Antimicrobial properties of heterocyclic compounds against clinical mastitis isolates / Propriedades antimicrobianas de compostos heterocíclicos contra isolados de mastite clínica

Mastitis causes significant economic losses to the dairy cattle industry. The present study aimed to evaluate the antibacterial properties of 39 heterocyclic derivatives (1,3-thiazoles and 4-thiazolidinones) against clinical mastitis isolates from dairy cows. Milk samples were collected from cows with clinical mastitis and the bacterial species were identified by PCR. Antibacterial activity was assessed using the broth microdilution method. First, 39 heterocyclic compounds were tested against four bacterial isolates (Staphylococcus aureus, Streptococcus agalactiae, Corynebacterium bovis and Escherichia coli) randomly chosen from those recovered from the milk samples (Study 1). Subsequently, the compounds with the strongest antibacterial activity were tested against all the bacterial isolates recovered from the milk samples (Study 2). 1,3-thiazoles showed the strongest antibacterial activity, specially compounds 30 and 38, which also showed bactericidal properties according to their minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) values. Corynebacterium spp. and Enterobacteriaceae isolates were the most susceptible to compounds 30 and 38. Compounds 30 and 38 are promising targets for new antimicrobial agents.(AU)

A mastite causa significativas perdas econômicas à indústria leiteira bovina. O presente estudo teve como objetivo avaliar as propriedades antibacterianas de 39 derivados heterocíclicos (1,3-tiazóis e 4-tiazolidinonas) contra isolados clínicos de mastite em vacas leiteiras. Amostras de leite foram coletadas de vacas com mastite clínica e as espécies bacterianas isoladas foram identificadas por PCR. A atividade antibacteriana foi avaliada pelo método de microdiluição em caldo. Primeiramente, os 39 compostos heterocíclicos foram testados contra quatro isolados bacterianos (Staphylococcus aureus, Streptococcus agalactiae, Corynebacterium bovis e Escherichia coli) escolhidos aleatoriamente dentre os recuperados das amostras de leite (Estudo 1). Posteriormente, compostos com atividade antibacteriana mais forte foram testados contra todos os isolados bacterianos recuperados das amostras de leite (Estudo 2). Os compostos 1,3-tiazóis apresentaram a maior atividade antibacteriana, principalmente os compostos 30 e 38, que também apresentaram propriedades bactericidas de acordo com seus valores de concentração inibitória mínima (CIM) e concentração bactericida mínima (CBM). Os isolados Corynebacterium spp. e Enterobacteriaceae foram os mais suscetíveis aos compostos 30 e 38. Os compostos 30 e 38 mostraram-se promissores como novos agentes antimicrobianos.(AU)

Antimicrobial properties of heterocyclic compounds against clinical mastitis isolates

ABSTRACT: Mastitis causes significant economic losses to the dairy cattle industry. The present study aimed to evaluate the antibacterial properties of 39 heterocyclic derivatives (1,3-thiazoles and 4-thiazolidinones) against clinical mastitis isolates from dairy cows. Milk samples were collected from cows with clinical mastitis and the bacterial species were identified by PCR. Antibacterial activity was assessed using the broth microdilution method. First, 39 heterocyclic compounds were tested against four bacterial isolates (Staphylococcus aureus, Streptococcus agalactiae, Corynebacterium bovis and Escherichia coli) randomly chosen from those recovered from the milk samples (Study 1). Subsequently, the compounds with the strongest antibacterial activity were tested against all the bacterial isolates recovered from the milk samples (Study 2). 1,3-thiazoles showed the strongest antibacterial activity, specially compounds 30 and 38, which also showed bactericidal properties according to their minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) values. Corynebacterium spp. and Enterobacteriaceae isolates were the most susceptible to compounds 30 and 38. Compounds 30 and 38 are promising targets for new antimicrobial agents.

