Discovery of Prenyltransferase-Guided Hydroxyphenylacetic Acid Derivatives from Marine Fungus Penicillium sp. W21C371.

Traditional isolation methods often lead to the rediscovery of known natural products. In contrast, genome mining strategies are considered effective for the continual discovery of new natural products. In this study, we discovered a unique prenyltransferase (PT) through genome mining, capable of catalyzing the transfer of a prenyl group to an aromatic nucleus to form C-C or C-O bonds. A pair of new hydroxyphenylacetic acid derivative enantiomers with prenyl units, (±)-peniprenydiol A (1), along with 16 known compounds (2-17), were isolated from a marine fungus, Penicillium sp. W21C371. The separation of 1 using chiral HPLC led to the isolation of the enantiomers 1a and 1b. Their structures were established on the basis of extensive spectroscopic analysis, including 1D, 2D NMR and HRESIMS. The absolute configurations of the new compounds were determined by a modified Mosher method. A plausible biosynthetic pathway for 1 was deduced, facilitated by PT catalysis. In the in vitro assay, 2 and 3 showed promising inhibitory activity against Escherichia coli ß-glucuronidase (EcGUS), with IC50 values of 44.60 ± 0.84 µM and 21.60 ± 0.76 µM, respectively, compared to the positive control, D-saccharic acid 1,4-lactone hydrate (DSL). This study demonstrates the advantages of genome mining in the rational acquisition of new natural products.

Synthesis, molecular dynamics simulation, and evaluation of biological activity of novel flurbiprofen and ibuprofen-like compounds.

The frequent use of anti-inflammatory drugs and the side effects of existing drugs keep the need for new compounds constant. For this purpose, flurbiprofen and ibuprofen-like compounds, which are frequently used anti-inflammatory compounds in this study, were synthesized and their structures were elucidated. Like ibuprofen and flurbiprofen, the compounds contain a residue of phenylacetic acid. On the other hand, it contains a secondary amine residue. Thus, it is planned to reduce the acidity, which is the biggest side effect of NSAI drugs, even a little bit. The estimated ADME parameters of the compounds were evaluated. Apart from internal use, local use of anti-inflammatory compounds is also very important. For this reason, the skin permeability values of the compounds were also calculated. And it has been found to be compatible with reference drugs. The COX enzyme inhibitory effects of the obtained compounds were tested by in vitro experiments. Compound 2a showed significant activity against COX-1 enzyme with an IC50 = 0.123 + 0.005 µM. The interaction of the compound with the enzyme active site was clarified by molecular dynamics studies.

New Hydroxyphenylacetic Acids and α-Pyrone Derivative from the Deep-Sea Cold Seep Sediment-Derived Fungus Penicillium corylophilum CS-682.

Two pairs of new enantiomeric hydroxyphenylacetic acid derivatives, (±)-corylophenols A and B ((±)-1 and (±)-2), a new α-pyrone analogue, corylopyrone A (3), and six andrastin-type meroterpenoids (4-9) were isolated and identified from the deep-sea cold-seep sediment-derived fungus Penicillium corylophilum CS-682. Their structures and stereo configurations were determined by detailed spectroscopic analysis of NMR and MS data, chiral HPLC analysis, J-based configuration analysis, and quantum chemical calculations of ECD, specific rotation, and NMR (with DP4+ probability analysis). Compound 3 showed inhibitory activity against some strains of pathogenic bacteria.

Sinovite e tenossinovite no Brasil: uma análise dos benefícios auxílio-doença / Synovitis and tenosynovitis in Brazil: analysis of sickness benefit claims

