Anti-Staphylococcus aureus Methicillin-Resistant (MRSA) activity of a novel 3-Chalcogenyl Indole / Atividade Anti-Staphylococcus aureus Meticilina Resistente (MRSA) de um novo composto 3-Calcogenil Indol

Objective: the development of new drugs against Methicillin-resistant Staphylococcus aureus is a priority to the World Health Organization. So, the objective of this study was to evaluate the antibacterial activity and toxicity of 5-bromo-3-((4-methoxyphenyl) sulfenyl)-1H-indole (3b) against MRSA. Methods: minimum inhibitory concentration (MIC) of 3b was determined against S. aureus ATCC 29213 and 43 clinical isolates. The time-kill assay was performed for 9 isolates. Analysis of variance followed by the post hoc Bonferroni test was used for the statistical tests. Results and conclusions: the MIC50 and MIC90 of 3b were 4 µg.mL-1 and 16 µg.mL-1 respectively. In time-kill assay, the 3b showed bactericidal activity to all evaluated isolates at concentrations of 1xMIC and 2xMIC and the re-growth effect was not observed. About the toxicity tests, 3b has not presented cytotoxicity, mutagenicity, or allergenicity. 3b had particularly good activity against MRSA demonstrating high potential for the development of new antimicrobials products.

Objetivo: o desenvolvimento de novos antimicrobianos contra Staphylococcus aureus resistentes à meticilina (MRSA) é uma prioridade para a Organização Mundial da Saúde. Então, o objetivo desse estudo foi avaliar a atividade antibacteriana e a toxicidade do 5-bromo-3-((4-metoxifenil) sulfenil)-1H-indol (3b) contra MRSA. Métodos: a concentração inibitória minima de 3b foi determinada contra S. aureus ATCC 29213 e 43 isolados clínicos. O ensaio de curva de morte foi realizado para nove isolados. Análise de variância seguida pelo teste post hoc Bonferroni foi usada para testes estatísticos. Resultados e conclusões: a MIC50 e MIC90 do 3b foi 4 µg.mL-1 e 16 µg.mL-1, respectivamente. No ensaio de curva de morte, o 3b demonstrou atividade bactericida contra todos os isolados avaliados na concentração de 1xMIC e 2xMIC e o recrescimento não foi observado. Em relação aos testes de toxicidade, 3b não apresentou citotoxicidade, mutagenicidade ou alergenicidade. 3b apresentou atividade particularmente interessante contra MRSA, demonstrando alto potencial para o desenvolvimento de novos produtos antimicrobianos.

Phytochemicals effective in lowering Low-Density Lipoproteins

Cardiovascular diseases are the leading cause of morbidity and mortalityaround the globe. The key risk factor of cardiovascular diseases, hypercholesterolemiais expected to increase in the future. Phytochemicals, are natural compounds found inplants, having antioxidant properties. These antioxidant properties can be utilized toreduce the occurrence of chronic diseases and provide many health benefits in humans.Phytochemicals such as Indoles, plant sterols, flavonoids and lignans have beenextracted and studied widely. It is because of their antioxidant properties they can beused in preventing hypercholesterolemia. This review illustrates and summarizesvarious phytochemicals and their mechanisms in lowering LDL cholesterol levels. Theprogress and the results achieved in studies relevant to the hypocholesterolemiceffects of these phytochemicals are also illustrated. It was interpreted that on theavailability of sufficient and confirmatory data about the efficacy of phytochemicals inlowering LDL cholesterol levels, plant-based diets or drugs containing extracts ofphytochemicals can then be deployed in the treatment of hypercholesterolemia

Antiedematogenic activity of the indole derivative N-salicyloyltryptamine in animal models