RESUMO: A mastite causa significativas perdas econômicas à indústria leiteira bovina. O presente estudo teve como objetivo avaliar as propriedades antibacterianas de 39 derivados heterocíclicos (1,3-tiazóis e 4-tiazolidinonas) contra isolados clínicos de mastite em vacas leiteiras. Amostras de leite foram coletadas de vacas com mastite clínica e as espécies bacterianas isoladas foram identificadas por PCR. A atividade antibacteriana foi avaliada pelo método de microdiluição em caldo. Primeiramente, os 39 compostos heterocíclicos foram testados contra quatro isolados bacterianos (Staphylococcus aureus, Streptococcus agalactiae, Corynebacterium bovis e Escherichia coli) escolhidos aleatoriamente dentre os recuperados das amostras de leite (Estudo 1). Posteriormente, compostos com atividade antibacteriana mais forte foram testados contra todos os isolados bacterianos recuperados das amostras de leite (Estudo 2). Os compostos 1,3-tiazóis apresentaram a maior atividade antibacteriana, principalmente os compostos 30 e 38, que também apresentaram propriedades bactericidas de acordo com seus valores de concentração inibitória mínima (CIM) e concentração bactericida mínima (CBM). Os isolados Corynebacterium spp. e Enterobacteriaceae foram os mais suscetíveis aos compostos 30 e 38. Os compostos 30 e 38 mostraram-se promissores como novos agentes antimicrobianos.

Presence of carbohydrate binding modules in extracellular region of class C G-protein coupled receptors (C GPCR): An in silico investigation on sweet taste receptor

Sweet taste receptor (STR) is a C GPCR family member and a suggested drug target for metabolic disorders such asdiabetes. Detailed characteristics of the molecule as well as its ligand interactions mode are yet considerably unclear due toexperimental study limitations of transmembrane proteins. An in silico study was designed to find the putative carbohydratebinding sites on STR. To this end, a-D-glucose and its a-1,4-oligomers (degree of polymerization up to 14) were chosen asprobes and docked into an ensemble of different conformations of the extracellular region of STR monomers (T1R2 andT1R3), using AutoDock Vina. Ensembles had been sampled from an MD simulation experiment. Best poses were furtherenergy-minimized in the presence of water molecules with Amber14 forcefield. For each monomer, four distinct bindingregions consisting of one or two binding pockets could be distinguished. These regions were further investigated withregard to hydrophobicity and hydrophilicity of the residues, as well as residue compositions and non-covalent interactionswith ligands. Popular binding regions showed similar characteristics to carbohydrate binding modules (CBM). Observationof several conserved or semi-conserved residues in these binding regions suggests a possibility to extrapolate the results toother C GPCR family members. In conclusion, presence of CBM in STR and, by extrapolation, in other C GPCR familymembers is suggested, similar to previously proposed sites in gut fungal C GPCRs, through transcriptome analyses. STRmodes of interaction with carbohydrates are also discussed and characteristics of non-covalent interactions in C GPCRfamily are highlighted.

Evaluation of canalis basilaris medianus using cone-beam computed tomography

The aim of this report is to present two cases of canalis basilaris medianus as identified on cone-beam computed tomography (CBCT) in the base of the skull. The CBCT data sets were sent for radiographic consultation. In both cases, multi-planar views revealed an osseous defect in the base of the skull in the clivus region, the sagittal view showed a unilateral, well-defined, non-corticated, track-like low-attenuation osseous defect in the clivus. The appearance of the defect was highly reminiscent of a fracture of the clivus. The borders of osseous defect were smooth, and no other radiographic signs suggestive of osteolytic destructive processes were noted. Based on the overall radiographic examination, a radiographic impression of canalis basilaris medianus was made. Canalis basilaris medianus is a rare anatomical variant and is generally observed on the clivus. Due to its potential association with meningitis, it should be recognized and reported to avoid potential complications.

