Black pepper, a commonly utilized culinary condiment, holds significant importance in Ayurvedic and Chinese medicinal practices due to its various biological benefits, including antioxidant, ...antimicrobial, and anti-inflammatory properties. To amplify these attributes and enhance their efficacy in formulations, the utilization of nanocarriers presents a promising approach. Thus, the objective of this study was to obtain a pepper extract, evaluate its constituents, and encapsulate it in polymeric nanoparticles. The ethanol extract of the grains powder had a higher concentration of piperine and better antioxidant activity when compared to whole grains. Pepper extract encapsulation efficiency in terms of piperine concentration was 84.8 ± 3.5%, and a sustained and prolonged release profile was observed, as well as other studies in the literature using polycaprolactone (PCL). The presence of the extract did not change the instability index and the sedimentation velocity of the nanoparticles, as well as the polydispersity index and the zeta potential of nanoparticles. However, there was a difference in the mean size and concentration of particles. This study highlights the potential of PCL nanoparticles as a promising delivery system for black pepper extract, which could have various applications in the cosmetic and pharmaceutical industries, maximizing the benefits of black pepper extract.
Direct antiviral agents (DAAs) are very efficient in inhibiting hepatitis C virus and might be used to treat infections caused by other flaviviruses whose worldwide detection has recently increased. ...The aim of this study was to verify the efficacy of DAAs in inhibiting yellow fever virus (YFV) by using drug repositioning (a methodology applied in the pharmaceutical industry to identify new uses for approved drugs).
Three DAAs were evaluated: daclatasvir, sofosbuvir and ledipasvir or their combinations. For in vitro assays, the drugs were diluted in 100% dimethyl sulfoxide. Vaccine strain 17D and a 17D strain expressing the reporter fluorescent protein were used in the assays. A fast and reliable cell-based screening assay using Vero cells or Huh-7 cells (a hepatocyte-derived carcinoma ell line) was carried out. Two patients who acquired yellow fever virus with acute liver failure were treated with sofosbuvir for one week as a compassionate use.
Using a high-content screening assay, we verified that sofosbuvir presented the best antiviral activity against YFV. Moreover, after an off-label treatment with sofosbuvir, the two female patients diagnosed with yellow fever infection displayed a reduction in blood viremia and an improvement in the course of the disease, which was observed in the laboratory medical parameters related to disease evolution.
Sofosbuvir may be used as an option for treatment against YFV until other drugs are identified and approved for human use. These results offer insights into the role of nonstructural protein 5 (NS5) in YFV inhibition and suggest that nonstructural proteins may be explored as drug targets for YFV treatment.
Neutrophils respond differently to violations of the body's physiological barriers during infections. Extracellular traps comprise one of the mechanisms used by these cells to reduce the spread of ...pathogens to neighboring tissues, as well as ensure a high concentration of antimicrobial agents at the site of infection. To date, this innate defense mechanism has not been previously demonstrated in neutrophils of cats exposed to Toxoplasma gondii. The aim of this study was to characterize the in vitro release of neutrophil extracellular traps (NETs) when neutrophils isolated from cats were exposed to T. gondii. First, cellular viability was tested at different time points after parasite exposure. The production of reactive oxygen species (ROS) and lactate dehydrogenase and the amount of extracellular DNA were quantified. In addition, the number of parasites associated with neutrophils was determined, and the observed NETs formed were microscopically characterized. Results showed that (i) in culture, neutrophils isolated from cats presented diminished cellular viability after 4 h of incubation, and when neutrophils were incubated with T. gondii, they displayed cytotoxic effects after 3 h of interaction; (ii) neutrophils were able to release structures composed of DNA and histones, characterized as NETs under optical, immunofluorescence, and electron scanning microscopy, when stimulated with T. gondii; (iii) only 11.4% of neutrophils were able to discharge NETs during 3 h of incubation; however, it was observed through extracellular quantification of DNA that this small number of cells were able to display different behavior compared to a negative control (no parasite) group; (iv) significant differences in ROS production were observed in neutrophils exposed to T. gondii. In conclusion, our results showed that neutrophils isolated from cats exposed to T. gondii release structures composed of DNA and histones, similar to what has already been described in other neutrophil species infected with the parasite.
