staphylococcus aureus.

Staphylococcus aureus remains a pathogen of high concern in public health programs worldwide due to antibiotic resistance and emergence of highly virulent strains. Many phytochemicals have demonstrated activity against S. aureus and other Gram-positive bacteria, but the minimum inhibitory concentration (MIC) values comparable to commonly used antibiotics are needed. In the present study, bio-guided fractionation of the ethanol extract of seeds of Mammea americana L. (Calophyllaceae) throughout the antibacterial activity, against S. aureus strains that are sensitive and resistant to methicillin, led to the isolation of four coumarins identified as mammea B/BA, mammea B/BC, mammea A/AA cyclo D and mammea A/AA cyclo F, and a mixture of mammea B/BA cyclo F plus mammea B/BD cyclo F. The extract inhibited the growth of S. aureus with MIC values of 2-4 µg/ml and Mammea B/BA (MaBBA) presented MIC values in a range between 0.5 and 1.0 µg/ml in six methicillin-sensitive strains and eight methicillin-resistant strains evaluated. We consider MaBBA the most potent of all mammea coumarins reported to date, according to the literature review carried out at the time of writing of this article. Toxicity assessment in vivo against the nematode Caenorhabditis elegans and in vitro against human fibroblasts of the extract and the compound MaBBA indicated that both had low toxicity.

Quiste aracnoideo sacro recidivante con meningocele anterior gigante: reporte de caso / Sacral arachnoid recurrent cyst with giant anterior meningocele: a case report

Los quistes aracnoideos corresponden a lesiones benignas expansivas del canal medular secundarias a defectos anatómicos durales, mientras que los meningoceles anteriores consisten en la herniación de la duramadre hacia la pelvis a través de forámenes dilatados o defectos óseos. Ambas entidades son infrecuentes y sus manifestaciones clínicas puede variar de acuerdo a estructuras anatómicas que comprimen. Una historia clínica completa, la pesquisa diagnóstica y la adecuada interpretación de imágenes orientan al diagnóstico y manejo de estos pacientes. Se presenta el caso de una paciente adulta mayor con historia de masa pélvica, dolor lumbar severo y monoparesia en quien se realizó el diagnóstico incidental de quiste aracnoideo sacro y meningioma sacro anterior.

Arachnoid cysts are benign expansive lesions of the spinal canal secondary to dural defects, whereas the anterior meningoceles consist of the herniation of the dura into the pelvis through dilated foramina or bone defects. Both pathologies are infrequent and its clinical manifestations vary according to compressed anatomical structures. A complete clinical history, the diagnostic investigation and the correct imaging studies interpretation guide the diagnosis and management of these patients. We present the case of an elderly adult patient with a history of pelvic mass, severe lumbar pain and monoparesis in whom the incidental diagnosis of sacral arachnoid cyst and anterior sacral meningioma was performed.

Susceptibility of Porphyromonas gingivalis and Streptococcus mutans to Antibacterial Effect from Mammea americana.

The development of periodontal disease and dental caries is influenced by several factors, such as microorganisms of bacterial biofilm or commensal bacteria in the mouth. These microorganisms trigger inflammatory and immune responses in the host. Currently, medicinal plants are treatment options for these oral diseases. Mammea americana extracts have reported antimicrobial effects against several microorganisms. Nevertheless, this effect is unknown against oral bacteria. Therefore, the aim of this study was to evaluate the antibacterial effect of M. americana extract against Porphyromonas gingivalis and Streptococcus mutans. For this, an experimental study was conducted. Ethanolic extract was obtained from seeds of M. americana (one oil phase and one ethanolic phase). The strains of Porphyromonas gingivalis ATCC 33277 and Streptococcus mutans ATCC 25175 were exposed to this extract to evaluate its antibacterial effect. Antibacterial activity was observed with the two phases of M. americana extract on P. gingivalis and S. mutans with lower MICs (minimum inhibitory concentration). Also, bactericidal and bacteriostatic activity was detected against S. mutans, depending on the concentration of the extract, while on M. americana extract presented only bacteriostatic activity against P. gingivalis. These findings provide important and promising information allowing for further exploration in the future.