ABSTRACT The N-salicyloyltryptamine (NST) is an indole derivative compound analogue to the alkaloid N-benzoyltryptamine. In the present study, the antiedematogenic activity of NST was investigated in animal models. Firstly, the acute toxicity for NST was assessed according to the OECD Guideline no. 423. The potential NST-induced antiedematogenic activity was evaluated by carrageenan-induced paw edema in rats, as well as by dextran-, compound 48/80-, histamine-, serotonin-, capsaicine-, and prostaglandin E2-induced paw edema in mice. The effect of NST on compound 48/80-induced ex vivo mast cell degranulation on mice mesenteric bed was investigated. No death or alteration of behavioral parameters was observed after administration of NST (2000 mg/kg, i.p.) during the observation time of 14 days. The NST (100 and 200 mg/kg, i.p.) inhibited the carrageenan-induced edema from the 1st to the 5th hour (**p<0.01; ***p<0.001). The edematogenic activity induced by dextran, compound 48/80, histamine, serotonin, capsaicin, and prostaglandin E2 was inhibited by NST (100 mg/kg, i.p.) throughout the observation period (**p<0.01; ***p<0.001). The pretreatment with NST (50, 100 or 200 mg/kg, i.p) attenuates the compound 48/80-induced mast cell degranulation (**p<0.01; ***p<0.001). Thus, the inhibition of both mast cell degranulation and release of endogenous mediators are probably involved in the NST-induced antiedematogenic effect.

Caracterización y efecto de Azotobacter, Azospirillum y Pseudomonas asociadas a Ipomoea Batatas del Caribe Colombiano / Characterization and effect of Azotobacter, Azospirillum and Pseudomonas associated with Ipomoea Batatas of Colombian Caribbean

Resumen El uso de Rizobacterias promotoras de crecimiento vegetal (PGPR, por sus siglas en ingles) constituye una alternativa al uso de fertilizantes químicos favoreciendo el rendimiento de los cultivos. La presente investigación tuvo como objetivo la búsqueda, selección y caracterización de PGPB de los géneros Azotobacter, Azospirillum y Pseudomonas nativas de la rizósfera de cultivos de Ipomoea batatas de zonas productoras representativas del Caribe Colombiano. Los aislados seleccionados se caracterizaron molecularmente y realizaron pruebas de solubilización de fósforo, producción de índoles y reducción de acetileno. Las cepas fueron probadas a nivel de invernadero en plántulas de Ipomoea batatas producidas in vitro en las que se evaluó la altura, longitud radicular, masa seca de la parte aérea y radicular. Asociada a la rizósfera de Ipomoea batatas se obtuvieron cepas de Azotobacter vinelandii, Azotobacter chroococcum, Azospirillum lipoferum, Azospirillum brasilense y Pseudomonas denitrificans, las cepas fueron capaces de solubilizar fósforo, producir índoles y reducir acetileno. Se obtuvo incrementos en parámetros de crecimiento como longitud radicular, altura, peso seco aéreo y radicular en plántulas de Ipomoea batatas en invernadero con la inoculación de las bacterias seleccionadas frente a plántulas sin inocular. Los resultados catalogan a los aislados obtenidos como posibles microorganismos con potencial como biofertilizantes en batata.

Abstract The use of plant growth promoting Rhizobacteria (PGPR) is an alternative to replace chemical fertilizers for the cultivation of agricultural crops. The aim of this research was to search, selection and characterization of PGPR from the genus Azotobacter, Azospirillum and Pseudomonas natives from sweet potato (Ipomoea batatas) plants and rhizosphere of representative production regions of the Colombian Caribbean. Selected isolates were identified by molecular methods and they were screenedin vitrofor activities related to plant growth such as phosphate solubilization, indole production and acetylene reduction. The strains were tested in the greenhouse on plants of Ipomoea batatas produced in vitro. The height, root length, dry mass of the shot and root were evaluated. Associated with sweet potato crop us finded strains identificated as Azotobacter vinelandii, Azotobacter chroococcum, Azospirillum lipoferum, Azospirillum brasilense and Pseudomonas denitrificans. The strains were able to solubilize phosphate, synthesize indole-3-acetic acid (IAA) and reduce acetylene. The inoculation of bacteria selected increased growth parameters such as root length, height, dry weight root and shoot in plants of sweet potato in greenhouse. Those results catalog to the isolated obtained as possible microorganisms with potential as biofertilizers in sweet potato.