OBJETIVO: Analisar os fatores pessoais associados à prevalência e duração dos benefícios auxílio-doença decorrentes de sinovite e tenossinovite (CID10 M65). MÉTODO: Estudo transversal referente aos benefícios auxílio-doença decorrentes de sinovite e tenossinovite concedidos pelo Instituto Nacional de Seguro Social aos empregados no Brasil em 2008. Dados sobre o ramo de atividade econômica (Classificação Nacional de Atividades Econômicas - CNAE divisão, classe), sexo, idade, espécie e duração dos benefícios foram coletados do Sistema Único de Benefícios. A população corresponde à média mensal dos vínculos empregatícios declarados ao Cadastro Nacional de Informações Sociais. RESULTADOS: Em 2008 foram concedidos 35.601 benefícios auxílio-doença decorrentes de sinovite e tenossinovite, com prevalência de 10,9/10.000 vínculos empregatícios. No conjunto dos benefícios auxílio-doença houve maior razão de prevalência (RP) acidentária (RP 1,2), sendo esta maior em mulheres (RP 3,3), e em trabalhadores com idade acima de 39 anos (RP 1,4). As CNAE 37-Esgoto (55,4) e 60-Atividade de rádio e TV (47,1) apresentaram as maiores prevalências, no entanto, 64-Atividade de serviços financeiros e 6422-Bancos múltiplos caracterizaram mais acidentes de trabalho (RP 3,2 e 3,8, respectivamente) e maior duração (70 e 73 dias, respectivamente). A maior duração de benefício ocorreu entre trabalhadores com idade superior a 39 anos. Tanto a CNAE-divisão 60-Atividade de rádio e TV, quanto a CNAE-classe 6010-Atividade de rádio apresentaram elevadas razões de feminilidade (RP 8,1 e 10,8, respectivamente). CONCLUSÃO: A incapacidade para o trabalho por sinovite e tenossinovite apresenta associação tanto da prevalência quanto da duração com o ramo de atividade, sexo, idade e espécie de benefício (previdenciário/acidentário). .

OBJECTIVE: To analyse the personal and occupational factors associated with the prevalence and duration of sickness benefit claims due to synovitis and tenosynovitis (CID10 M65). METHODS: Cross-sectional study regarding sickness benefit claims due to synovitis and tenosynovitis granted to employees by National Institute of Social Security in Brazil in 2008. Data on economic activity (Economic Activities National Classification - CNAE division, class), sex, age, type and duration of benefits were collected from the Unified Benefit System. The study's population consists of the average monthly employment contracts declared to the National Register of Social Information. RESULTS: In 2008, 35,601 employees were granted sickness benefits due to synovitis and tenosynovitis, with a prevalence of 10.9/10,000 employments. Sickness benefits showed higher prevalence rates (PR) for work-related claims (PR 1,2), mostly made by females (PR 3.3) and by workers older than 39 years (PR 1,4). The CNAE 37-Sewage (55.4) and 60-Broadcasting Activity (47.1) had the highest overall prevalence. However, the 64-Financial service activities, except insurance and pension funding and 6422-Multiple banks with commercial service had the highest rates of work-related claims (RP 3.2 and 3.8, respectively), and the longer duration (70 and 73 days, respectively). Workers older than 39 years had the highest durations of work disability claims. Both the CNAE-division 60-Broadcasting Activity, and the CNAE-class 6010-Radio showed a high activity ratio of females (PR 8.1 and 10.8, respectively). CONCLUSION: The work disability due to synovitis and tenosynovitis presents prevalence and duration associated with economic activity, sex, age and kind of benefit (non work-related and work-related claims). .

Riesgo potencial de parásitos zoonóticos presentes en heces caninas en Puerto Escondido, Oaxaca / Potential hazard of zoonotic parasites present in canine feces in Puerto Escondido, Oaxaca

Objetivo. Estimar la prevalencia de parásitos potencialmente zoonóticos en heces caninas de Puerto Escondido. Material y métodos. La ciudad se dividió en diez zonas de estudio y éstas se categorizaron en hábitats natural, urbano y suburbano. Se colectaron muestras fecales caninas del piso. Se recuperaron los parásitos por medio de técnicas coproparasitológicas de flotación y frotis directo para su observación microscópica y posterior identificación. Se estimó la prevalencia parasitaria en las heces caninas. Resultados. Todas las zonas presentaron fecalismo canino. La prevalencia parasitaria fue de 73.33%. Los parásitos con mayor prevalencia fueron Toxocara canis (47.78%), Ancylostoma caninum (17.88%) y Dipylidium caninum (13.89%). Conclusión. El fecalismo canino proviene de perros errantes y con dueño. Del total de parásitos encontrados, 66.66% son zoonóticos. Los factores que favorecen la problemática son el hábitat suburbano, el manejo indeseable de la basura y la tenencia irresponsable de los cánidos.

