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Natural Products from Garcinia brasiliensis as Leishmania Protease Inhibitors
Ivan O. Pereira,Diego M. Assis,Maria A. Juliano,Rodrigo L.O.R. Cunha,Clara L. Barbieri,Luis V.S. do Sacramento,Marcos J. Marques,Marcelo H. dos Santos 한국식품영양과학회 2011 Journal of medicinal food Vol.14 No.6
The infections by protozoans of the genus Leishmania are a major worldwide health problem, with high endemicity in developing countries. The drugs of choice for the treatment of leishmaniasis are the pentavalent antimonials, which cause renal and cardiac toxicity. As part of a search for new drugs against leishmaniasis, we evaluated the in vitro Leishmania protease inhibition activity of extracts (hexanic, ethyl-acetate, and ethanolic) and fukugetin, a bioflavonoid purified from the ethyl-acetate extract of the pericarp of the fruit of Garcinia brasiliensis, a tree native to Brazilian forests. The isolated compound was characterized by using spectral analyses with nuclear magnetic resonance, mass spectroscopy, ultraviolet, and infrared techniques. The ethyl-acetate extract and the compound fukugetin showed significant activity as inhibitors of Leishmania's proteases, with mean (±SD) IC50 (50% inhibition concentration of protease activity) values of 15.0±1.3 μg/mL and 3.2±0.5 μM/mL, respectively, characterizing a bioguided assay. In addition, this isolated compound showed no activity against promastigote and amastigote forms of L. (L.) amazonensis and mammalian cells. These results suggest that fukugetin is a potent protease inhibitor of L. (L.) amazonensis and does not cause toxicity in mammalian or Leishmania cells in vitro. This study provides new perspectives on the development of novel drugs that have leishmanicidal activity obtained from natural products and that target the parasite's proteases.
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Mayra Cristina da Luz Pádua Guimarães,Juliana Chaves Coelho,Juliano dos Santos,Camila Braga de Oliveira Higa,Carime Farah Flórido,Renata Jae Won Lee,Grazielli Soares Paes,Giovanio Vieira da Silva,Luci 대한고혈압학회 2022 Clinical Hypertension Vol.28 No.-
Background: Nonadherence to antihypertensive treatment is one of the main causes of the lack of blood pressure (BP) control. The coronavirus disease (COVID-19) pandemic imposes substantial social restriction impairing the medical care routine, which may influence adherence to the antihypertensive treatment. To assess the rate of nonadherence to antihypertensive drug treatment during the COVID-19 pandemic. Methods: This is a cross-sectional study evaluating hypertensive adult patients from a tertiary outpatient clinic. From March to August 2020, patients were interviewed by telephone during the social distancing period of the COVID-19 pandemic. We evaluated biosocial data, habits, attitudes, and treatment adherence using the 4-item Morisky Green Levine Scale during the social distancing. Uncontrolled BP was defined by BP ≥ 140/90 mmHg. Clinical and prescription variables for drug treatment were obtained from the electronic medical record. We performed a multivariate analysis to determine the predictors of nonadherence to BP treatment. Results: We studied 281 patients (age 66 ± 14 years, 60.5% white, 62.3% women, mean education of 9.0 ± 4 years of study). We found that 41.3% of the individuals reported poor adherence to antihypertensive drug treatment and 48.4% had uncontrolled BP. Subsample data identified that adherence was worse during the pandemic than in the previous period. The variables that were independently associated with the nonadherence during the pandemic period were black skin color (odds ratio [OR], 2.62; 95% confidence interval [CI], 1.46–4.68), and intermittent lack of access to antihypertensive medication during the pandemic (OR, 2.56; 95% CI, 1.11–5.89). Conclusions: Beyond traditional variables associated with poor adherence, the lack of availability of antihypertensive medications during the study underscore the potential role of pandemic on hypertension burden.
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