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•Here, we demonstrated that cat neutrophils exposed to T. gondii can release NETs.•Tachyzoites from T. gondii are trapped by extracellular NETs released by cat neutrophils.•Toxoplasma gondii diminishes neutrophils viability after 3 h of interaction.•Cat neutrophils, when in contact with T. gondii, produce ROS after 30 min of interaction.•The amount of extracellular DNA released by neutrophils after parasite interaction was time-dependent.
The intensive use of pesticides to control pests in agriculture has promoted several issues relating to environment. As chemical pesticides remain controversial, biocontrol agents originating from ...fungi could be an alternative. Among them, we highlight biocontrol agents derived from the fungi genus
, which have been documented in limiting the growth of other phytopathogenic fungus in the roots and leaves of several plant species. An important member of this genus is
, whose biocontrol agents have been used to promote plant growth while also treating soil diseases caused by microorganisms in both greenhouses and outdoor crops. To evaluate the safety of fungal biological agents for human health, tests to detect potentially adverse effects, such as allergenicity, toxicity, infectivity and pathogenicity, are crucial. In addition, identifying possible immunomodulating properties of fungal biocontrol agents merits further investigation. Thus, the aim of this study was to evaluate the effects of
spores in the internalization of
yeast by mice phagocytes, in order to elucidate the cellular and molecular mechanism of this interaction, as a model to understand possible
effects of this fungus. For this, mice were exposed to a fungal spore suspension through-intraperitoneal injection, euthanized and cells from the peripheral blood and peritoneal cavity were collected for functional, quantitative and phenotypic analysis, throughout analysis of membrane receptors gene expression, phagocytosis ability and cells immunophenotyping M1 (CCR7 and CD86) and M2 (CCR2 and CD206). Our analyses showed that phagocytes exposed to fungal spores had reduced phagocytic capacity, as well as a decrease in the quantity of neutrophils and monocytes in the peripheral blood and peritoneal cavity. Moreover, macrophages exposed to
spores did not display the phenotypic profile M1/M2, and had reduced expression of pattern recognition receptors, such as TLR2, dectin-1 and dectin-2, all involved in the first line of defense against clinically important yeasts. Our data could infer that
spores may confer susceptibility to infection by
.
Migraine is one of the most common forms of headache and affects approximately 15% of the world's population, and it is considered a disabling disease. There are several treatments to control ...migraine pain and symptoms, and the most common pharmaceutical form used is oral tablets. Oral treatment during acute migraine attacks is not fully effective because of its associated symptoms, such as nausea and vomiting, and oral administration of actives also limits bioavailability. Transdermal formulations are a promising alternative for the administration of these actives, as they can considerably improve the bioavailability and efficacy of the treatment, without the inconvenience of invasive treatments. Thus, this article reviews transdermal delivery systems for migraine, emphasizing advantages, as promising technological strategies for effective, comfortable, and strong adhesion promoters to migraine treatment, presenting studies available in the area, as well as the lack of drugs available on the market for transdermal delivery.
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•T. stromaticum biocontrol agent induces autophagy, up-regulating autophagy-related genes•T. stromaticum modulates expression of micro RNAs that control imune response•T. stromaticum dow-nregulates ...expression of TLR2, TLR4, CLEC7A, NLRP3, IL-10, IL1β and IL18•T. stromaticum modulates ROS production
Trichoderma spp. are usually considered safe and normally used as biocontrol and biofertilization. Safety for human health is evaluated by several tests that detect various effects such as allergenicity, toxicity, infectivity, and pathogenicity. However, they do not evaluate the effects of the agent upon the immune system. The aim of this study was to investigate the interaction between T. stromaticum spores and mammalian cells to assess the immunomodulatory potential of the spores of this fungus. First, mouse macrophage cell line J774 and human macrophages were exposed to fungal spores and analyzed for structural features, through scanning and transmission electron microscopy. Then, various analysis were performed in human macrophages as to their effect in some functional and molecular aspects of the immune system through immunocytochemistry, flow cytometry and gene expression assays. We demonstrated that T. stromaticum spores induces autophagy and autophagy-related genes (ATGs) and downmodulate inflammatory mediators, including ROS, NLRP3, the cytokines IL-1β, IL-18, IL-12 and IL-10, as well as TLR2, TLR4, miR-146b and miR-155, which may lead to an augmented susceptibility to pathogens. Our study shows the extension of damages the biofungicide Tricovab® can cause in the innate immune response. Further studies are necessary to elucidate other innate and adaptive immune responses and, consequently, the safety of this fungus when in contact with humans.
