Natural metabolites present an extraordinary chemo-diversity and have been used as the inspiration for new drugs. Considering the need for new treatments against the neglected parasitic disease leishmaniasis, three semi-synthetic derivatives of natural neolignane licarin A were prepared: O-acetyl (1a), O-allyl (1b), and 5-allyl (1c). Using an ex vivo assay, compounds 1a, 1b, and 1c showed activity against the intracellular amastigotes of Leishmania (L.
View Article and Find Full Text PDFLancet Glob Health
November 2021
The search for the pharmacophore of a bioactive compound, crucial for drug discovery studies, involves the adequate arrangement of different atoms in the molecule. As part of a continuous work aiming discovery of new drug candidates against the protozoan parasite Trypanosoma cruzi, the hexane extract of Hydrocotyle bonariensis was subjected to a bioactivity-guided fractionation to afford two chemically related dibenzylbutyrolactone lignans - hinokinin (1) and hibalactone (2). Compounds 1 and 2 showed activity against trypomastigote with EC values of 17.
View Article and Find Full Text PDFInfections caused by parasitic worms impose a considerable worldwide health burden. One of the most impactful is schistosomiasis, a disease caused by blood-dwelling of the genus Schistosoma that affects more than 230 million people worldwide. Since praziquantel has also been extensively used to treat schistosomiasis and other parasitic flatworm infections, there is an urgent need to identify novel anthelmintic compounds, mainly from natural sources.
View Article and Find Full Text PDFBackground: Manaus, located in the Brazilian rainforest, has experienced two health system collapses due to the coronavirus disease 2019 (COVID-19) pandemic. However, little is known about which groups among the general population have been most affected.
Methods: A convenience sampling strategy via online advertising recruited 3046 adults between 19 August 2020 and 2 October 2020.
Schistosomiasis is a widespread human parasitic disease currently affecting over 200 million people, particularly in poor communities. Chemotherapy for schistosomiasis relies exclusively on praziquantel (PZQ). Previous studies have shown that licarin A (LIC-A), a dihydrobenzofuran neolignan, exhibited in vitro antiparasitic activity against Schistosoma mansoni adult worms.
View Article and Find Full Text PDFRev Soc Bras Med Trop
April 2021
Introduction: Electron microscopy (EM) is a rapid and effective tool that can be used to create images of a whole spectrum of virus-host interactions and, as such, has long been used in the discovery and description of viral mechanisms.
Methods: Electron microscopy was used to evaluate the pulmonary pathologies of postmortem lung sections from three patients who died from infection with SARS-associated coronavirus 2 (SARS-CoV-2), a new member of the Coronaviridae family.
Results: Diffuse alveolar damage (DAD) was predominant in all three patients.
Background: Schistosomiasis is a socioeconomically devastating parasitic infection afflicting hundreds of millions of people and animals worldwide. It is the most important helminth infection, and its treatment relies solely on the drug praziquantel. Oral H1-antihistamines are available worldwide, and these agents are among the most widely used of all medications in children and adults.
View Article and Find Full Text PDFLeishmaniasis is a vector-borne disease among the 10 most Neglected Tropical Diseases with diverse clinical manifestations caused by protozoan parasites of the genus. Around 80% of leishmaniasis cases are found in the Old World affecting populations mainly in low and middle-income countries. Its control relies mostly on chemotherapy which still presents many drawbacks.
View Article and Find Full Text PDFNeolignan licarin A (1) was isolated from leaves of Nectandra oppositifolia (Lauraceae) and displayed activity against trypomastigote forms of the etiologic agent of American trypanosomiasis, Trypanosoma cruzi. Aiming for the establishment of SAR, five different compounds (1a - 1e) were prepared and tested against T. cruzi.
View Article and Find Full Text PDFSchistosomiasis is one of the most important parasitic infections in terms of its negative effects on public health and economics. Since praziquantel is currently the only drug available to treat schistosomiasis, there is an urgent need to identify new anthelmintic agents. Piplartine, also known as piperlongumine, is a biologically active alkaloid/amide from peppers that can be detected in high amounts in the roots of Piper tuberculatum.
