Determining the affinity of anti-mitotic compounds binding to colchicine binding site of tubulin by affinity probe capillary electrophoresis.

The colchicine binding site of tubulin is often used to screen the anti-mitotic compounds, which are widely used as anti-cancer therapies. In the present work, an affinity probe capillary electrophoresis (APCE) method was developed for determining the affinity of anti-mitotic compounds. To this end, a fluorescently labeled affinity probe, 5-carboxyfluorescein-colchicine (F-colchicine), was prepared for the affinity competition experiment. The probe can form a stable complex with tubulin with the binding stoichiometry of 0.75, and the dissociation constant Kd of the complex was determined as 5.7 × 10-5 mol/L. In the affinity competition experiment, F-colchicine was incubated with tubulin and the test compound in the solution. The F-colchicine-tubulin complexes and free F-colchicine were quickly separated by CE and the concentration of free F-colchicine was accurately determined with the laser induced fluorescence detection. The affinity constant of the tested compound can be measured with the affinity competition binding curve. The enantiomers of the anti-mitotic compound were evaluated by using the method. The binding affinity of the enantiomers displayed an enantioselective manner. Compared to other affinity binding assay methods, our method is more straightforward, more accurate, and more cost-effective.

Prácticas agrícolas para el cultivo de Cajanus indicus Spreng (gandul) con fines terapéuticos / Agricultural practice for cultivation of Cajanus indicus Spreng (gandul) for therapeutic purposes

Introducción: Cajanus indicus Spreng (gandul), presenta gran interés terapéutico, sobre todo en la búsqueda de compuestos de origen vegetal que mediante mecanismo antimitótico inhiban el desarrollo de procesos cancerosos. Objetivos: determinar los aspectos agrícolas que proporcionen mayor producción de la parte aérea para su explotación con estos fines. Métodos: durante 2007-2009 se hicieron diferentes investigaciones en la Estación Experimental de Plantas Medicinales Dr. Juan Tomás Roig; en julio de 2007 se realizó un estudio para analizar el comportamiento de la planta y determinar la altura de corte que proporcionara su mejor rebrotación, posteriormente se estudió por 2 años consecutivos, febrero de 2008 hasta febrero de 2009, 2 distancias de siembra: 90 x 30 cm y 90 x 60 cm; y 2 momentos de inicio de cosecha: 3 y 4 meses de edad...

Introduction: Cajanus indicus Spreng. (gandul) is of great therapeutic interest mainly in the search of vegetal compounds capable of inhibiting cancerous processes through the antimycotic mechanism. Objectives: to determine the agricultural aspects that favour higher production of the aerial part of this plant to this end. Methods: in the 2007-2009 period, several research studies were performed in Dr Juan Tomás Roig experimental center of medicinal plants. In July, 2007 a study was conducted to analyze the behaviour of the plant and to determine the cutting height that will encourage the best sprout. From February 2008 to February 2009, 2 sowing distances (90 x 30 cm and 90 x 60 cm) and 2 times of harvest starting (3 and 4 months of age) were studied...

Prácticas agrícolas para el cultivo de Cajanus indicus Spreng (gandul) con fines terapéuticos / Agricultural practice for cultivation of Cajanus indicus Spreng (gandul) for therapeutic purposes

Introducción: Cajanus indicus Spreng (gandul), presenta gran interés terapéutico, sobre todo en la búsqueda de compuestos de origen vegetal que mediante mecanismo antimitótico inhiban el desarrollo de procesos cancerosos. Objetivos: determinar los aspectos agrícolas que proporcionen mayor producción de la parte aérea para su explotación con estos fines. Métodos: durante 2007-2009 se hicieron diferentes investigaciones en la Estación Experimental de Plantas Medicinales Dr. Juan Tomás Roig; en julio de 2007 se realizó un estudio para analizar el comportamiento de la planta y determinar la altura de corte que proporcionara su mejor rebrotación, posteriormente se estudió por 2 años consecutivos, febrero de 2008 hasta febrero de 2009, 2 distancias de siembra: 90 x 30 cm y 90 x 60 cm; y 2 momentos de inicio de cosecha: 3 y 4 meses de edad...(AU)

