The hexane extract from aerial parts Baccharis sphenophylla Dusén ex Malme (Asteraceae) displayed activity against amastigote forms of Trypanossoma cruzi and was subjected to chromatographic steps to afford one unreported – 7α‐hydroxy‐ent‐abieta‐8(14),13(15)‐dien‐16,12β‐olide (1) and three known diterpenes – ent‐kaur‐16‐en‐19‐oic acid, (2), grandifloric acid (3), and 15β‐tiglinoyloxy‐ent‐kaur‐16‐en‐19‐oic acid (4), two sesquiterpenes – spathulenol (5) and oplopanone (6) – as well as hexacosyl p‐coumarate (7). Isolated compounds were characterized by NMR and ESI‐HR‐MS spectra and were evaluated in vitro for activity against amastigote forms of the parasite T. cruzi – the relevant clinical form in the chronic phase of Chagas disease. In addition, the activity of compounds 1–7 against NCTC cells was evaluated. Compounds 1 and 7 showed effectiveness with EC50 values of 21.3 and 16.9 μM, respectively. Both compounds also exhibited reduced toxicity against NCTC cells (CC50>200 μM) with SI values higher than 9.4 and 11.9. Obtained results suggest that the new ent‐abietane diterpene 1 and alkyl coumarate 7 could be used as prototypes for the development of novel and selective semisynthetic derivatives against intracellular forms of T. cruzi.
Terpenes are one of the most abundant classes of secondary metabolites produced by plants and can be divided based on the number of isoprene units (C5) in monoterpenes (2 units—C10), sesquiterpenes (3 units—C15), diterpenes (4 units—C20), triterpenes (6 units—C30), etc. Chemically, triterpenes are classified based on their structural skeleton including lanostanes, euphanes, cycloartanes, ursanes, oleananes, lupanes, tirucallanes, cucurbitanes, dammaranes, baccharanes, friedelanes, hopanes, serratanes etc. Additionally, glycosylated (saponins) or highly oxidated/degraded (limonoids) triterpenes could be found in nature. The antiinflammatory effect and action as immunomodulators of these secondary metabolites have been demonstrated in different studies. This review reports an overview of articles published in the last 15 years (from 2006 to 2021 using PubMed and SciFinder database) describing the antiinflammatory effects of different triterpenes with their presumed mechanism of action, suggesting that triterpenes could be appointed as natural products with future pharmaceutical applicability.
The therapeutic arsenal for the treatment of leishmaniasis is limited and has serious obstacles, such as variable activity, high toxicity, and costs. To overcome such limitations, it becomes urgent to characterize new bioactive molecules. Plants produce and accumulate different classes of bioactive compounds, and these molecules can be studied as a strategy to combat leishmaniasis. The study presented herein evaluated the leishmanicidal effect of maslinic acid isolated from the leaves of Hyptidendron canum (Lamiaceae) and investigated the morphological that occurred on Leishmania (Leishmania) infantum upon treatment. Maslinic acid was active and selective against promastigote and amastigote forms in a dose-dependent manner. Additionally, it was not toxic to peritoneal macrophages isolated from golden hamsters, while miltefosine and amphotericin B showed mild toxicity for macrophages. Morphological changes in promastigotes of L. (L.) infantum treated with maslinic acid were related to cytoplasmic degeneration, intense exocytic activity, and blebbing in the kDNA; disruption of mitochondrial cristae was observed in some parasites. The nucleus of promastigote forms seems to be degraded and the chromatin fragmented, suggesting that maslinic acid triggers programmed cell death. These results indicate that maslinic acid may be an interesting molecule to develop new classes of drugs against leishmaniasis.
Neste trabalho apresentamos duas contribuições para a literatura de redes de sensores sem fio(WSN). A primeira é um modelo geral para alcançar a reprodutibilidade no nível do kernelem simuladores paralelos. Infelizmente, os usuários devem implementar do zero como suassimulações se repetem em simuladores WSN, mas uma simulação paralela ou distribuída im-põe o princípio de concorrência, não trivial de ser implementada por não especialistas. Testesusando o simulador chamadoJSensorcomprovaram que o modelo garante o nível mais restritode reprodutibilidade, mesmo quando as simulações adotam diferentes números de threads oudiferentes máquinas em múltiplas execuções. A segunda contribuição é o simuladorJSensor,um simulador paralelo de uso geral para aplicações WSN de grande escala e algoritmos dis-tribuídos de alto nível. OJSensorintroduz elementos de simulação mais realistas, como oambiente representado por células personalizáveis e eventos de aplicação que representam fenô-menos naturais, como raios, vento, sol, chuva e muito mais. As células são colocadas em umagrade que representa o ambiente com características do espaço definido pelos usuários, comotemperatura, pressão e qualidade do ar. Avaliações experimentais mostram que oJSensortem boa escalabilidade em arquiteturas de computadores multi-core, alcançando umspeedupde 7,45 em uma máquina com 16 núcleos com tecnologiaHyper-Threading, portanto 50% dosnúcleos são virtuais. O JSensor também provou ser 21% mais rápido que oOMNeT++aosimular um modelo do tipo flooding.
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