Modificación de sesgos cognitivos (MSC) en depresión: una revisión crítica de nuevos procedimientos para el cambio de sesgos cognitivos / Cognitive bias modification (CBM) in depression: a critical review of new procedures to change cognitive biases

Los sesgos cognitivos juegan un papel importante como factores de vulnerabilidad en los trastornos emocionales. Recientemente se han empezado a desarrollar intervenciones para la Modificación de Sesgos Cognitivos (MSC), con el objetivo final de mejorar los síntomas clínicos. Aunque estos procedimientos innovadores se han utilizado más en los problemas de ansiedad, existe una investigación creciente sobre su uso en la depresión. En este trabajo efectuamos una revisión del marco teórico, los procedimientos utilizados y los principales resultados de la MSC en la depresión, en especial en la corrección de sesgos atencionales y de interpretación. Finalmente se analizan las limitaciones conceptuales y metodológicas de estas nuevas intervenciones y se discuten sus implicaciones clínicas, teóricas y aplicadas.

Cognitive biases play an important role as vulnerability factors in emotional disorders. Interventions for Cognitive Bias Modification (CBM) have recently begun to be developed with the ultimate goal of improving clinical symptoms. Although these innovative procedures have been applied mainly in anxiety problems, there is increasing research on the application in depression. This work reviews the theoretical framework, the procedures used, and the main results of CBM in depression, especially in the modification of attention and interpretative bias. Finally the conceptual and methodological limitations of these promising interventions procedures are analyzed as well as the clinical, theoretical and applied implications.

Avaliação da atividade antimicrobiana da planta Tradescantia pallida Munt (Taboquinha Roxa) / Evaluation of antimicrobial activity of the Tradescantia pallida Munt plant (Taboquinha Roxa)

RESUMO O objetivo deste estudo foi pesquisar o efeito antimicrobiano in vitro do extrato hidroalcóolico das folhas Tradescantia pallida Munt conhecida como Taboquinha roxa. Foram realizados testes em meio sólido, onde não observou qualquer halo de inibição, e o método de microdiluição, em que os resultados foram expressivos, com determinação da Concentração Inibitória Mínima (CIM) e Concentração Bactericida Mínima (CBM), com resultados em diferentes concentrações. Foram utilizadas cepas padrão de bactérias Gram positivas e Gram negativas. De acordo com os resultados, sugere-se que essa planta apresenta um potencial antimicrobiano.

ABSTRACT The aim of this study was to investigate the in vitro antimicrobial effect of the hydroalcoholic extract of the Tradescantia pallida Munt leaves,known as Taboquinha roxa. The tests were both conducted on solid mean, where it was not observed any zone of inhibition, and by the micro dilution method, in which the results of the Minimum Inhibitory Concentration (MIC) and the Minimum Bactericidal Concentration (MBC) were significant and related with the different concentrations. Standard strains of bacteria type Gram positive and Gram negative were employed. According to the results, this plant has an antimicrobial potential.

Comparative analysis of Chinese oncology papers included by CBM and SCI in 2012 / 国际肿瘤学杂志

Objective To analyze Chinese oncology papers included by Chinese biomedical literature database (CBM) and science citation index (SCI),and to comprehensively and objectively reflect the current situation of Chinese oncology literatures published in domestic and international journals.Methods Chinese oncology papers were retrieved by using CBM and SCI.A comparison analysis was made from the respects of subject distribution,district distribution,organization distribution and high citation situation.Results 67 071 papers of 2012 were retrieved from CBM database,while 9226 papers were indexed by SCI.In terms of district distribution,the first three districts were Jiangsu (6707),Guangdong (4897) and Beijing (2214) in CBM database,while in SCI database,they were Beijing (2214),Shanghai (2008) and Guangdong (1393).The institute with the most amount of literature is university,respectively 9725 and 5755.Moreover,the mostly funded project is National Natural Science Foundation (4710,35.38％ ; 3290,35.68％).Conclusion The 2012 Chinese oncology literatures published in domestic journals has advantage with respect to quantity,compared with the international published journals.However,there exists a bigger difference in terms of quality.Through the comparative analysis,the medical researchers in our country will have some implications in the research orientation.