Introduction: Cajanus indicus Spreng. (gandul) is of great therapeutic interest mainly in the search of vegetal compounds capable of inhibiting cancerous processes through the antimycotic mechanism. Objectives: to determine the agricultural aspects that favour higher production of the aerial part of this plant to this end. Methods: in the 2007-2009 period, several research studies were performed in Dr Juan Tomás Roig experimental center of medicinal plants. In July, 2007 a study was conducted to analyze the behaviour of the plant and to determine the cutting height that will encourage the best sprout. From February 2008 to February 2009, 2 sowing distances (90 x 30 cm and 90 x 60 cm) and 2 times of harvest starting (3 and 4 months of age) were studied...(AU)

Avaliação da atividade antimicrobiana de Maytenus rigida Mart. (Celastraceae) / Evaluation of the antimicrobial activity of Maytenus rigida Mart. (Celastraceae)

A realização de estudos farmacológicos é fundamental para comprovar a eficácia do uso de plantas medicinais pela população para o tratamento de doenças e descobrir novos fitoterápicos. Esse estudo teve como objetivo avaliar o potencial antimicrobiano do extrato etanólico e fase acetato de etila do bom nome (Maytenus rigida Mart.) sobre Staphylococcus aureus ATCC 25923, 3 amostras de Staphylococcus aureus multirresistentes isoladas de pacientes com infecções nosocomiais, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 e Salmonella sp. (228-R-Tet, 118-R-Sut e 01-S) isoladas de ambiente aquático, utilizando o método de difusão em agar. Os testes revelaram que o extrato e fase de M. rigida apresentaram atividade antimicrobiana in vitro frente a todas as cepas de S. aureus testadas, apresentando concentração inibitória mínima (MIC) de 400 mg mL-1. Entretanto, estes produtos não apresentaram atividade frente às linhagens de bactérias Gram-negativas testadas, Escherichia coli, Pseudomonas aeruginosa e Salmonella sp.

Ppharmacological studies are essential to prove the effectiveness of using medicinal plants to treat diseases and discover new phytotherapics. This study aimed to evaluate the antimicrobial potential of ethanol and ethyl acetate extracts of "bom-nome" (Maytenus rigida Mart.) against Staphylococcus aureus ATCC 25923, three samples of multiresistant Staphylococcus aureus isolated from patients with nosocomial infections, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 and Salmonella sp. (228-R-Tet, 118-R-Sut and 01-S) isolated from water environment, using the agar diffusion test. Both extracts showed in vitro antimicrobial activity against all S. aureus strains, presenting 400 mg mL-1 minimum inhibitory concentration (MIC). However, these products did not show activity against strains of the Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa and Salmonella sp.

Potencial antioxidante e antimicrobiano de espécies da família Asteraceae / Antioxidant and antimicrobial potential of Asteraceae species

Espécies da família Asteraceae são amplamente utilizadas na medicina popular para diversos fins terapêuticos. Neste contexto, este estudo teve por objetivo averiguar a atividade antimicrobiana e antioxidante in vitro de extratos metanólicos de plantas pertencentes a Asteraceae, a maioria comumente utilizada na medicina tradicional. A prospecção química dos extratos também foi realizada. A atividade antimicrobiana foi avaliada pelo método de susceptibilidade em microdiluição em caldo e a atividade antioxidante determinada pelo ensaio com o radical DPPH. O extrato da folha de Baccharis dracunculifolia apresentou significativa atividade antimicrobiana para Pseudomonas aeruginosa,Bacillus cereus e Cryptococcus neoformans (CIM = 0,005; 0,005 e 0,039 mg mL-1, respectivamente). Os extratos das folhas de Bidens segetum e Matricaria chamomilla foram seletivos para Shigella sonnei e P. aeruginosa (CIM = 0,005 e 0,078 mg mL-1, respectivamente). Já as folhas de Acanthospermun australe e Baccharis trimera apresentaram atividade significativa apenas para Candida albicans (CIM = 0,039 mg mL-1) enquanto as folhas de Taraxacum officinale foram ativos contra ambas leveduras com CIM 0,039 mg mL-1. Em relação à atividade antioxidante, os extratos das folhas de B. dracunculifolia, T. officinale e das inflorescências de B. segetum apresentaram significativa atividade com CI50 de 5, 5 e 4 µg mL-1, respectivamente. A prospecção química dos extratos identificou presença de compostos como flavonoides, terpenos e outros que podem ser responsáveis pelas atividades observadas.

