Dengue virus (DENV) infection can lead to a wide range of clinical manifestations, including fatal hemorrhagic complications. There is a need to find effective pharmacotherapies to treat this disease due to the lack of specific immunotherapies and antiviral drugs. That said, the DENV NS2B/NS3pro protease complex is essential in both the viral multiplication cycle and in disease pathogenesis, and is considered a promising target for new antiviral therapies. Here, we performed a systematic review to evaluate the pharmacophoric characteristics of promising compounds against NS2B/NS3pro reported in the past 10 years. Online searches in the PUBMED/MEDLINE and SCOPUS databases resulted in 165 articles. Eight studies, which evaluated 3,384,268 molecules exhibiting protease inhibition activity, were included in this review. These studies evaluated anti-dengue activity in vitro and the IC and EC values were provided. Most compounds exhibited non-competitive inhibition. Cytotoxicity was evaluated in BHK-21, Vero, and LLC-MK2 cells, and the CC values obtained ranged from < 1.0 to 780.5 µM. Several groups were associated with biological activity against dengue, including nitro, catechol, halogen and ammonium quaternaries. Thus, these groups seem to be potential pharmacophores that can be further investigated to treat dengue infections.
Abstractobjective To entomologically monitor Aedes spp. and correlate the presence of these vectors with the recent epidemic of dengue in Divinopolis, Minas Gerais State, Brazil.methods Ovitraps were installed at 44 points in the city, covering six urban areas, from May 2011 to May 2012. After collection, the eggs were incubated until hatching. In the 4th stage of development, the larvae were classified as Ae. aegypti or Ae. albopictus.results In total, 25 633 Aedes spp. eggs were collected. February was the month with the highest incidence, with 5635 eggs collected and a hatching rate of 46.7%. Ae. aegypti eggs had the highest hatching rate, at 72.3%, whereas Ae. albopictus eggs had 27.7%. Climate and population density influenced the number of eggs found. Indicators of vector presence were positively correlated with the occurrence of dengue cases.conclusion These data reinforce the need for entomological studies, highlight the relevance of Ae. albopictus as a possible disease vector and demonstrate its adaptation. Ae. albopictus, most commonly found in forested areas, comprised a substantial proportion of the urban mosquito population.
Infections caused by multidrug-resistant bacteria are a problem of public health, turning the search for natural products an alternative to antibiotics of great importance. The aim of this study was to investigate the in vitro antimicrobial activities of Hymenaea courbaril and Stryphnodendron adstringens against bacterial clinical isolates. The crude extracts of both vegetal species in study showed bacteriostatic activity against almost all bacteria evaluated, with minimum inhibitory concentration (MIC) ranging from 125 to 1250 µg/ml. The bacteriostatic activity was observed in all the fractions of H. courbaril and S. adstringens against at least one bacterial strain, except in the fraction dichloromethane of S. adstringens. In regard to bactericidal activity, H. courbaril was active only against E. faecalis, and S. adstringens showed activity against all bacterial strains, except to Enterococcus faecalis. The combination of extracts showed potent synergistic antimicrobial activity, with MIC values of 31.25 µg/ml against Acinetobacter baumannii, Escherichia coli and Staphylococcus aureus. S. adstringens were considered less cytotoxic compared to H. courbaril and the half-maximum cytotoxic concentration (CC 50) resulting from the combination of the two plants was 0.0082 ± 3.19 mg/ml. The results showed for the first time the synergic antibacterial activities of H. courbaril and S. adstringens against resistant bacteria, suggesting their potential use to development of new drugs.
Background:
Coronaviruses have caused outbreaks of respiratory disease since the beginning of the 21st century, representing a significant threat to public health. Together, the severe acute respiratory syndrome coronavirus (SARS-CoV), the respiratory syndrome coronavirus (MERS-CoV), and, more recently, the novel coronavirus (SARS-CoV-2) have caused hundreds of thousands of deaths around the world. Thus, investments in research and the development of strategies aimed at diagnosing, treating, and preventing these infections are urgently needed.
Objective:
The objective of this study was to analyze the patents that address pathogenic coronaviruses in Google Patents databases in the last year (2019-2020).
Method :
The search strategy was carried out in April 2020, based on the keywords “SARS”, “SARS-CoV”, “MERS”, “MERS-CoV”, “SARS-CoV-2” and “COVID-19. Out of the patents examined, 25 were selected for a short description in this study. Results: A total of 191 patents were analyzed, 149 of which were related to SARS-CoV, and 29 and 12 were related to MERS-CoV and SARS-CoV2, respectively. The patents addressed the issues of diagnosis, therapeutic agents, prevention and control, along with other applications.
Conclusion:
Several promising strategies have been documented in intellectual property databases favoring the need for further studies on the pathogenesis and optimization of the diagnosis and therapeutic treatment for these emerging infections.
Atualmente, a bactéria Staphylococcus aureus tem se tornado resistente aos principais antibióticos disponíveis, sendo necessária a descoberta de novos medicamentos. Assim, o objetivo deste trabalho foi avaliar a atividade bacteriostática, através do método de diluição em caldo, e bactericida de vinte e dois compostos glicídicos sintetizados frente à Staphylococcus aureus. Os resultados obtidos demonstraram que dois compostos, denominados CABN (derivado de beta-naftol) e PROP (derivado de benzamidina), apresentam atividade bacteriostática na concentração de 100 µmol/L, sendo que o composto 18 apresentou também atividade bactericida na concentração de 200 µmol/L. Dessa forma, os resultados obtidos são prospectivos na elaboração de novos fármacos com a obtenção de dois compostos sintéticos glicídicos e aromáticos com potencial função antibacteriana.
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