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PVA-CO-AAM and peg-co-aam hydrogels as bromelain carriers Coco, Julia Cedran; Tundisi, Louise Lacalendola; Santos, Érica Mendes dos ...
Journal of drug delivery science and technology,
June 2021, 2021-06-00, Letnik:
63
Journal Article
Recenzirano
In this paper, hydrogels were prepared by copolymerization of acrylamide (AAm) with PVA and PEG to study the incorporation and release of bromelain. The association of bromelain with polyvinyl ...alcohol (PVA) or polyethylene glycol (PEG) in a hydrogel for controlled release has potential for burns noninvasive treatment and topical inflammatory occurrences. Total protein concentration and bromelain enzymatic activity was determined by Bradford and azocasein assay methods, respectively. Bro-PVA-co-AAm (bromelain loaded PVA hydrogels) incorporated 42.5 mg and 23.1 U, corresponding to 91.3% and 88.9%, respectively of protein content and enzymatic activity; while PEG hydrogels incorporated 41.4 mg and 16.0 U, corresponding to 88.9% and 53.8%, respectively. PVA and PEG hydrogels released less than 5% of the incorporated protein content after 24 h of study. However, release in terms of enzymatic activity reached 60% (Bro-PVA-co-AAm hydrogel) and 100% (Bro-PEG-co-AAm hydrogel). The joint analysis of hydrogels mechanical properties indicated that bromelain-loaded PVA hydrogels have more structural compatibility to biological conditions, due to a complex molecular architecture, with a lightweight, mucoadhesive, strong and soft constitution. Also, PVA-co-AAm synthesized hydrogels are able to absorb and release bromelain, indicating their potential use in a modified protein release system.
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The industry has been paying more attention to the quality of excipients since they play a fundamental role in the efficacy, safety, and acceptability of pharmaceutical products. However, in the case ...of topical products synthetic compounds have been a concern for consumers, since they can lead to sensitization reactions, disturbance of the microbiota, and impairment in the skin barrier function. Consequently, the pharmaceutical industry has been looking for safer, cheaper, more effective, and more eco-friendly alternatives, and so natural raw materials (or natural ingredients) are good candidates to meet this demand. This narrative review aims to present studies that use natural excipients and describe their advantages, disadvantages and overall performance. In topical formulations, natural ingredients can be found in the form of emulsifiers, emollients, preservatives, gelling agents, humectants, and permeation enhancers. The studies show that they fulfill their role in formulations, demonstrating rheological and stable characteristics, as well as not being toxic to skin cells and the microbiota. Moreover, many natural raw materials are biodegradable, being less harmful to the environment. More studies are still needed to effectively replace synthetic excipients with natural ones, while maintaining quality control. These raw materials present themselves as a potential alternative and there are vast resources still little explored, and those already used are highly effective and safe.
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•Excipients act in efficacy, safety and acceptability of pharmaceutical products.•There is a search for safer, more effective and eco-friendly-based excipients.•Different roles in formulation can be fulfilled with natural ingredients.•More studies are needed in order to replace synthetic excipients with natural ones.•Challenges of natural ingredients include their extraction process and price.
This study aims to evaluate properties as antioxidant activity, solar protection factor (SPF) and wound healing ability of jaboticaba peel's extract by in vitro methods. Jaboticaba peels were ...removed, dried, and then subjected to extraction method using ethanol. The extract was in vitro evaluated for preliminary studies about SPF, antioxidant activity and wound healing assay. Thereafter the extract was incorporated in an oil-in-water emulsion (phytocosmetic). The phytocosmetic was submitted to stability study and in vitro SPF evaluation. The extract's showed purple color with in vitro SPF of 24.86, stimulated keratinocytes migration after 9 h of exposition and presented antioxidant activity. The incorporation of the extract gave the phytocosmetic formulation a light pink shade with an in vitro SPF of 19.00. Under stress conditions, the formulation was stable, especially when stored in low temperatures. Jaboticaba peel extract promoted wound healing in vitro presenting SPF and antioxidant activity. Final phytocosmetic formulation was stable when stored protect from light and heat, indicating that Jaboticaba extract can be used to develop products to protect skin against aging and sun exposure.
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•Jabuticaba extract has potential to be used to products development.•Extract presented solar protection factor of 24.86 by in vitro test.•Emulsion with extract presented light pink color and SPF equal to 19.00•Formulation was stable especially when stored in refrigerator.
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