Dihydropyrimidinones Against Multiresistant Bacteria.

The increase in bacterial resistance to antimicrobials has led to high morbidity and mortality rates, posing a major public health problem, requiring the discovery of novel antimicrobial substances. The biological samples were identified as the Gram-negative bacilli Acinetobacter baumannii, Escherichia coli, Enterobacter cloacae, Klebsiella pneumoniae, Morganella morgannii, Pseudomonas aeruginosa and Serratia marcescens and the Gram-positive cocci Enterococcus faecium, and Staphylococcus aureus, all of them resistant to at least three classes of antimicrobials. The antibacterial activity of the compounds was checked in vitro by determining the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) by the broth microdilution method and plating in brain heart infusion (BHI) agar, respectively. The chemical characterization of the compounds was performed by measuring the melting point and gas chromatography coupled with mass spectrometry (GC-MS) on a Shimadzu GC-MS-QP system 2010SE. Synthetic compounds showed antimicrobial activity against Gram-positive cocci at MIC concentrations 0.16-80 µg/ml and Gram-negative bacilli at MIC concentrations 23.2-80 µg/ml. Enterococcus faecium and S. aureus had the best MIC values. The results of the cytotoxicity test indicated that the synthetic compounds showed no significant difference in three concentrations tested (5, 20, and 80 µg/ml), allowing cell viability not different from that assigned to the control, without the tested compounds. In this context, the development of DHPM derivatives brings an alternative and perspective on effectiveness of drugs as potential future antimicrobial agents.

Avaliação antifúngica de uma solução à base de glucoprotamina e do óleo essencial de Cymbopogon citratusem leveduras de ambiente hospitalar / Antifungal action of a solution based on the glucoprotamine and the essential oil from Cymbopogon citratus on the yeasts from the hospital environment

O objetivo deste estudo foi de avaliar a atividade antifúngica de uma solução à base de glucoprotamina (GLU) e de óleo essencial (OE) de Cymbopogon citratus. Candida tropicalis, Claviceps lusitaniae, Meyerozyma (Pichia) guilliermondii e Candida parapsilosis foram isoladas das superfícies de um hospital público de Pelotas, RS. A atividade antifúngica da GLU foi analisada nas concentrações de 0,25% a 0,0005%, e para o OE, obtido por Clevenger, foi utilizado nas concentrações de 17.500 µg/mL a 0,034 µg/mL. A análise cromatográfica foi efetuada por meio de CG/MS. A atividade anti-Candidafoi analisada pela técnica de Microdiluição em Caldo para determinar a Concentração Inibitória Mínima (CIM) e a Concentração Fungicida Mínima (CFM). A inibição pela GLU ocorreu em todas as concentrações testadas, enquanto o OE apresentou resultado de CIM que oscilou de 2846 a 5450 µg/mL, e CFM de 2853 a 5330 µg/mL. Alfa­citral (37,10%), beta­citral (32,77% e beta-mirceno (18,75%) foram considerados como os compostos majoritários do OE. Os dados obtidos neste trabalho destacam a atividade antifúngica da solução à base de GLU e do OE de C. citratus na eliminação dos isolados de Candida spp ambientais. (AU)

This study aimed at evaluating the antifungal activity of glucoprotamine solution (GLU) and the essential oil from Cymbopogon citratus (EO). Candida tropicalis, Claviceps lusitaniae, Meyerozyma(Pichia) guilliermondii and Candida parapsilosis were isolated from the samples, which were collected from the surfaces of a public hospital located in Pelotas, RS. The antifungal activity of GLU was detected at the concentrations from 0.25% to 0.0005%, while the EO, by Clevenger, was used at concentrations from 17.500 µg mL to 0.034 µg/mL. Chemical analysis was determined by GC/MS. The anti-Candida activity was performed by using Broth Microdilution technique to determine the Minimal Fungicidal Concentration (MFC) and the Minimal Inhibitory Concentration (MIC). The inhibition by GLU occurred at all of the tested concentrations, whereas the EO showed MIC ranging from 2.846 to 5.450 µ/mL and the CFM from 2.853 to 5.330 µg/mL. Alfa­citral (37.10%), beta­citral (32.77%) and beta-mirceno (18.75%) were the majority compounds in the EO. The data obtained in the present study highlight the effectiveness of the solution based on GLU and EO for eliminating the environmental isolates of Candida spp. (AU)

Avaliação antifúngica de uma solução à base de glucoprotamina e do óleo essencial de Cymbopogon citratus em leveduras de ambiente hospitalar / Antifungal action of a solution based on the glucoprotamine and the essential oil from Cymbopogon citratus on the yeasts from the hospital environment

