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•Q. brasiliensis QB-80 saponins revealed chemical similarities to the commercial Q. saponaria barks-extracted saponin.•The QB-80 saponins were able to self-assembly with lipids in ...ISCOM-like nanoparticle named IMXQB-80.•Subcutaneous administration of QB-80 and IMXQB-80 induced high titres of anti-Zika virus with neutralizing antibodies.
Vaccine adjuvants are compounds that enhance/prolong the immune response to a co-administered antigen. Saponins have been widely used as adjuvants for many years in several vaccines – especially for intracellular pathogens – including the recent and somewhat revolutionary malaria and shingles vaccines. In view of the immunoadjuvant potential of Q. brasiliensis saponins, the present study aimed to characterize the QB-80 saponin-rich fraction and a nanoadjuvant prepared with QB-80 and lipids (IMXQB-80). In addition, the performance of such adjuvants was examined in experimental inactivated vaccines against Zika virus (ZIKV). Analysis of QB-80 by DI-ESI-ToF by negative ion electrospray revealed over 29 saponins that could be assigned to known structures existing in their congener Q. saponaria, including the well-studied QS-21 and QS-7. The QB-80 saponins were a micrOTOF able to self-assembly with lipids in ISCOM-like nanoparticles with diameters of approximately 43 nm, here named IMXQB-80. Toxicity assays revealed that QB-80 saponins did present some haemolytical and cytotoxic potentials; however, these were abrogated in IMXQB-80 nanoparticles. Regarding the adjuvant activity, QB-80 and IMXQB-80 significantly enhanced serum levels of anti-Zika virus IgG and subtypes (IgG1, IgG2b, IgG2c) as well as neutralized antibodies when compared to an unadjuvanted vaccine. Furthermore, the nanoadjuvant IMXQB-80 was as effective as QB-80 in stimulating immune responses, yet requiring fourfold less saponins to induce the equivalent stimuli, and with less toxicity. These findings reveal that the saponin fraction QB-80, and particularly the IMXQB-80 nanoadjuvant, are safe and capable of potentializing immune responses when used as adjuvants in experimental ZIKV vaccines.
Pests and diseases are responsible for most of the losses related to agricultural crops, either in the field or in storage. Moreover, due to indiscriminate use of synthetic pesticides over the years, ...several issues have come along, such as pest resistance and contamination of important planet sources, such as water, air and soil. Therefore, in order to improve efficiency of crop production and reduce food crisis in a sustainable manner, while preserving consumer’s health, plant-derived pesticides may be a green alternative to synthetic ones. They are cheap, biodegradable, ecofriendly and act by several mechanisms of action in a more specific way, suggesting that they are less of a hazard to humans and the environment. Natural plant products with bioactivity toward insects include several classes of molecules, for example: terpenes, flavonoids, alkaloids, polyphenols, cyanogenic glucosides, quinones, amides, aldehydes, thiophenes, amino acids, saccharides and polyketides (which is not an exhaustive list of insecticidal substances). In general, those compounds have important ecological activities in nature, such as: antifeedant, attractant, nematicide, fungicide, repellent, insecticide, insect growth regulator and allelopathic agents, acting as a promising source for novel pest control agents or biopesticides. However, several factors appear to limit their commercialization. In this critical review, a compilation of plant-derived metabolites, along with their corresponding toxicology and mechanisms of action, will be approached, as well as the different strategies developed in order to meet the required commercial standards through more efficient methods.
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•Caffeine intake does not alter working memory and general attention.•The placebo effect can influence the caffeine response due to the expectation.•Long-term exposure to caffeine may ...have an influence on the results.•Caffeine’s influence may be greater in activities involving attention and movement.
This study aimed to evaluate the effect of caffeine on cognitive parameters in premenstrual syndrome women of childbearing age undergoing caffeine withdrawal, observing the influence of cytochrome P450 enzyme isozyme 1A2 genotypes. This is a crossover study with 26 women (all participants) grouped according to genotype (17 AA and 9 AC/CC). The cognitive assessment was carried out before and after caffeine or placebo. A significant increase in attention was showed both after placebo and caffeine administration, however, no statistical difference was observed between caffeine and placebo groups. This occurred both for all participants and in the genotype groups. Working memory was improved for all participants, and in the AC/CC group after placebo ingestion; the same did not occur after caffeine intake. In the AA group, no significant changes were observed for placebo or caffeine. Caffeine does not promote effects on cognitive performance in premenstrual syndrome women after caffeine abstinence.
