Drug combination therapy is a current trend to treat complex diseases. Many benefits are expected from this strategy, such as cytotoxicity decrease, retardation of resistant strains development, and activity increment. This study evaluated in vitro combination between an innovative thiosemicarbazone molecule – BZTS with miltefosine, a drug already consolidated in the leishmaniasis treatment, against Leishmania amazonensis. Cytotoxicity effects were also evaluated on macrophages and erythrocytes. Synergistic antileishmania effect and antagonist cytotoxicity were revealed from this combination therapy. Mechanisms of action assays were performed in order to investigate the main cell pathways induced by this treatment. Mitochondrial dysfunction generated a significant increase of reactive oxygen and nitrogen species production, causing severe cell injuries and promoting intense autophagy process and consequent apoptosis cell death. However, this phenomenon was not strong enough to promote dead in mammalian cell, providing the potential selective effect of the tested combination for the protozoa. Thus, the results confirmed that drugs involved in distinct metabolic routes are promising agents for drug combination therapy, promoting a synergistic effect.
Vulvovaginal candidiasis (VVC) is a disease caused by the abnormal growth of yeast-like fungi in the mucosa of the female genital tract. Candida albicans is the principal etiological agent involved in VVC, but reports have shown an increase in the prevalence of Candida non-C. albicans (CNCA) cases, which complicates VVC treatment because CNCA does not respond well to antifungal therapy. Our group has reported the in vitro antifungal activity of extracts from Sapindus saponaria L. The present study used scanning electron microscopy and transmission electron microscopy to further evaluate the antifungal activity of hydroalcoholic extract from S. saponaria (HE) against yeast obtained from VVC and structural changes induced by HE. We observed the antifungal activity of HE against 125 vaginal yeasts that belonged to four different species of the Candida genus and S. cerevisae. The results suggest that saponins that are present in HE act on the cell
OPEN ACCESSMolecules 2015, 20 9406 wall or membrane of yeast at the first moments after contact, causing damage to these structures and cell lysis.
Previous studies reported antiprotozoal activities of Sapindus saponaria L. The aim of this work was the evaluation of antileishmanial activity and mechanism of action of extract and fractions of S. saponaria L. Hydroethanolic extract (EHA) obtained from fruit pericarps was fractionated using solid-phase extraction in a reversed phase, resulting in fractions enriched with saponins (SAP fraction) and acyclic sesquiterpene oligoglycosides (OGSA fraction). The activities of EHA, SAP, and OGSA were evaluated by antiproliferative assays with promastigote and intracellular amastigote forms. Cytotoxicity on macrophages and hemolytic activity were also analyzed. Morphological and ultrastructural changes in Leishmania amazonensis promastigotes were evaluated by electron microscopy. Flow cytometry was used to investigate mitochondrial dysfunction and phosphatidylserine exposure. OGSA was more selective for parasites than mammalian J774A1 macrophage cells, with selectivity indices of 3.79 and 7.35, respectively. Our results showed that only the OGSA fraction did not present hemolytic activity at its IC50 for promastigote growth. Electron microscopy revealed changes in parasite flagellum, cell body shape, and organelle size, mainly mitochondria. Flow cytometry analysis indicated mitochondrial membrane and cell membrane dysfunction. OGSA showed antileishmanial activity, resulting in several changes to protozoa cells, including mitochondrial depolarization and early phosphatidylserine exposure, suggesting a possible apoptotic induction.
A interação entre proteínas e polissacarídeos pode resultar em novos produtos com propriedades superiores aos polímeros originais com grande potencial tecnológico, e neste sentido, uma importante técnica é encapsulação, especialmente de ingredientes lipídicos, como óleos essenciais. As cápsulas ou esferas formadas possuem potencial para facilitar o emprego de óleos essenciais em alimentos e na indústria farmacêutica, preservando sua atividade biológica, agregando valor nutricional e propriedades tecnológicas. O objetivo deste trabalho foi realizar uma revisão de literatura sobre óleos essenciais e diferentes técnicas de encapsulação para preservação destes compostos. Para realizar a pesquisa foram utilizadas as seguintes palavras-chave: óleo essencial; óleos vegetais; encapsulação; microencapsulação nas bases de dados: Science direct, Scielo e PubMed. Como resultado foi constatada a importância dos óleos essenciais como antimicrobianos naturais para aplicação em alimentos devido aos terpenos presentes em sua composição e, uma vez que são compostos instáveis, pesquisas científicas demonstram a eficiência na encapsulação e preservação da atividade biológica através de diferentes técnicas, com ênfase na importância dos fatores envolvidos no processo, como a escolha dos polímeros para o revestimento do núcleo e a temperatura envolvida na encapsulação para maior preservação dos óleos essenciais.
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