Bacillus EFFECT ON THE GERMINATION AND GROWTH OF TOMATO SEEDLINGS (Solanum lycopersicum L) / Efecto de Bacillus sobre la germinación y crecimiento de plántulas de tomate (Solanum lycopersicum L)

ABSTRACT The capacity to solubilize phosphate and to produce indole compounds Indole Acetic Acid type, was evaluated in 15 strains isolated from castor bean lignocellulosic residues (Ricinus communis). To determine the solubilizing activity of phosphates a qualitative test by using Pikovskaya culture medium was employed and for the evaluation of the production of indole compounds (IAA) a Salkowsky colorimetric analysis technique was applied. Among the microorganisms tested, the Bacillus pumilus GIBI 206 demonstrated capacity to solubilize phosphates and Bacillus subtilis GIBI 200 showed of capacity to solubilize phosphates and to produce Indoleacetic Acid (IAA). To determine the effect of the Bacillus subtilis strain on germination and growth promotion, tomato seeds (Solanum lycopersicum 'Santa Clara') were inoculated; the inoculation of the seeds along with the microorganism revealed statistically significant differences, during the germination stage compared to the control treatment. Nevertheless, it revealed a positive influence on the development of tomato plants, originating a significant increase on the mass and length of its stem and root. The results of this research offer the possibility of using the Bacillus subtilis as a growth promoter in tomato seedlings and in the formulation of bio-products.

RESUMEN La capacidad para solubilizar fosfatos y producir compuestos indólicos del tipo Ácido Indol Acético, se evaluó en 15 cepas aisladas de residuos lignocelulósicos de higuerilla (Ricinus communis). Para determinar la actividad solubilizadora de fosfatos se realizó una prueba cualitativa utilizando medio de cultivo Pikovskaya y para evaluar la producción de compuestos indólicos (AIA) se empleó la técnica colorimétrica de Salkowsky. Entre los microorganismos evaluados, Bacillus pumilus GIBI 206 mostró tener la capacidad para solubilizar fosfatos y Bacillus subtilis GIBI 200 evidenció capacidad para solubilizar fosfatos y producir Ácido Indolacético (AIA). Para determinar el efecto de la cepa Bacillus subtilis sobre la germinación y promoción de crecimiento, se inoculó en semillas de tomate (Solanum lycopersicum cultivar Santa Clara); la inoculación de las semillas con el microorganismo no mostró diferencias estadísticamente significativas en el tiempo de germinación en comparación con el tratamiento control, sin embargo mostró influir positivamente en el desarrollo de las plantas de tomate generando un aumento significativo sobre la masa y longitud del tallo y de la raíz. Los resultados de esta investigación ofrecen la posibilidad de utilizar a Bacillus subtilis como promotora de crecimiento en plántulas de tomate y en la formulación de bioinsumos.

Comparison of the effects of methylprednisolone and dexamethasone individually combined with tropisetron on the prevention of postoperative nausea and vomiting of high risk in patients with thyroid surgery / 中国医师杂志

Objective To compare the effects of methylprednisolone and dexamethasone individually combined with tropisetron on the prevention of postoperative nausea and vomiting (PONV) of high risk in patients with thyroid surgery.Methods One hundred and sixty patients of high risk of postoperative nausea and vomiting scheduled for radical operation of thyroid with general anesthesia were randomly divided into four groups with 40 cases each.Four groups of the patients were intravenously injected methylprednisolone 40 mg plus tropisetron 5 mg at the end of the operations (group MT),dexamethasone 7.5 mg before anesthesia induction,and tropisetron 5 mg at the end of the operations (group DT),tropisetron 5 mg at the end of the operations (group T),and normal saline (group C).Incidence and severity of nausea,vomiting and adverse reactions were recorded during 24 hours after end of the operations.Results Compared to group DT,the incidences of PONV during the 0 ～ 2 h and 2 ～ 6 h,and the visual analogue scale (VAS) of PONV at 2 h after the operations in group MT were significantly lower (P ＜ 0.05).Compared to group C,the incidences of PONV and VAS score during the 0 ～ 24 h after the operations in group MT and group DT were significantly lower (P ＜0.05),the incidences of PONV during the 2 ～6 h and 6 ～ 12 h after the operations,and VAS score of PONV at 6 h and 12 h after the operations in group T were significantly lower (P ＜0.05).Compared to group C,incidences of headache in group MT and group DT were significantly lower (P ＜ 0.05),and incidence of swim in group T was also significantly lower (P ＜ 0.05).Incidence of adverse reactions in group MT and group DT were no significant difference.Conclusions Preventive effect of methylprednisolone combined with tropisetron for PONV in high-risk patients within 6 hours after thyroid surgery was significantly better than that of dexamethasone combined with tropisetron.