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)

Actividad Antibacteriana in vitro de extractos y fracciones de Physalis peruviana L. y Caesalpinia pulcherrima (L.) Swartz / In vitro antibacterial activity of extracts and fractions of Physalis peruviana L. and Caesalpinia pulcherrima (L.) Swartz

We evaluated the in vitro antibacterial activity of extracts and fractions of Physalis peruviana L. calyces and flowers and leaves of Caesalpinia pulcherrima (L.) Swartz against ATCC strains Staphylococcus aureus, Klebsiella pneumoniae and Pseudomonas aeruginosa, determining the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). We find potent activity with MIC < 0,256 mg/mL for the chloroform fraction of P. peruviana calyces, the ethanol fraction of flowers of C. pulcherrima and ethanol and ether fractions of leaves of C. pulcherrima. Based on these results, we conclude that both species are promising and it is recommended to continue exploring them in order to isolate, purify and to elucidate the chemical structure from those compounds responsible for the biological activity of each active fraction.

Se evaluó la actividad antibacteriana in vitro de extractos y fracciones de los cálices de Physalis peruviana L. y flores y hojas de Caesalpinia pulcherrima (L.) Swartz frente a cepas ATCC de Staphylococcus aureus, Klebsiella pneumoniae y Pseudomonas aeruginosa, determinando la concentración mínima inhibitoria (CMI) y la concentración mínima bactericida (CMB). Encontramos potente actividad, con valores de CMI < 0,256 mg/mL para la fracción en cloroformo de los cálices de P. peruviana, la fracción en etanol de las flores de C. pulcherrima y las fracciones en etanol y éter de las hojas de C. pulcherrima. En función de los resultados obtenidos, concluimos que ambas especies son promisorias y se recomienda continuar su estudio intentando aislar, purificar y dilucidar la estructura química de los compuestos responsables de la actividad biológica en cada fracción activa.

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.

Estudio biofarmacéutico comparativo de marcas comerciales de tabletas de ciprofloxacino disponibles en el mercado colombiano / A comparative biopharmaceutical study of brands of ciprofloxacin tablets available on the Colombian market

Objetivo: Determinar la equivalencia biofarmacéutica de marcas comerciales de Ciprofloxacino 500 mg disponibles en el mercado colombiano. Métodos: Se tomaron 12 productos comerciales de Ciprofloxacino tabletas 500 mg, adquiridos en droguerías y farmacias de cuatro de las principales ciudades del país, a los cuales se les realizaron los siguientes ensayos: Identificación del principio activo por HPLC, contenido de ingrediente activo, uniformidad de dosificación, pruebas de desintegración y disolución; además se compararon los perfiles de disolución de los productos frente a uno tomado como referencia. Los resultados se analizaron a fin de establecer diferencias estadísticamente significativas y posible intercambiabilidad entre los productos evaluados. Resultados: El análisis comparativo de los productos, permitió evidenciar marcadas diferencias en cuanto a la liberaciónin vitrodel principio activo, con uno de los productos incumpliendo este importante parámetro de calidad. Todos los productos evaluados cumplen con las especificaciones oficiales de identificación y valoración del principio activo, uniformidad de dosificación y tiempo de desintegración. En cuanto a la cinética de disolución se encontraron diferencias entre las formulaciones, con productos de deficiente Eficiencia de Disolución (ED) y que a pesar de cumplir con la especificación a Q30, se disuelven muy lentamente. Conclusiones: Once productos cumplen con todas las especificaciones establecidas en la USP-33/NF28. Los resultados de este trabajo constituyen un valioso aporte para en un futuro cercano y en función de las políticas nacionales, poder establecer bioequivalencia entre estos productos.