Lamiaceae is one of the largest families of angiosperms and is classified into 12 subfamilies that are composed of 295 genera and 7775 species. It presents a variety of secondary metabolites such as ...diterpenes that are commonly found in their species, and some of them are known to be chemotaxonomic markers. The aim of this work was to construct a database of diterpenes and to use it to perform a chemotaxonomic analysis among the subfamilies of Lamiaceae, using molecular descriptors and self-organizing maps (SOMs). The 4115 different diterpenes corresponding to 6386 botanical occurrences, which are distributed in eight subfamilies, 66 genera, 639 different species and 4880 geographical locations, were added to SistematX. Molecular descriptors of diterpenes and their respective botanical occurrences were used to generate the SOMs. In all obtained maps, a match rate higher than 80% was observed, demonstrating a separation of the Lamiaceae subfamilies, corroborating with the morphological and molecular data proposed by Li et al. Therefore, through this chemotaxonomic study, we can predict the localization of a diterpene in a subfamily and assist in the search for secondary metabolites with specific structural characteristics, such as compounds with potential biological activity.
Leishmaniasis is endemic in at least 98 countries. Due to the high toxicity and resistance associated with the drugs, we chose lignans as an alternative, due to their favorable properties of ...absorption, distribution, metabolism, excretion, and toxicity (ADMET). To investigate their leishmanicidal potential, the biological activities of a set of 160 lignans were predicted using predictive models that were built using data for
and
. A combined analysis, based on ligand and structure, and several other computational approaches were used. The results showed that the combined analysis was able to select 11 lignans with potential activity against
and 21 lignans against
, with multitargeting effects and low or no toxicity. Of these compounds, four were isolated from the species
(Nees) Lindau. All of the identified compounds were able to inhibit the growth of
promastigotes, with the most active compound, (
) epipinoresinol-4-
-β-d-glucopyranoside, presenting an IC
value of 5.39 µM and IC
value of 36.51 µM for
. Our findings indicated the potential of computer-aided drug design and development and demonstrated that lignans represent promising prototype compounds for the development of multitarget drugs against leishmaniasis.
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•Nutraceutical formulations with L. fermentum, quercetin, and resveratrol were prepared.•The formulations impacted the abundance of distinct intestinal bacterial populations.•The ...formulations had positive prebiotic indexes during colonic fermentation.•Tested formulations increased the antioxidant activities in colonic fermentation media.•Tested formulations remodeled metabolite production during colonic fermentation.
This study evaluated the impacts of different nutraceutical formulations combining Limosilactobacillus fermentum 296 (∼10 log CFU/mL), quercetin (QUE, 160 mg), and or resveratrol (RES, 150 mg) on the relative abundance of various intestinal bacterial populations, production of microbial metabolites, and antioxidant capacity during 48 h of in vitro colonic fermentation. The nutraceutical formulations increased the relative abundance of Lactobacillus spp./Enterococcus spp. and Bifidobacterium spp. and decreased the relative abundance of Bacteroides spp./Prevotella spp., Clostridium histolyticum, and E. rectale/C. coccoides during the colonic fermentation. Medium with the formulation containing L. fermentum, QUE, and RES had the highest prebiotic indexes, indicating synergistic or additive interaction between QUE and RES to modulate the intestinal microbiota. The nutraceutical formulations increased the production of bioactive metabolites and antioxidant capacity in the colonic fermentation media. The results indicate the capability of the tested nutraceutical formulations to beneficially modulate the composition and metabolite production of human intestinal microbiota and increase the antioxidant capacity in the intestinal environment.