Efficacy of acupuncture combined with tropisetron in treating nausea and vomiting induced by car-boprost tromethamine in cesarean section / 中华麻醉学杂志

Objective To evaluate the efficacy of acupuncture combined with tropisetron in treating nausea and vomiting induced by carboprost tromethamine in cesarean section. Methods Sixty-six patients aged 22-40 yr who received carboprost tromethamine and developed nausea and vomiting during cesarean section under lumbar anesthesia, were randomly divided into 3 groups(n=22 each): acupuncture group (group A), tropisetron group(group T)and acupuncture+ tropisetron group(group AT). In group A, 09% normal saline 2 ml was intravenously injected immediately, acupuncture was given at Renzhong, Neiguan and Hegu acupoints with lifting thrusting twirling the acupuncture needle for 10 min. In group T, tropisetron 10 mg was intravenously injected immediately, the needle was placed on Renzhong, Neiguan and Hegu skin surface. In group AT, tropisetron 10 mg was intravenously injected immediately, acupunc-ture was given at Renzhong, Neiguan and Hegu acupoints with lifting thrusting twirling the acupuncture nee-dle for 10 min. The nausea and vomiting score was assessed before anesthesia induction(T0), when nause-a or vomiting occurred(T1)and at 1, 3, 5 and 15 min after acupuncture or administration(T1-5). The degree of patient′s satisfaction with therapeutic effect was recorded. Results Compared with group A, the nausea and vomiting scores were significantly decreased at T4, and the patient's satisfaction score was in-creased in group AT(P<005). Compared with group T, the nausea and vomiting scores were significantly decreased at T2-4and the patient's satisfaction score was increased in group AT(P <005). Conclusion Acupuncture combined with ondansetron can quickly and effectively relieve the nausea and vomiting induced by carboprost tromethamine during cesarean section.

Effect of bazedoxifene on endometriosis in a rat model / 中华妇产科杂志

Objective To investigate the therapeutic mechanism of bazedoxifene, the third-generation selective ER modulator (SERM), on endometriosis lesions in a rat model. Methods Endometriosis was induced by transplanting pieces of endometrium from other syngeneic rats that were as donors onto the subcutaneous of other unmated female rats. The rats with successful ectopic implants were divided into two groups:control group (n=10) and bazedoxifene group (n=10). The macroscopic morphology, volume, histopathology of ectopic implant and rats uterine wet weight were determined before and after the treatment. Expression of proliferation cell nuclear antigen (PCNA), ER and PR in the eutopic endometrium and endometriosis lesions detected by immunohistochemistry in the two groups. Results (1) The gross morphology and histological changes of endometriosis lesions in rats after treatment: compared with the control group, it was obviously depauperated and had more less glands and blood vessels in the stroma. (2) The change of rats′weight, the volume of endometriosis lesion before and after treatment and rats uterine wet weigh after treatment respectively in the control group and the bazedoxifene group:rats′ weight were respectively before treatment: (201±17) g, (202±18) g, that were respectively after treatment: (266±16) g, (261±16) g, which showed no significant difference between two groups before and after treatment (P>0.05). The volume of ectopic implant before treatment were respectively (85±17) mm3, (85±12) mm3, and showed no significant difference between two groups;that were respectively (48±11) mm3, (24±9) mm3 afte rtreatment, which was significantly decreased compared with the control group (P0.05). Conclusion Bazedoxifene could obviously reduce the size of endometriosis lesions, the mechanism may be related with suppressing estrogen-induced proliferation, the expression of ER and direct ER antagonism by this SERM.

Efecto de rizobacterias promotoras de crecimiento vegetal solubilizadoras de fosfato en Lactuca sativa cultivar White Boston / Effect of plant growth promoting rhizobacteria phosate solubilizing Lactuca sativa cultivar White Boston

