Chemotherapy is limited in the treatment of leishmaniasis due to the toxic effects of drugs, low efficacy of alternative treatments, and resistance of the parasite. This work assesses the in vitro activity of flavopereirine on promastigote cultures of Leishmania amazonensis. In addition, an in silico evaluation of the physicochemical characteristics of this alkaloid is performed. The extract and fractions were characterized by thin-layer chromatography and HPLC-DAD, yielding an alkaloid identified by NMR. The antileishmanial activity and cytotoxicity were assayed by cell viability test (MTT). The theoretical molecular properties were calculated on the Molinspiration website. The fractionation made it possible to isolate a beta-carboline alkaloid (flavopereirine) in the alkaloid fraction. Moreover, it led to obtaining a fraction with greater antileishmanial activity, since flavopereirine is very active. Regarding the exposure time, a greater inhibitory effect of flavopereirine was observed at 24 h and 72 h (IC50 of 0.23 and 0.15 μg/mL, respectively). The extract, fractions, and flavopereirine presented low toxicity, with high selectivity for the alkaloid. Furthermore, flavopereirine showed no violation of Lipinski’s rule of five, showing even better results than the known inhibitor of oligopeptidase B, antipain, with three violations. Flavopereirine also interacted with residue Tyr-499 of oligopeptidase B during the molecular dynamics simulations, giving a few insights of a possible favorable mechanism of interaction and a possible inhibitory pathway. Flavopereirine proved to be a promising molecule for its antileishmanial activity.
Introdução: Um grande desafio para a utilização de registros e bases de dados secundárias é a qualidade do registro e o percentual de perdas em variáveis estratégicas e necessárias à plena utilização do banco. Objetivo: Propor um método de correção para a variável de estadiamento no âmbito dos Registro Hospitalares de Câncer (RHC), a fim de aprimorar sua completude e qualidade. Método: Estudo descritivo, abrangendo as Unidades da Federação, utilizando-se como fonte de informação o RHC, de janeiro de 2013 a dezembro de 2019. O câncer de pulmão foi escolhido como caso para a correção do banco, em razão da sua alta taxa de mortalidade no Brasil e no mundo. As análises foram realizadas com o software de análises estatísticas SAS Studio e a base de dados organizada em Excel®. Resultados: O total de casos registrados no RHC foi de 86.026, e a variável de interesse, o estadiamento, teve um total de 32,0% de perda. Ao final de todas as etapas de correção, a perda foi de 9,8%, correspondendo a 22,2% de recuperação. Conclusão: A metodologia proposta representa um avanço na correção do banco do RHC, possibilitando a utilização dos dados de base secundária, com melhor representatividade das diferentes Regiões do país, sobre o tratamento de câncer de pulmão, com possibilidade de expansão de seu uso para outras topografias.
e18512 Background: Cervical cancer (CC) is one of the most common cancers in Brazil. This study analyzes the epidemiological and clinical characteristics of CC patients from 2012 to 2017 and their care pathway in Rio de Janeiro, Brazil, considering the municipal and state regulations. Methods: Retrospective study using interrupted time series, including women registered in the Hospital Cancer Registry from January 2012 to December 2017. The interventions analyzed were the implementation of the municipal (August 2013) and state (June 2015) regulation for the treatment of CC in Rio de Janeiro. The main outcomes were (A) Individuals from the metropolitan region I (%); (B) referred by the public sector (%); (C) Group I or II staging (%) (D) Patients who received surgery as first treatment (%) (E) positive outcome (%). Results: 3,460 women were included, 71% were 30 to 59 years old. (A) Individuals from the metropolitan region I accounted for over 68% of the patients, with a statistically decrease after municipal regulation and an increase after state regulation. (B) The public sector referred more than 85% of patients by the end of the period, and despite less than 60% of patients diagnosed with stage I and II (C) the percentage of surgery (D) and positive outcomes (E) were increased over time. Conclusions: Municipal and state regulations organized the flow of patients nevertheless is important to invest in infrastructure to increase early detection, aiming to improve equity of access.[Table: see text]
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