Objective: Determining the biopharmaceutical equivalency of 500 mg ciprofloxacin tablets available on the Colombian market (i.e. comparing different trademarks). Methods: Twelve commercial 500 mg ciprofloxacin tablets were obtained from drugstores and pharmacies in Colombia’s four major cities. They were submitted to the following assays: HPLC identification of active ingredients, active ingredient content, dose uniformity, disintegration and dissolution tests and comparing the products’ dissolution profiles to that of the innovator. The results were analyzed to establish statistically significant differences and possible inter-changeability between the products being tested. Results: Comparative analysis of the products revealed marked differences regardingin vitrorelease of the active principle (one product failing this important quality parameter). All the products tested here complied with the official specifications for identifying and assaying the active principle, dosage unit uniformity and the disintegration test. Regarding dissolution kinetics, differences were found between formulations as some products had poor dissolution efficiency (DE) and dissolved very slowly despite complying with the Q30specification. Conclusions: 11 products complied with USP33-NF28specifications (guidelines on specifications for impurities in antibiotics). This work has made a valuable contribution towards establishing these products’ bioequivalence in the near future regarding national policy.

[A comparative biopharmaceutical study of brands of ciprofloxacin tablets available on the Colombian market]. / Estudio biofarmacéutico comparativo de marcas comerciales de tabletas de ciprofloxacino disponibles en el mercado colombiano.

OBJECTIVE: Determining the biopharmaceutical equivalency of 500 mg ciprofloxacin tablets available on the Colombian market (i.e. comparing different trademarks). METHODS: Twelve commercial 500 mg ciprofloxacin tablets were obtained from drugstores and pharmacies in Colombia's four major cities. They were submitted to the following assays: HPLC identification of active ingredients, active ingredient content, dose uniformity, disintegration and dissolution tests and comparing the products' dissolution profiles to that of the innovator. The results were analyzed to establish statistically significant differences and possible inter-changeability between the products being tested. RESULTS: Comparative analysis of the products revealed marked differences regardingin vitrorelease of the active principle (one product failing this important quality parameter). All the products tested here complied with the official specifications for identifying and assaying the active principle, dosage unit uniformity and the disintegration test. Regarding dissolution kinetics, differences were found between formulations as some products had poor dissolution efficiency (DE) and dissolved very slowly despite complying with the Q30specification. CONCLUSIONS: 11 products complied with USP33-NF28specifications (guidelines on specifications for impurities in antibiotics). This work has made a valuable contribution towards establishing these products' bioequivalence in the near future regarding national policy.

Folk medicine in the northern coast of Colombia: an overview.

BACKGROUND: Traditional remedies are an integral part of Colombian culture. Here we present the results of a three-year study of ethnopharmacology and folk-medicine use among the population of the Atlantic Coast of Colombia, specifically in department of Bolívar. We collected information related to different herbal medicinal uses of the local flora in the treatment of the most common human diseases and health disorders in the area, and determined the relative importance of the species surveyed. METHODS: Data on the use of medicinal plants were collected using structured interviews and through observations and conversations with local communities. A total of 1225 participants were interviewed. RESULTS: Approximately 30 uses were reported for plants in traditional medicine. The plant species with the highest fidelity level (Fl) were Crescentia cujete L. (flu), Eucalyptus globulus Labill. (flu and cough), Euphorbia tithymaloides L. (inflammation), Gliricidia_sepium_(Jacq.) Kunth (pruritic ailments), Heliotropium indicum L. (intestinal parasites) Malachra alceifolia Jacq. (inflammation), Matricaria chamomilla L. (colic) Mentha sativa L. (nervousness), Momordica charantia L. (intestinal parasites), Origanum vulgare L. (earache), Plantago major L. (inflammation) and Terminalia catappa L. (inflammation). The most frequent ailments reported were skin affections, inflammation of the respiratory tract, and gastro-intestinal disorders. The majority of the remedies were prepared from freshly collected plant material from the wild and from a single species only. The preparation of remedies included boiling infusions, extraction of fresh or dry whole plants, leaves, flowers, roots, fruits, and seeds. The parts of the plants most frequently used were the leaves. In this study were identified 39 plant species, which belong to 26 families. There was a high degree of consensus from informants on the medical indications of the different species. CONCLUSIONS: This study presents new research efforts and perspectives on the search for new drugs based on local uses of medicinal plants. It also sheds light on the dependence of rural communities in Colombia on medicinal plants.