(Cactaceae), popularly known as "palma" or "palma doce", is from Mexico, but it was widely introduced in Brazil through crops. It has been used as food and in traditional medicine and is a good ...source of phenolic compounds. In this study the phytochemical profile and gastroprotective activity of phenolic-rich extract of
in acute gastric lesion models induced by ethanol and indomethacin were evaluated. High-performance liquid chromatography coupled with mass spectrometry (HPLC/ESI/MS
) allowed the characterization of 12 compounds such as sugars, phenolics and flavonoids. Among polyphenols, the main peak was assigned to isorhamnetin-3-
-(2'',3''-
-di-rhamnose)-glucoside. The TPC and TFC in the dry extract were 67.85 mg of gallic acid equivalent per g/extract and 46.16 mg quercetin equivalent per g/extract, respectively. In the
MTT assay, the extract showed no cytotoxicity and suppressed ROS levels in LPS-treated RAW 264.7 cells. Preclinical models in rats showed that a dose of 100 mg kg
(
< 0.0001) in the ethanol model and doses of 100 mg kg
(
< 0.5) and 200 mg kg
(
< 0.01) in the indomethacin model reduced the gastric lesions. Also, the extract reduced the MPO, MDA, TNF-α and IL-1β levels and increased the GSH and IL-10 levels. The pre-treatment with the extract led to the upregulation of SOD and the downregulation of COX-2 by immunohistochemical analysis. It also showed a cytoprotective effect in the histopathological analysis and stimulated the restoration of the mucus content as observed in the periodic acid-Schiff analysis without modifying the pH, volume or total acidity of the gastric juice. Taken together,
extract can be applied as a novel gastroprotective ingredient for food or pharmaceutical products.
Bidens pilosa L. is a cosmopolitan annual herb, known for its traditional use in treating various diseases and thus much studied for the biological activity of its extracts, fractions and isolated ...compounds. Polyacetylenes and flavonoids, typical metabolite classes in the Bidens genus, predominate in the phytochemistry of B. pilosa. These classes of compounds have great taxonomic significance. In the Asteraceae family, the acetylene moiety is widely distributed in the Heliantheae tribe and some representatives, such as 1-phenylhepta-1,3,5-triyne, are noted for their biological activity and strong long-wave UV radiation absorbance. The flavonoids, specifically aurones and chalcones, have been reported as good sub-tribal level markers. Natural products from several other classes have also been isolated from different parts of B. pilosa. This review summarizes the available information on the 198 natural products isolated to date from B. pilosa.
Chagas disease, a neglected tropical disease, is endemic in 21 Latin American countries and particularly prevalent in Brazil. Chagas disease has drawn more attention in recent years due to its ...expansion into non‐endemic areas. The aim of this work was to computationally identify and experimentally validate the natural products from an Annonaceae family as antichagasic agents. Through the ligand‐based virtual screening, we identified 57 molecules with potential activity against the epimastigote form of T. cruzi. Then, 16 molecules were analyzed in the in vitro study, of which, six molecules displayed previously unknown antiepimastigote activity. We also evaluated these six molecules for trypanocidal activity. We observed that all six molecules have potential activity against the amastigote form, but no molecules were active against the trypomastigote form. 13‐Epicupressic acid seems to be the most promising, as it was predicted as an active compound in the in silico study against the amastigote form of T. cruzi, in addition to having in vitro activity against the epimastigote form.
Chagas disease is a neglected disease, considered endemic in 21 Latin American countries, especially in Brazil. Using a Annonaceae dataset obtained from SistematX, ligand‐based virtual screening was performed using two different algorithms. After the models have been built the predictions of the molecules were combined to select potential antiepimastigote molecules. The best molecules were evaluated in vitro. Molecules that obtained in vitro activity were evaluated in silico against the amastigote and trypomastigote forms in search of multitarget molecules.
Essential oils stand out among natural products for their complex composition, frequently described in the literature with a range of biological effects. This study evaluated the cytotoxic activity ...against several human cancer cell lines of essential oils extracted from the leaves of Lippia microphylla (EO‐LM) Cham. (Verbenaceae). The melanoma cell line SK‐MEL‐28 was the most sensitive to the EO‐LM, presenting an IC50 of 33.38±1.16 μg/mL. Afterward, the effects of EO‐LM on the cell cycle, induction of apoptosis, and production of reactive oxygen species (ROS) were evaluated. We stated a significant increase in the sub‐G1 population, indicating apoptosis, later confirmed by an increase of SK‐MEL‐28 cells labeled with Annexin V‐FITC and by the formation of apoptotic bodies and membrane blebs, observed by confocal microscopy. Additionally, EO‐LM reduced the production of ROS, indicating antioxidant activity. Therefore, EO‐LM exhibits anti‐melanoma activity in vitro, suggesting its potential as an anticancer agent.
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