Anti-Trichomonas vaginalis activity and chemical analysis of metabolites produced by marine-associated fungi.

Trichomoniasis is the most common non-viral sexually transmitted infection worldwide and it may have serious consequences, especially for women. Currently, 5-nitroimidazole drugs are the treatment of choice for trichomoniasis, although presenting adverse effects and reported cases of drug resistance. Metabolites isolated from marine fungi have attracted considerable attention due to their unique chemical structures with diverse biological activities, including antiprotozoal activity. In this study, we showed the anti-Trichomonas vaginalis activity of fractions obtained from marine fungi and the chemical composition of the most active fraction was determined. Ethyl acetate fractions of the fungus Aspergillus niger (EAE03) and Trichoderma harzianum/Hypocrea lixii complex (EAE09) were active against T. vaginalis. These samples, EAE03 and EAE09, were also effective against the fresh clinical isolate metronidazole-resistant TV-LACM2R, presenting MIC values of 2.0 mg/mL and 1.0 mg/mL, respectively. The same MIC values were found against ATCC 30,236 T. vaginalis isolate. In vitro cytotoxicity revealed only the fraction named EAE03 with no cytotoxic effect; however, the active fractions did not promote a significant hemolytic effect after 1-h incubation. Already, the in vivo toxicity evaluation using Galleria mellonella larvae demonstrated that none of the tested samples caused a reduction in animal survival. The fraction EAE03 was followed for purification steps and analyzed by LC-DAD-MS. Eleven compounds were annotated, including butyrolactone, butanolide, and atromentin. Overall, the range of activities reported confirms the potential of marine fungi to produce bioactive molecules.

Avaliação da terapia medicamentosa de pacientes idosos portadores de hipertensão arterial sistêmica e diabetes mellitus tipo 2 atendidos em uma unidade básica de saúde no município de Xanxerê - SC / Evaluation of the drug therapy of patients with systemic arterial hypertension and Type 2 diabetes mellitus attended at a basic health unit in the city of Xanxerê ­ SC / Evaluación de la terapia medicamentosa de pacientes ancianos portadores de hipertensión arterial sistémica y diabetes mellitus tipo 2 atendidos en una unidad básica de salud en el municipio de Xanxerê - SC

Justificativa e Objetivos: Os idosos representam a parcela da população que mais usa medicamentos, por esse motivo é comum encontrar erros de medicação entre esses pacientes. A hipertensão e o diabetes são as doenças crônicas mais comuns nos idosos, portanto os fármacos anti-hipertensivos e hipoglicemiantes merecem atenção e cuidados na administração e dispensação. A pesquisa teve por objetivo avaliar a farmacoterapia prescrita aos idosos portadores de hipertensão arterial sistêmica e diabetes mellitus tipo 2 atendidos em uma unidade básica de saúde no município de Xanxerê-SC. Métodos: A pesquisa embasou-se na análise da farmacoterapia, patologias associadas e dados socioeconômicos de pacientes com hipertensão arterial sistêmica e diabetes mellitus tipo 2. Resultados: Os 20 idosos incluídos no estudo, tinham média de idade de 70,7 anos (±6,1), com idade mínima de 60 anos e máxima de 84 anos, sendo 70% do gênero feminino e 30% do masculino. O número de medicamentos utilizados variou de 2 a 10, num total de 116 medicamentos em uso pelos pacientes incluídos no estudo. A média por pessoa foi de 5,8 medicamentos (±2,1). Foram identificadas 56 interações medicamentosas. Conclusão: Os dados analisados nesta pesquisa demonstram a existência de riscos de resultados negativos relacionados aos medicamentos em pacientes com hipertensão arterial sistêmica e diabetes mellitus tipo 2. Tais resultados estimulam o desenvolvimento de mecanismos de avaliação de processos que visem reduzir esses riscos, elevando a chance de resultados terapêuticos positivos e benefícios para os pacientes.(AU)