O objetivo deste estudo foi de avaliar a atividade antifúngica de uma solução à base de glucoprotamina (GLU) e de óleo essencial (OE) de Cymbopogon citratus. Candida tropicalis, Claviceps lusitaniae, Meyerozyma (Pichia) guilliermondii e Candida parapsilosis foram isoladas das superfícies de um hospital público de Pelotas, RS. A atividade antifúngica da GLU foi analisada nas concentrações de 0,25% a 0,0005%, e para o OE, obtido por Clevenger, foi utilizado nas concentrações de 17.500 μg/mL a 0,034 μg/mL. A análise cromatográfica foi efetuada por meio de CG/MS. A atividade anti-Candida foi analisada pela técnica de Microdiluição em Caldo para determinar a Concentração Inibitória Mínima (CIM) e a Concentração Fungicida Mínima (CFM). A inibição pela GLU ocorreu em todas as concentrações testadas, enquanto o OE apresentou resultado de CIM que oscilou de 2846 a 5450 μg/mL, e CFM de 2853 a 5330 μg/mL. Alfa–citral (37,10%), beta–citral (32,77% e beta-mirceno (18,75%) foram considerados como os compostos majoritários do OE. Os dados obtidos neste trabalho destacam a atividade antifúngica da solução à base de GLU e do OE de C. citratus na eliminação dos isolados de Candida spp ambientais.

This study aimed at evaluating the antifungal activity of glucoprotamine solution (GLU) and the essential oil from Cymbopogon citratus (EO). Candida tropicalis, Claviceps lusitaniae, Meyerozyma (Pichia) guilliermondii and Candida parapsilosis were isolated from the samples, which were collected from the surfaces of a public hospital located in Pelotas, RS. The antifungal activity of GLU was detected at the concentrations from 0.25% to 0.0005%, while the EO, by Clevenger, was used at concentrations from 17.500 μg mL to 0.034 μg/mL. Chemical analysis was determined by GC/MS. The anti-Candida activity was performed by using Broth Microdilution technique to determine the Minimal Fungicidal Concentration (MFC) and the Minimal Inhibitory Concentration (MIC). The inhibition by GLU occurred at all of the tested concentrations, whereas the EO showed MIC ranging from 2.846 to 5.450 μ/mL and the CFM from 2.853 to 5.330 μg/mL. Alfa–citral (37.10%), beta–citral (32.77%) and beta-mirceno (18.75%) were the majority compounds in the EO. The data obtained in the present study highlight the effectiveness of the solution based on GLU and EO for eliminating the environmental isolates of Candida spp.

Evaluation of phytotherapy alternatives for controlling Rhipicephalus (Boophilus) microplus in vitro.

The objective of this study was to identify the main chemical components of the essential oil of Cuminum cyminum L. (cumin) and of the fixed oils of Bertholletia excelsa (Brazil nut) and of Helianthus annuus (sunflower seed). As well as testing the three oils and three different commercial synthetic acaricides against engorged females of Rhipicephalus (Boophilus) microplus in order to explore their acaricidal efficacy. Six different concentrations of the oils (200, 100, 50, 25, 12.5 and 6.25 mg/mL) and the active principles were evaluated with the Adult Immersion Test (AIT). The two main chemicals components of C. cyminum L. were the cuminaldehyde and the γ-terpinene. In both B. excelsa and H. annuus were the linoleic and oleic acid. C. cyminum L. showed high acaricidal activity (100%) over the engorged females and on their reproductive characteristat from the concentration of 100 mg/mL. B. excelsa and H. annuus had low acaricidal activity (39.39% and 58.75% in the concentration of 200 mg/mL respectively). The amidine and the pyrethroid (35.12% and 1.50% respectively). It can be concluded that the oil of C. cyminum L. may be a phytoterapic alternative for the cattle's tick control.

Evaluation of phytotherapy alternatives for controlling Rhipicephalus (Boophilus) microplus in vitro / Avaliação de alternativas fitoterápicas no controle in vitro de Rhipicephalus (Boophilus) microplus

Abstract The objective of this study was to identify the main chemical components of the essential oil of Cuminum cyminum L. (cumin) and of the fixed oils of Bertholletia excelsa (Brazil nut) and of Helianthus annuus (sunflower seed). As well as testing the three oils and three different commercial synthetic acaricides against engorged females of Rhipicephalus (Boophilus) microplus in order to explore their acaricidal efficacy. Six different concentrations of the oils (200, 100, 50, 25, 12.5 and 6.25 mg/mL) and the active principles were evaluated with the Adult Immersion Test (AIT). The two main chemicals components of C. cyminum L. were the cuminaldehyde and the γ-terpinene. In both B. excelsa and H. annuus were the linoleic and oleic acid. C. cyminum L. showed high acaricidal activity (100%) over the engorged females and on their reproductive characteristat from the concentration of 100 mg/mL. B. excelsa and H. annuus had low acaricidal activity (39.39% and 58.75% in the concentration of 200 mg/mL respectively). The amidine and the pyrethroid (35.12% and 1.50% respectively). It can be concluded that the oil of C. cyminum L. may be a phytoterapic alternative for the cattle's tick control.