Screening antimicrobial activity of various extracts of Urtica dioica

Urtica dioica or stinging nettle is traditionally used as an herbal medicine in Western Asia. The current study represents the investigation of antimicrobial activity of U. dioica from nine crude extracts that were prepared using different organic solvents, obtained from two extraction methods: the Soxhlet extractor (Method I), which included the use of four solvents with ethyl acetate and hexane, or the sequential partitions (Method II) with a five solvent system (butanol). The antibacterial and antifungal activities of crude extracts were tested against 28 bacteria, three yeast strains and seven fungal isolates by the disc diffusion and broth dilution methods. Amoxicillin was used as positive control for bacteria strains, vancomycin for Streptococcus sp., miconazole nitrate (30µg/mL) as positive control for fungi and yeast, and pure methanol (v/v) as negative control. The disc diffusion assay was used to determine the sensitivity of the samples, whilst the broth dilution method was used for the determination of the minimal inhibition concentration (MIC). The ethyl acetate and hexane extract from extraction method I (EA I and HE I) exhibited highest inhibition against some pathogenic bacteria such as Bacillus cereus, MRSA and Vibrio parahaemolyticus. A selection of extracts that showed some activity was further tested for the MIC and minimal bactericidal concentrations (MBC). MIC values of Bacillus subtilis and Methicillin-resistant Staphylococcus aureus (MRSA) using butanol extract of extraction method II (BE II) were 8.33 and 16.33mg/mL, respectively; while the MIC value using ethyl acetate extract of extraction method II (EAE II) for Vibrio parahaemolyticus was 0.13mg/mL. Our study showed that 47.06% of extracts inhibited Gram-negative (8 out of 17), and 63.63% of extracts also inhibited Gram-positive bacteria (7 out of 11); besides, statistically the frequency of antimicrobial activity was 13.45% (35 out of 342) which in this among 21.71% belongs to antimicrobial activity extracts from extraction method I (33 out of 152 of crude extracts) and 6.82% from extraction method II (13 out of 190 of crude extracts). However, crude extracts from method I exhibited better antimicrobial activity against the Gram-positive bacteria than the Gram-negative bacteria. The positive results on medicinal plants screening for antibacterial activity constitutes primary information for further phytochemical and pharmacological studies. Therefore, the extracts could be suitable as antimicrobial agents in pharmaceutical and food industry.

Urtica dioica u ortiga se utiliza tradicionalmente como medicina herbaria en el oeste de Asia. En esta investigación se estudia la actividad antimicrobiana de nueve extractos crudos de U. dioica, los cuales fueron preparados utilizando diferentes disolventes orgánicos y obtenidos a partir de dos métodos de extracción: el extractor Soxhlet (Método I), que incluía el uso de cuatro disolventes con acetato de etilo y hexano, y las particiones secuenciales (Método II) con un sistema de cinco disolventes (butanol). Las actividades antibacterianas y antifúngicas de extractos crudos fueron ensayados contra 28 bacterias, tres cepas de levadura y siete cepas fúngicas por la difusión en disco y el método de dilución en caldo. La amoxicilina se utilizó como control positivo para cepas de bacterias, vancomicina para Streptococcus sp., nitrato de miconazol (30μg/mL) como control positivo para los hongos y levaduras, y el metanol puro (v / v) como control negativo. El ensayo de difusión en disco se utilizó para determinar la sensibilidad de las muestras, mientras que el método de dilución en caldo se utilizó para la determinación de la concentración de inhibición mínima (CIM). El acetato de etilo y el extracto de hexano del método de extracción I (AE I y EH I) mostraron mayor inhibición contra algunas bacterias patógenas tales como Bacillus cereus, MRSA y Vibrio parahaemolyticus. Una selección de extractos que mostraron algún tipo de actividad se probó para el CIM y las concentraciones mínimas bactericidas (CMB). Los valores de CIM de Bacillus subtilis y de Staphylococcus aureus resistentes a la meticilina (MRSA) usando extracto de butanol mediante el método de extracción II (EB II) fueron: 8.33 y 16.33mg/ mL, respectivamente; mientras que el valor de MIC con el uso del extracto de acetato de etilo por el Método de extracción II (EAE II) para Vibrio parahaemolyticus fue 0.13mg/mL. Nuestro estudio mostró que el 47.06% de los extractos inhibieron bacterias Gram-negativas (8 de 17), y el 63,63% de los extractos también inhibieron bacterias Gram-positivas (7 de 11), además que estadísticamente la frecuencia de la actividad antimicrobiana fue de 13.45% (35 de 342), que de este porcentaje un 21.71% pertenece alos extractos de actividad antimicrobiana con el método de extracción I (33 de 152 de los extractos crudos) y un 6.82% del método de extracción II (13 de 190 de los extractos crudos). Sin embargo, los extractos crudos del método I exhibieron una mejor actividad antimicrobiana contra las bacterias Gram-positivas que las Gram-negativas. Los resultados positivos en la detección de plantas medicinales para la actividad antibacteriana constituye información primaria para la realización de nuevos estudios fitoquímicos y farmacológicos. Por lo tanto, los extractos podrían ser adecuados como agentes antimicrobianos en la industria farmacéutica y de alimentos.