En las últimas décadas, la agricultura colombiana se ha visto afectada por la reducción de la productividad en las zonas hortícolas, el incremento de los costos de producción y la dependencia del uso de productos químicos, produciendo un daño irreversible al medio ambiente y la calidad de vida de productores y consumidores. El objetivo de investigación fue evaluar el efecto de rizobacterias promotoras del crecimiento vegetal del género Pseudomonas sp. sobre Lactuca sativa cultivar White Boston como solubilizadoras de roca fosfórica. El estudio se realizó en el Centro de Investigación Tibaitatá (Corpoica) ubicado en Mosquera (Cundinamarca-Colombia). Los resultados demostraron que las cepas tienen la capacidad intrínseca para solubilizar fuentes de fósforo de baja solubilidad como la roca fosfórica. La aplicación de inoculantes con base en las cepas: Pseudomonas fluorescens FR1, Pseudomonas sp., UVLO27 y Pseudomonas sp. LEAV18 arrojaron los mejores resultados. Las cepas Pseudomonas sp. FR2, UVLO27 y K35, tienen la capacidad de producir índoles y sideróforos. El experimento en invernadero evidenció que las cepas Pseudomonas fluorescens FR1, Pseudomonas sp. FR2 y UVLO27 incrementaron de manera significativa (P<0.05) la biomasa y el desarrollo de las plantas. El uso de rocas fosfóricas representa una alternativa económica y ecológica viable, en sistemas de agricultura sostenible.

In the last decades, Colombian agriculture has been affected by the reduction in productivity in horticultural areas, increase in production costs and the dependence of chemical products usage, causing and irreversible damage to environment and producers and consumers life quality. The aim of this research was to evaluate the effect of plant growth promoting rhizobacteria of the genus Pseudomonas sp. under Lactuca sativa cultivar White Boston as phosphate rock solubilizing bacteria. The study took place in the Research Centre Tibaitatá-Corpoica, located in Mosquera (Cundinamarca-Colombia). Results demonstrated that the strains have an intrinsic capacity to solubilize low solubility phosphorus sources as phosphate rock. Inoculants application based on: Pseudomonas fluorescensFR1, Pseudomonas sp., UVLO27 and Pseudomonas sp. LEAV18 strains displayed the best results. The strains Pseudomonas sp. FR2, UVLO27 and K35, are capable of producing indoles and siderophores. The green house experiment showd that strain Pseudomonas fluorescens FR1, Pseudomonas sp. FR2 of phosphate rocks represents a viable economic and ecological alternative in sustainable agriculture systems.

In Silico Analysis of Indoles Against 1KE8 Inhibitors Using Autodock.

1KE8 is known as a potential target for anti-cancer medication. Indoles are biologically active nitrogen heterocyclics known for broad spectrum activities. Modification of Indole ring system with selected structural descriptors has offered a high degree of stereo specificity and diversity in activity to the moiety.

Evaluación de microorganismos con potencial de promoción de crecimiento vegetal y biocontrol de Spongospora subterranea / Evaluation of microorganisms with potential for plant growth promotion and biological control of Spongospora subterranea

La sarna polvosa de la papa es causada por el patógeno Spongospora subterranea, que disminuye la calidad y producción de tubérculos y facilita la entrada de otros patógenos. Esta enfermedad afecta las principales zonas productoras del mundo, debido a la falta de tratamientos efectivos contra el patógeno y al comercio de tubérculos-semilla infectados. Algunas investigaciones indican que los agentes biocontroladores podrían contribuir a reducir la actividad de S. subterranea a través de efectos sobre la viabilidad de sus quistosoros o mediante efectos estimulantes del crecimiento de la planta. En este estudio se emplearon bacterias aisladas del interior de raí­z, rizósfera y superficie de tubérculos de un cultivo de papa ( Solanum tuberosum variedad Diacol Capiro) y seleccionadas por su capacidad para producir indoles totales y quitinasas. En estudios paralelos se determinó su capacidad para promover la velocidad de germinación en brotes de tubérculos o para controlar S. subterranea en raíces y promover el crecimiento vegetal de plántulas en invernadero. La mayoria de los aislamientos evaluados incrementraron la longitud de brotes de tubérculos en el laboratorio. En el invernadero, en suelo no estéril y en presencia del patógeno, se encontró que 2 de los 10 aislamientos seleccionados por su capacidad para producir indoles totales y quitinasas, presentaron promoción de crecimiento vegetal y posible biocontrol del patógeno. Estos resultados sugieren un gran potencial para la selección de microorganismos biocontroladores y desarrollo de bioproductos a partir de recursos microbiológicos locales.