View Article and Find Full Text PDFThe treatment and control of schistosomiasis, a neglected disease that affects more than 200 million people worldwide, rely on the use of a single drug, praziquantel. A vaccine has yet to be developed and since new drug design and development is a lengthy and costly process, drug repurposing is a promising strategy. In this study, the efficacy of promethazine, a first-generation antihistamine, was evaluated against and in a murine model of schistosomiasis.
View Article and Find Full Text PDFThis work describes the isolation of six metabolites from leaves and branches of Piper cernuum (Piperaceae): (-)-cubebin (1), (-)-hinokinin (2), (-)-kusunokinin (3), trans-dehydroagarofuran (4), 11-hydroxi-4,5-secoeudesmane-4,5-dione (5), and (-)-bornyl p-coumarate (6). Antitrypanosomal activity and toxicity of purified compounds were performed in vitro against trypomastigote forms of Trypanosoma cruzi and NCTC cells, respectively. Compounds 2, 3 and 5 showed moderate activities with IC values of 33.
View Article and Find Full Text PDFIntroduction: In two previous studies, the quality of randomized controlled trials (RCTs) with the participation of at least one plastic surgeon was evaluated in two periods: 1966-2003 and 2004-2008.
Objective: To evaluate the evolution of the quality of RCT publications by plastic surgeons in the subsequent 5-year period, from 2009 to 2013.
Methods: RCTs published from 2009 to 2013 in English with the participation of at least one plastic surgeon were identified by electronic search and classified for concealment of allocation by two independent evaluators.
Epi-polygodial, a drimane sesquiterpene was isolated from Drimys brasiliensis (Winteraceae). This compound demonstrated high parasite selectivity towards Trypanosoma cruzi trypomastigotes (IC = 5.01 μM) with a selectivity index higher than 40.
View Article and Find Full Text PDFHere is reported the anti activity of 48 hexane, CHCl and MeOH extracts from 16 macroalgae collected on the Iberian Coast. Seven hexane and CHCl and extracts were active towards promastigotes (IC 29.8-101.
View Article and Find Full Text PDFThe development of novel drugs for the treatment of leishmaniases continues to be crucial to overcome the severe impacts of these diseases on human and animal health. Several bioactivities have been described in extracts from macroalgae belonging to the Cystoseira genus. However, none of the studies has reported the chemical compounds responsible for the antileishmanial activity observed upon incubation of the parasite with the aforementioned extracts.
View Article and Find Full Text PDFMarine organisms are a prolific source of drug leads in a variety of therapeutic areas. In the last few years, biomedical, pharmaceutical and nutraceutical industries have shown growing interest in novel compounds from marine organisms, including macroalgae. Cystoseira is a genus of Phaeophyceae (Fucales) macroalgae known to contain bioactive compounds.
View Article and Find Full Text PDFMolecules
May 2014
Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro antiparasitic activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.
View Article and Find Full Text PDFThe present study investigates the arguments used by university students in order to explain social differences between social minorities and majorities. In Brazil, the issues investigated refer to White and Black people. In Spain, the reference is to native Spaniards and Moroccan immigrants.
View Article and Find Full Text PDFBackground: One of the major risk variables for surgical site infection is wound management. Understanding infection risk factors for breast operations is essential in order to develop infection-prevention strategies and improve surgical outcomes. The aim of this trial is to assess the influence of dressing wear time on surgical site infection rates and skin colonization.
View Article and Find Full Text PDFPurpose: To analyze the direct costs of conservative surgical treatment of breast cancer, performed in a university hospital, to the Brazilian National Health Care Public System (SUS), checking the impact of the oncoplastic approach on these costs.
Methods: One hundred thirty eight breast cancer patients who had undergone conservative treatment with oncoplastic approach (n=36) or not (control group, n=102), in the period from 2005 to 2010, were enrolled. Sociodemographic and clinical data were recorded.
Leishmaniasis, Chagas disease, and malaria affect the poorest population around the world, with an elevated mortality and morbidity. In addition, the therapeutic alternatives are usually toxic or ineffective drugs especially those against the trypanosomatids. In the course of selection of new anti-protozoal compounds from Brazilian flora, the CH(2)C(l2) phase from MeOH extract obtained from the leaves of Pentacalia desiderabilis (Vell.
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