Asteraceae species have been largely used in folk medicine for several therapeutic purposes. Thus, the aim of this work was to investigate the in vitro antimicrobial and antioxidant activities of methanol extracts from plants belonging to the Asteraceae family, most of which are commonly used in traditional medicine. Chemical prospecting of extracts was also performed. The antimicrobial activity was evaluated through the broth microdilution susceptibility method and the antioxidant activity was determined through DPPH assay. Leaf extract of Baccharis dracunculifolia presented a significant antimicrobial activity against Pseudomonas aeruginosa,Bacillus cereus and Cryptococcus neoformans (0.005, 0.005 and 0.039 mg mL-1 MIC, respectively). Leaf extracts of Bidens segetum and Matricaria chamomilla were selective for Shigella sonnei and P. aeruginosa (0.005 and 0.078 mg mL-1 MIC, respectively). On the other hand, Acanthospermun australe and Baccharis trimera leaves only showed significant activity against Candida albicans (0.039 mg mL-1 MIC), while Taraxacum officinale leaves were active against both yeasts, with 0.039 mg mL-1 MIC. As regards antioxidant activity, extracts of B. dracunculifolia and T. officinale leaves and B. segetum inflorescences presented significant activity, with 5, 5 and 4 µg mL-1 IC50, respectively. The chemical prospecting identified the presence of flavonoids, terpenes and other compounds which may be responsible for the observed activities.

Occurrence and loss over three years of 72 pharmaceuticals and personal care products from biosolids-soil mixtures in outdoor mesocosms.

Municipal biosolids are in widespread use as additives to agricultural soils in the United States. Although it is well known that digested sewage sludge is laden with organic wastewater contaminants, the fate and behavior of micropollutants in biosolids-amended agricultural soils remain unclear. An outdoor mesocosm study was conducted in Baltimore, Maryland, to explore the fate of 72 pharmaceuticals and personal care products (PPCPs) over the course of three years in that were placed in plastic containers made from polyvinylchloride and kept exposed to ambient outdoor conditions. Of the 72 PPCPs tested for using EPA Method 1694, 15 were initially detected in the soil/biosolids mixtures at concentrations ranging from low parts-per-billion to parts-per-million levels. The antimicrobials triclocarban and triclosan showed the highest initial concentrations at 2715 and 1265 µg kg(-1), respectively. Compounds showing no discernable loss over three years of monitoring included diphenhydramine, fluoxetine, thiabendazole and triclocarban. The following half-life estimates were obtained for compounds showing first-order loss rates: azithromycin (408-990 d) carbamazepine (462-533 d), ciprofloxacin (1155-3466 d), doxycycline (533-578 d), 4-epitetracycline (630 d), gemfibrozil (224-231 d), norfloxacin (990-1386 d), tetracycline (578 d), and triclosan (182-193 d). Consistent with other outdoor degradation studies, chemical half-lives determined empirically exceeded those reported from laboratory studies or predicted from fate models. Study results suggest that PPCPs shown in the laboratory to be readily biotransformable can persist in soils for extended periods of time when applied in biosolids. This study provides the first experimental data on the persistence in biosolids-amended soils for ciprofloxacin, diphenhydramine, doxycycline, 4-epitetracycline, gemfibrozil, miconazole, norfloxacin, ofloxacin, and thiabendazole.