The powdery scab of potato is caused by the pathogen Spongospora subterranea which reduces the quality and yield of tubers and facilitates the establishment of other pathogens. This disease affects main potato production zones in the world, because there is not a completely effective and available control method against the disease, and due to the trading of infested seed tubers. Some research suggests that biological control agents could reduce the activity of S. subterranea through effects on the viability of their cystosoris or zoospores or by stimulating plant growth. In this research, bacteria previously isolated, from inside the roots, the rhizosphere and tuber peel of potato plants (Solanum tuberosum var. Diacol Capiro), were used, and then selected according to their capacity for producing total indoles and chitinases. Here was tested in parallel studies the capacity of nine bacterial isolates differing in total indole and chitinase production, for its capacity at increasing tuber sprout length and in promoting plant growth and biocontrol of S. subterranea . Inoculated in excised minitubers in laboratory most indole producing isolates tested resulted in increased tuber sprout length. In the greenhouse assay, in non-sterile soil and under a high pathogen pressure, two of the ten isolates selected because for their ability to produce total indoles and chitinases, showed plant growth promotion and possible biocontrol of the pathogen. These results suggest a great potential for the selection of biocontrol microorganisms and the development of new bioproducts from local microbial resources.

Selección y caracterización de rizobacterias promotoras de crecimiento vegetal (RPCV) asociadas al cultivo de algodón (Gossypium hirsutum) / Selection and characterization of plant growth promoting rhizobacteria (PGPR’s) associated with cotton crop (Gossypium hirsutum)

Como parte de las estrategias de una agricultura sostenible, se hace necesario disminuir el uso de fertilizantes nitrogenados de síntesis, mediante la utilización de los biofertilizantes. En particular, los géneros Azotobacter y Azospirillum son utilizados como agentes promotores de crecimiento vegetal debido a su capacidad para fijar nitrógeno atmosférico y producir hormonas de tipo indólico. Por tal razón, en este estudio se aislaron bacterias diazotróficas de los géneros Azotobacter y Azospirillum a partir de la rizósfera de cultivos de algodón en el Espinal (Tolima). Las poblaciones microbianas se caracterizaron fenó­picamente en los medios de cultivo semiespecificos: Ashby y LG (Azotobacter sp.) y NFb, LGI y Batata (Azospirillum sp.). La promoción de crecimiento vegetal se determinó mediante la actividad de la enzima nitrogenasa por medio de la técnica de reducción de acetileno y producción de índoles por el método colorimérico de Salkowsky. Se obtuvieron 9 aislamientos tentativos de Azotobacter sp. y 4 de Azospirillum sp. Se presentaron diferencias significativas en la prueba de reducción de acetileno con las cepas presuntivas de Azotobacter sp.: NAT 9 (206.43 nmol C2H2 mL-1.h-1), NAT 4, (292.77 nmol C2H2 mL-1.h-1), y NAT 6 (460.60 nmol C2H2 mL-1.h-1) y en la producción de índoles de las cepas NAT 19 (19.87 íµg.mL-1) y NAT 13 (20.08 íµg.mL-1). Por su eficiencia In vitro en la promoción de crecimiento vegetal se seleccionaron las cepas NAT9, NAT4, NAT6, NAT19 y NAT13 para ser evaluadas como principio activo en futuros inoculantes para el algodón en esta zona del departamento del Tolima.

As part of strategies for sustainable agriculture, it is necessary to reduce the use of synthetic nitrogen fertilisers through the use of biofertilisers. In particular, the genera Azotobacter and Azospirillum are used as plant growth promoters because of their ability to fix atmospheric nitrogen and indolic type hormones. For this reason, in this study were isolated diazotrophic bacteria of the genera Azotobacter and Azospirillum from the rhizosphere of cotton crops in Espinal (Tolima). The microbial populations were characterized phenotypically in specific semi culture media: Ashby and LG (Azotobacter sp.) and NFb, LGI and Batata (Azospirillum sp.). The promotion of plant growth was determined by the enzyme nitrogenase activity through acetylene reduction technique and production of indoles by the salkowsky colorimetric method. 9 isolates were obtained tentative Azotobacter sp. and 4 of Azospirillum sp. Significant differences in acetylene reduction test with presumptive strains of Azotobacter sp.: NAT 9 (206.43 nmol C2H2 mL-1.h-1), NAT, 4, (292.77 nmol C2H2 mL-1.h-1), and NAT 6 (460.60 nmol C2H2 mL-1.h-1) and indole production strains NAT 19 (19.87 µg.mL-1) and NAT 13 (20.08 µg.mL-1). In vitro efficiency in promoting plant growth were selected strains NAT9, NAT4, NAT6, NAT19 and NAT13 to be evaluated as active in future inoculants on cotton in this part of the department of Tolima.