Antibacterial activity tannin-rich fraction from leaves of Anacardium humile / Atividade antibacteriana de frações tânicas de folhas de Anacardium humile

In vitro tests conducted with extracts rich in tannins have identified several biological activities of this class of substance. Thus, this paper intends to evaluate the antibacterial activity of tannin-rich fraction obtained from leaf extracts of Anacardium humile A.St.-Hil. Extracts of A. humile leaves in 70% acetone were semi-purified with ethyl acetate and butanol. We quantified the total tannins of the semi-purified fractions, of the crude extract and of aqueous residues and then performed tests of the antibacterial activity of the tannins against Staphylococcus aureus ATCC 6538, Pseudomonas aeruginosa ATCC 27853 and Enterococcus faecalis ATCC 29212. All positive extracts underwent tannin isolation using a Sephadex LH-20 column. The tannins isolated from the samples were quantified and tested for the minimal inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC). The tannins from crude extracts, semi-purifications and residues showed inhibition of S. aureus growth with MIC=500 g mL-1. All tannin fractions showed MIC against all strains and MBC, except against E. faecalis. The tannin fractions from Anacardium humile have antibacterial activity against Staphylococcus aureus, Pseudomononas aeruginosa and Enterococcus faecalis and, therefore, may be promising for future synthesis of new antibacterial agents.

Testes in vitro realizados com extratos ricos em taninos têm identificado muitas atividades biológicas dessa classe de substâncias. Nesse contexto, esse artigo propõe a avaliação da atividade antibacteriana de frações tânicas, obtidas de extratos de folhas de Anacardium humile A.St.-Hil. Extratos de A. humile em acetona 70% foram particionados com acetato de etila e butanol. Foram quantificados taninos totais das frações particionadas, do extrato bruto e dos resíduos aquosos, e foi realizado teste de atividade antibacteriana dos taninos contra Staphylococcus aureus ATCC 6538, Pseudomonas aeruginosa ATCC 27853 e Enterococcus faecalis ATCC 29212. Todos os extratos positivos foram submetidos ao isolamento de taninos, utilizando-se coluna de Sephadex LH-20. Os taninos isolados das amostras foram quantificados e testados sua concentração inibitória mínima (CIM) e concentração bactericida mínima (CBM). Os taninos do extrato bruto, partições e resíduos apresentaram inibição do crescimento de S.aureus com CIM =500 g mL-1. As frações tânicas apresentaram CIM contra todas as cepas e CBM, exceto contra E. faecalis. As frações tânicas de Anacardium humile possuem atividade antibacteriana contra Staphylococcus aureus, Pseudomononas aeruginosa e Enterococcus faecalis e, portanto, podem ser promissoras em sínteses futuras de novos agentes antimicrobianos.

Comparative antimicrobial activity of two new mutacins / Actividad microbiana comparativa de dos nuevas mutacinas