Objective. To estimate the zoonotic parasites prevalence in feral dog feces in Puerto Escondido. Material and methods. The fecalism frecuency was estimated in ten zones. To identify the parasites parasitological flotation and direct smear methods were used. The parasitic prevalence was estimated in the canine feces. Results. All the zones presented canine fecalism. The parasitic prevalence in the feces was 73.33%. The parasites with the highest prevalence were Toxocara canis (47.78%), Ancylostoma caninum (17.88%), and Dipylidium caninum (13.89%). Conclusion. Canine fecalism comes from strayed and owned dogs. 66.66% of the parasites found in the dog feces are zoonotics. The factors associated to this problem are the suburban habitat, waste mishandling and nil tenure of stray dogs.

Use and records of child health handbook focused on growth and development / Uso y llenado de la libreta de salud infantil con el foco en el crecimiento y el desarrollo / Uso e preenchimento da caderneta de saúde da criança com foco no crescimento e desenvolvimento

Objective To evaluate the use and records of the Child Health Handbook (CHH), especially growth and development. Method Cross-sectional study with 358 mother-child pairs registered in 12 Primary Health Centers (PHCs) of a small municipality. Mothers were interviewed at the PHC from February to April 2013 using a questionnaire. Data analysis was done using WHO Anthro software, Epi InfoTM and Stata. Results Fifty-three percent of the mothers were carrying the CHH at the time of the interview, similar to the proportion of mothers who were instructed to bring the CHH to health appointments. Annotations in the CHH during the visits were reported by 49%. The vaccination schedule was completed in 97% of the CHH, but only 9% and 8% of the CHH, respectively, contained growth charts and properly completed developmental milestones. Conclusion Low rates of use and unsatisfactory record-keeping in the CHH reinforce the need for investment in professional training and community awareness for the CHH to become an effective instrument of promotion of child health. .

Objetivo Evaluar el uso y llenado de la Libreta de Salud Infantil (LSI), especialmente el crecimiento y el desarrollo. Método Estudio transversal con 358 pares de madres e hijos matriculados en 12 Unidades Básicas de Salud (UBS) de una ciudad pequeña. Las madres fueron entrevistadas en el UBS desde febrero a abril 2013 mediante un cuestionario. Se utilizó Epi-info y software SPSS. Resultados 53% de las madres estaban llevando LSI durante la entrevista, proporción similar a las madres que recibieron instrucciones para llevar el LSI a la atención de la salud. Anotaciones en LSI durante las visitas se registraron en un 49%. Calendario de vacunas fue completa en el 97% de LSI, pero sólo el 9% y el 8% de LSI tenido, respectivamente, las curvas de crecimiento y desarrollos debidamente cumplimentados. Conclusión El uso y el relleno satisfactorio de LSI refuerzan la necesidad de inversión en la formación profesional y el acercamiento a la comunidad para la LSI se convierte efectivamente en un instrumento de promoción de la salud infantil.
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Objetivo Avaliar uso e preenchimento da Caderneta de Saúde da Criança (CSC), especialmente crescimento e desenvolvimento. Método Estudo transversal com 358 pares mãe-criança atendidos em 12 Unidades Básicas de Saúde (UBS) de município de pequeno porte. As mães foram entrevistadas nas UBS, de fevereiro a abril de 2013, com o uso de questionário. Utilizou-se softwares Epi-info e Stata. Resultados No momento da entrevista, 53% das mães portavam a CSC, proporção similar à de mães que referiram orientação para levar a CSC aos atendimentos de saúde. Anotações na CSC durante os atendimentos foram referidos por 49%. Esquema vacinal estava completo em 97% das CSC, mas apenas 9% e 8% das CSC tinham, respectivamente, gráficos de crescimento e desenvolvimento adequadamente preenchidos. Conclusão O uso e o preenchimento insatisfatório da CSC reforçam a necessidade de investimentos na capacitação dos profissionais e na sensibilização da comunidade para que a CSC se torne efetivamente um instrumento de promoção da saúde infantil. .