Background and Objectives: The elderly represent the portion of the population that uses the most drugs, so it is common to find medication errors among these patients. Hypertension and diabetes are the most common chronic diseases in the elderly, so antihypertensive and hypoglycemic drugs deserve attention and care in administration and dispensation. The aim of this study was to evaluate the pharmacotherapy prescribed to elderly patients with systemic arterial hypertension and type 2 diabetes mellitus who were treated at a basic health unit in the city of Xanxerê-SC. Methods: The research was based on the analysis of pharmacotherapy, associated pathologies and socioeconomic data of patients with systemic arterial hypertension and type 2 diabetes mellitus. Results: The 20 elderly subjects included in the study had a mean age of 70,7 years (±6,1), with a minimum age of 60 years and a maximum of 84 years, 70% of the female gender and 30% of the male. The number of drugs used ranged from 2 to 10, in a total of 116 medications in use by patients included in the study. The mean per person was 5.8 medications (±2,1). We identified 56 drug interactions. Conclusion: The data analyzed in this study demonstrate the existence of risks of negative drug-related outcomes in patients with systemic arterial hypertension and type 2 diabetes mellitus. These results stimulate the development of process evaluation mechanisms aimed at reducing these risks, increasing the chance of positive therapeutic results and benefits for the patients.(AU)

Justificación y objetivos: Los ancianos representan la porción de la población que más usa medicamentos, por lo que es común encontrar errores de medicación entre estos pacientes. La hipertensión y la diabetes son las enfermedades crónicas más comunes en los ancianos, por lo que los fármacos antihipertensivos e hipoglucemiantes merecen atención y cuidados en la administración y dispensación. La investigación tuvo por objetivo evaluar la farmacoterapia prescrita a los ancianos portadores de hipertensión arterial sistémica y diabetes mellitus tipo 2 atendidos en una unidad básica de salud en el municipio de Xanxerê-SC. Métodos: La investigación se basó en el análisis de la farmacoterapia, patologías asociadas y datos socioeconómicos de pacientes con hipertensión arterial sistémica y diabetes mellitus tipo 2. Resultados: Los 20 ancianos incluidos en el estudio, tenían una media de edad de 70,7 años (±6,1),con edad mínima de 60 años y máxima de 84 años, siendo el 70% del género femenino y el 30% del masculino. El número de medicamentos utilizados varía de 2 a 10, en un total de 116 medicamentos en uso por los pacientes incluidos en el estudio. La media por persona fue de 5,8 medicamentos (±2,1). Se identificaron 56 interacciones medicamentosas. Conclusiones: Los datos analizados en esta investigación demuestran la existencia de riesgos de resultados negativos relacionados con los medicamentos en pacientes con hipertensión arterial sistémica y diabetes mellitus tipo 2. Estos resultados estimulan el desarrollo de mecanismos de evaluación de procesos para reducir estos riesgos, elevando la probabilidad de resultados terapéuticos positivos y beneficios para los pacientes.(AU)

Anti-Trichomonas vaginalis activity of betulinic acid derivatives.

Caused by Trichomonas vaginalis, trichomoniasis is the most common non-viral STD worldwide. Currently, metronidazole and tinidazole are the only drugs approved for treatment of the condition. However, problems such as metronidazole-resistant T. vaginalis isolates and allergic reactions have been reported. Based on data previously published by our group, structural changes in betulinic acid (1) were performed, generating three new compounds that were tested for in vitro anti-T.vaginalis activity in this study. Whereas derivative 2 did not demonstrate anti-T. vaginalis activity, derivatives 3 and 4 reduced trophozoite viability by 100%, with MIC values of 50µM. The structural difference of two compounds was performed only on the C-28 position. Derivative 3 showed low cytotoxicity against Vero cells in 24h; however, derivative 4 was highly cytotoxic, but efficient when associated with metronidazole in the synergism assay. ROS production by neutrophils was reduced, and derivative 3 showed anti-inflammatory effect. Collectively, the results of this study provide in vitro evidence that betulinic acid derivatives 3 and 4 are potential compounds with anti-T. vaginalis activity.