The effects of different tropisetron administration routes and dosages on cisplatin-induced kaolin intake in rats / 中国医师杂志

Objective To compare the effects of different administration routes and dosages of tropisetron on cisplatin-induced kaolin intake in rats.Methods Ninety-six healthy adult male Wistar SPF rats were randomly divided into 8 groups(n =12 each):intrathecal (IT) control group (group TC) and 3 tropisetron groups receiving IT tropisetron 10,20 and 30 μg,the volume of each group was 30 μl (group T10,T20,T30),intravenous(Ⅳ) control group (group IC) and 3 tropisetron groups receiving Ⅳ tropisetron 0.3,0.5 and 0.7 mg/kg respectively (group I0.3,I0.5,I0.7).In group TC and IC,normal saline 30 μl and 0.5 ml were injected IT and Ⅳ,respectively.All rats received cisplatin 3mg/kg by intraperitoneal injection at the time point of thirty minutes after administration,each rat weight,the daily food and kaolin intakes were detected at the time point of 48 hours after cisplatin administration.Results Compared with group Tc,each rat weight loss,the kaolin intakes were significantly decreased (P ＜ 0.05),and food intake dose was significantly increased in group T20 (P ＜ 0.05).Compared with group IC,each rat weight loss,the kaolin intakes were significantly decreased (P ＜ 0.05),and food intake dose was significantly increased in group I0.5 and I0.7 (P ＜0.05).There was no significant difference between group I0.5,I0.7 and group T20.Conclusions The kaolin intakes and the rat weight loss can be decreased by IT tropisetron,and the food take dose was increased meanwhile,and IT tropisetron 20 μg has equivalent efficacy to IV tropisetron 0.5 or 0.7 mg/kg.IT could be the new administration route of tropisetron.

In-silico ADME and toxcity studies of some novel indole derivatives.

Drug design is a process which begins with a compound that displays an interesting biological profile and ends with optimizing both the activity profile for the molecule. The process is initiated when the chemist conceives a hypothesis which relates the chemical features of the molecule (or series of molecules) to the biological activity. Study of Quantitative structural activity relationships (QSAR) is an important aspect of computational chemistry for optimizing the structural features to obtain better activity. Present research work focuses on in-silico drug design studies of novel indole derivatives containing pteridine and benzimidazole moieties. These studies include QSAR (Quantitative structure activity relationship) and QSTR (Quantitative Structure Toxicity Relationship) and are carried out using different software’s namely DS Viewer Pro suite, Accord for Excel (v6.1) and TOPKAT (v6.2). All the software’s were obtained from Accelrys Discovery studio. In-silico pharmacokinetic studies implied that these derivatives had no CYP4502D6 inhibitions, no BBB penetration and good oral absorptions. QSTR (Quantitative Structure Toxicity Relationship) studies by using TOPKAT (v6.1) in various computational animal models showed high LD50 values and the compounds are found to be noncarcenogenic.

Effect of Tenidap on expression of inwardly rectifying potassium channel 2.3 in hippocampi of chronic temporal lobe epileptic rats / 中华神经科杂志

Objective To observe the change of expression of inwardly rectifying K+(Kir)2.3 mRNA and protein of Kir in the hippocampus of rats with chronic temporal lobe epilepsy(TLE)in different time points and the effect of Tenidap a Kir2.3 channel opener on its expression,investigate the relationship between Kir2.3 and the pathogenesis of TLE and to explore the potential of Kir agonists as anti-epileptic drugs.Methods The pilocarpine TLE rat model was used.Animals were randomly assigned to the control or the status epilepticus(SE)groups,which were further divided into four time point subgroups consisting of 0.6,72 hours,and 2 weeks post-SE termination.Another subgroup was given Tenidap,a Kir2.3 channel opener,and tested 2 weeks post-SE.Hippoeampi were removed and the expression of Kir2.3 mRNA and protein at different time points was measured by reverse transcription polymerase chain reaction(RT-PCR)and western blotting.Results The ratios of Kir2.3 mRNA and β-actin in normal control and 0,6,72hours and 2 weeks after SE termination were 0.080±0.030,0.103±0.045,0.164±0.026,0.132±0.024.0.011±0.008,respectively(F=23.684,P<0.01).The ratios of Kir2.3 protein and GAPDH in propotional groups were0.305±0.030,0.263±0.028,0.767±0.167,0.498±0.077,0.176±0.026(F=44.183.P<0.05).The expression of Kir2.3 channel in the epileptic rats was bimodal,increasing immediately after SE,relative to controls,and declining in the chronically epileptic period.Tenidap administration upregulated both the mRNA(0.021±0.006)and protein expression(0.636±0.140) of Kir2.3(F=25.216 and 47.355,P<0.05 and 0.01).Condusion These findings suggest that the pathogenesis of TLE is accompanied by a decrease in Kit2.3 expression,which may be ameliorated by the administration of tenidap.