OBJECTIVES: To compare the in vitro activity of mutacins D-123.1 and F-59.1 against different bacteria including antibiotic-resistant strains, in order to evaluate their application potential. DESIGN AND METHODS: The antibacterial activity spectrum of purified F-59.1 and the MIC and MBC of F-59.1 and D-123.1 against target bacteria were determined. RESULTS: Most bacteria were inhibited by the purified mutacins. Mutacin F-59.1 shows a relatively wide activity spectrum. Mutacin D-123.1 has low Minimum Inhibitory Concentrations [MICs] (0.25-4 µ/ml) against human pathogens while F-59.1 has higher MICs (3.2-12.8 fig/ml) mainly against food-borne pathogens. CONCLUSION: The effectiveness of mutacins D-123.1 and F-59.1 against human and food-borne pathogens is demonstrated. Mutacin D-123.1 shows potential as a new antibiotic while F-59.1 shows promising application in food products. ABBREVIATIONS: MALDI-TOF MS, matrix assisted laser desorption ionisation-time of flight mass spectrometry; MB(I)C, minimum bactericidal (inhibitory) concentrations; OD, optical density; RP-HPLC, reverse-phase high-pressure liquid chromatography; TSBYE, trypticase soy broth yeast extract.

OBJETIVOS: Comparar la actividad in vitro de las mutacinas D-123.1 y F-59.1 frente a diferentes bacterias incluyendo las cepas resistentes a los antibióticos, a fin de evaluar el potencial de su aplicación. DISEÑO Y MÉTODOS: Se determinó el espectro de actividad antibacteriana de F-59.1 purificada y la CIM y la CBM de F-59.1 y D-123.1 frente a determinadas bacterias. RESULTADOS: La mayor parte de las bacterias eran inhibidas por las mutacinas purificadas. La mutacina F-59.1 muestra un espectro de actividad relativamente amplio. La mutacina D-123.1 posee bajas concentraciones de inhibición mínimas [CIM] (0.25-4 fig/ml) contra los patógenos humanos, mientras que el F-59.1 posee concentraciones CIM más altas (3.2-12.8 fig/ml) principalmente frente a los patógenos alimentarios. CONCLUSIÓN: Queda demostrada la efectividad de las mutacinas D-123.1 y F-59.1 frente a los patógenos humanos y alimentarios. La mutacina D-123.1 muestra poseer un potencial como nuevo antibiótico, en tanto que F-59.1 se presenta como una aplicación promisoria en relación con los productos alimentarios. ABREVIATURAS: MALDI-TOF MS, espectrometría de masas con desorción/ionización mediante láser asistida por matriz asociada a un analizador de tiempo de vuelo (del inglés: matrix assisted laser desorption ionisation-time de flight mass spectrometry). CIM: concentración inhibitoria mínima (inglés MIC). CBM: concentración bactericida mínima (inglés MBC). DO: densidad óptica (inglés OD); RP-HPLC: cromatografía líquida de alta resolución en fase revertida; TSBYE:caldo tripticasa soya- extracto de levadura.

Standardization Realization and Application of CBM Retrieval Strategies for Commonly Used Words in Medical Sci-Tech Novelty Assessment / 医学信息学杂志

The paper expounds the function and significance of establishing CBM retrieval strategies for commonly used words, it could not only promote the quality and efficiency but also have important significance to upgrade and standardize the quality of novelty as-sessment report.

Design of Collaborative Telemedicine Application System on Integrated Multimedia DooRae Framework / 대한의료정보학회지

We propose the various Telemedicine applications on the DooRae (Distributed Object Oriented Multimedia Application Crafting Environment for Collaboration) framework(or platform). DooRae-Telemedicine supports the application development of the collaborative multimedia environment connected with the network(LAN, MAN, WAN) in the CBM(Computer based Multimedia) based. Also, it is not restrict on space between a doctor(s) and a patient(s) into cyberspace made by network. The kinds of Telemedicine in this paper have different distinction, and the development of these application system is possible on DooRae environment. DooRae-Telemedicine has a interaction, various communication type, a question and an answer, multi-session, application sharing and whiteboard which resembles chalkboard. Also, various supplementary functions such as video conference and voice conference for DooRae-telemedicine are what makes face-to-face medicine effective. Also it supports real or non-real type. The operating system developed on windows 95 and windows NT This research has been done creating multimedia-based telemedicine system for home PCs in network environment. Most of telemedicine used hardware and exclusive line of high cost as CATV broadcasting technique. But DooRae-telemedicine will contribute to change the Home-PC for better use of collaborations among doctor and patients through various modes o interactions in cyberspace.