Resumo O objetivo do presente estudo foi identificar os componentes químicos majoritários do óleo essencial de Cuminum cyminum L. (comino) e dos óleos fixos de Bertholletia excelsa (castanha do Brasil) e de Helianthus annuus (semente de girassol). Assim como testar os três óleos e três diferentes acaricidas comerciais sintéticos contra fêmeas ingurgitadas de Rhipicephalus (Boophilus) microplus, para explorar sua eficácia acaricida. Seis concentrações dos óleos (200, 100, 50, 25, 12,5 and 6,25 mg/mL) e os princípios ativos foram avaliados por meio do Teste de Imersão de Adultas (AIT). Os dois componentes químicos majoritários de C. cyminum L. foram o cuminaldeído e o y-terpineno. Nos óleos de B. excelsa e H. annuus os componentes majoritários foram o ácido n linoleico e oleico, respectivamente. C. cyminum L. mostrou alta atividade acaricida (100%) sobre as fêmeas ingurgitadas e suas caraterísticas reprodutivas, a partir da concentração 100 mg/mL., tornando-se uma fonte alternativa para controlar o carrapato do gado. No entanto sao necessários estudos adicionais, a serem conduzidos in vivo. B. excelsa e H. annuus tiveram baixa atividade acaricida (39,39% e 58,75% na concentração de 200 mg/mL respectivamente), não obstante apresentaram maior efeito que a amidina e o piretroide (35,12% e 1,50% respetivamente). Pode-se concluir que o óleo de C. cyminum pode ser uma alternativa fitoterápica para o controle do carrapato do gado.

Fungi isolated rrom the excreta of wild birds in screening centers in pelotas, rs, Brazil / Fungos isolados de excretas de aves silvestres em centro de reabilitação em Pelotas, RS, Brasil

The identification of the fungal species belonging to the healthy microflora in animals is a precondition for the recognition of pathological processes causing them. The aim of this study was to investigate the presence of potentially pathogenic fungi in the feces of wild birds collected in Screening Centers. Samples were collected from the feces of 50 cages with different species of birds. The samples were processed according to the modified method STAIB and the plates incubated at 32 °C for up to ten days with daily observation for detection of fungal growth. The isolation of the following species was observed: Malassezia pachydermatis, Candida albicans, C. famata, C. guilliermondii, C. sphaerica, C. globosa, C. catenulata, C. ciferri, C. intermedia, Cryptococcus laurentii, Trichosporon asahii, Geotrichum klebahnii, Aspergillus spp., A. niger and Penicillium spp. Knowing the character of some opportunistic fungi is important in identifying them, facilitating the adoption of preventive measures, such as proper cleaning of cages, since the accumulation of excreta may indicate a risk for both health professionals and centers for screening public health.

A identificação das espécies de fungos pertencentes à microbiota saudável em animais é pré-condição para o reconhecimento dos processos patológicos causados por esses. O objetivo deste estudo foi investigar a presença de fungos potencialmente patogênicos nas fezes de aves selvagens coletadas em Centros de Triagem. Foram coletadas amostras de fezes de 50 gaiolas com diferentes espécies de aves. As amostras foram processadas de acordo com o método modificado STAIB e as placas foram incubadas a 32 °C por até dez dias, com observações diárias para detecção do crescimento dos fungos. Observamos o isolamento de espécies: Malassezia pachydermatis, Candida albicans, C. famata, C. guilliermondii, C. sphaerica, C. globosa, C. catenulata, C. ciferri, C. intermedia, Cryptococcus laurentii, Trichosporon asahii, Geotrichum klebahnii, Aspergillus spp., A. niger e Penicillium spp. Conhecendo o caráter de alguns fungos oportunistas resalta-se a importância para identificá-los, facilitando a adoção de medidas preventivas, como a limpeza adequada das gaiolas, uma vez que a acumulação de excrementos pode indicar um risco tanto para os profissionais de saúde e centros de triagem de saúde pública.

Fungi isolated from the excreta of wild birds in screening centers in Pelotas, RS, Brazil.

The identification of the fungal species belonging to the healthy microflora in animals is a precondition for the recognition of pathological processes causing them. The aim of this study was to investigate the presence of potentially pathogenic fungi in the feces of wild birds collected in Screening Centers. Samples were collected from the feces of 50 cages with different species of birds. The samples were processed according to the modified method STAIB and the plates incubated at 32 °C for up to ten days with daily observation for detection of fungal growth. The isolation of the following species was observed: Malassezia pachydermatis, Candida albicans, C. famata, C. guilliermondii, C. sphaerica, C. globosa, C. catenulata, C. ciferri, C. intermedia, Cryptococcus laurentii, Trichosporon asahii, Geotrichum klebahnii, Aspergillus spp., A. niger and Penicillium spp. Knowing the character of some opportunistic fungi is important in identifying them, facilitating the adoption of preventive measures, such as proper cleaning of cages, since the accumulation of excreta may indicate a risk for both health professionals and centers for screening public health.