Effect of propentofylline on NGF and IL-1β release from rat cerebral cortical astrocytes / 中华麻醉学杂志

Objective To investigate the effect of propentofylline on nerve growth factor (NGF) and IL-1βrelease from rat cerebral cortical astrocytes. Methods Primary cultured rat astrocytes from SD rats (1-3 d,weighing 6-8 g) after 4 passages were randomly divided into 8 groups ( n = 6 wells each): group Ⅰ control (group C); group Ⅱ , Ⅲ, Ⅳ the astrocytes were exposed to propentofylline 10, 100 and 1000 μmol/L respectively (group P1, P2, P3 ); group Ⅴ the astrocytes were exposed to LPS 1 μg/ml and group Ⅵ, Ⅶ, Ⅷ the astrocytes were exposed to propentofylline 10, 100 and 1000 μmol/L in addition to LPS 1 μg/ml (group P1 + LPS, P2 + LPS,P3 + LPS). The astrocytes were then incubated for 3 days in all 8 groups. The concentrations of IL-1β and NGF in the supernatant were detected at 1 and 3 days of incubation using ELISA. Results LPS activated astrocytes resulting in decrease in NGF release and increase in IL-1β release. Propentofylline significantly increased NGF release and decreased IL-1β release from astrocytes incubated alone or with LPS by suppressing activation of astrocytes. Conclusion Propentofylline can enhance NGF release and inhibit IL-1β release from rat cerebral cortical astrocytes.

A novel method for rapid identification and drug resistance of Moraxella catarrhalis / 中华检验医学杂志

Objective To establish a novel method for rapid identification and drug resistance of Moraxella catarrhalis, Different sourses of blood and the formula of chocklate agars were detected the Growth Index(GI). Methods Moraxella catarrhalis from specimens contaminated by microbial flora were isolated with a choclate agar with 50 mg/L vancomycin (CHOC-V) method. Nine media were inoculated,on which GI were calculated and compared. beta-Lactamase were determined by nitrocefin slip method. Results 228 strains of Moraxella catarrhalis and 203 strains of recent limbus bacteria were examined. The sensitivity of this method was 100%,and the specificity was 100%. The GI of Moraxella catarrhalis on chocklate agars and blood agars was higher than that of the BCA, NUA, MHA ( P

Protective mechanism of 7-nitro indazole in neonatal rats with hypoxic-ischemic brain damage / 中华围产医学杂志

Objective To investigate the protective mechanism of 7-nitro indazole (7-NI) in neonatal rats with hypoxic-ischemic brain damage. Methods Seventy-two Wistar rats of 7-day-old were randomly divided into the sham-operation、HIBD and 7-NI treated group. The HIBD models were established in 7-NI treated and HIBD groups.7-NI (100 mg/kg) or peanut oil (10 ml/kg) was injected intraperitoneally 0.5 h before hypoxia in 7-NI treated group or HIBD group. NOS,NO,SOD and MDA were examined at different time (1 h、2 h、6 h、8 h). Terminal deoxynucleotidyl transferase mediated dUTP-biotin nick end labeling(TUNEL) method was used to detect neuronal apoptosis. Results NOS and NO level of HIBD group at different time were significantly higher than that of the sham-operation group [NOS:1 h (3.345?0.367)U/mg, 8 h (4.469?0.275) U/mg vs (1.555?0.223) U/mg; NO: 1 h (2.419?0.254) ?mol/g, 8 h (3.556?0.309) ?mol/g vs (0.749?0.135) ?mol/g, P