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1.
Molecules ; 29(16)2024 Aug 15.
Article in English | MEDLINE | ID: mdl-39202939

ABSTRACT

Marine organisms represent a potential source of secondary metabolites with various therapeutic properties. However, the pharmaceutical industry still needs to explore the algological resource. The species Caulerpa lamouroux Forssk presents confirmed biological activities associated with its major compound caulerpin, such as antinociceptive, spasmolytic, antiviral, antimicrobial, insecticidal, and cytotoxic. Considering that caulerpin is still limited, such as low solubility or chemical instability, it was subjected to a structural modifications test to establish which molecular regions could accept structural modification and to elucidate the cytotoxic bioactive structure in Vero cells (African green monkey kidney cells, Cercopithecus aethiops; ATCC, Manassas, VA, USA) and antiviral to Herpes simplex virus type 1. Substitution reactions in the N-indolic position with mono- and di-substituted alkyl, benzyl, allyl, propargyl, and ethyl acetate groups were performed, in addition to conversion to their acidic derivatives. The obtained analogs were submitted to cytotoxicity and antiviral activity screening against Herpes simplex virus type 1 by the tetrazolium microculture method. From the semi-synthesis, 14 analogs were obtained, and 12 are new. The cytotoxicity assay showed that caulerpin acid and N-ethyl-substituted acid presented cytotoxic concentrations referring to 50% of the maximum effect of 1035.0 µM and 1004.0 µM, respectively, values significantly higher than caulerpin. The antiviral screening of the analogs revealed that the N-substituted acids with methyl and ethyl groups inhibited Herpes simplex virus type 1-induced cytotoxicity by levels similar to the positive control acyclovir.


Subject(s)
Antiviral Agents , Herpesvirus 1, Human , Antiviral Agents/pharmacology , Antiviral Agents/chemistry , Chlorocebus aethiops , Herpesvirus 1, Human/drug effects , Vero Cells , Animals , Structure-Activity Relationship , Molecular Structure , Cell Survival/drug effects
2.
Food Microbiol ; 123: 104596, 2024 Oct.
Article in English | MEDLINE | ID: mdl-39038898

ABSTRACT

This study evaluated the use of acerola (Malpighia glabra L., CACE), cashew (Anacardium occidentale L., CCAS), and guava (Psidium guayaba L., CGUA) fruit processing coproducts as substrates to promote the growth, metabolite production, and maintenance of the viability/metabolic activity of the probiotics Lactobacillus acidophilus LA-05 and Lacticaseibacillus paracasei L-10 during cultivation, freeze-drying, storage, and exposure to simulated gastrointestinal digestion. Probiotic lactobacilli presented high viable counts (≥8.8 log colony-forming units (CFU)/mL) and a short lag phase during 24 h of cultivation in CACE, CCAS, and CGUA. Cultivation of probiotic lactobacilli in fruit coproducts promoted sugar consumption, medium acidification, and production of organic acids over time, besides increasing the of several phenolic compounds and antioxidant activity. Probiotic lactobacilli cultivated in fruit coproducts had increased survival percentages after freeze-drying and during 120 days of refrigerated storage. Moreover, probiotic lactobacilli cultivated and freeze-dried in fruit coproducts had larger subpopulations of live and metabolically active cells when exposed to simulated gastrointestinal digestion. The results showed that fruit coproducts not only improved the growth and helped to maintain the viability and metabolic activity of probiotic strains but also enriched the final fermented products with bioactive compounds, being an innovative circular strategy for producing high-quality probiotic cultures.


Subject(s)
Fruit , Probiotics , Probiotics/metabolism , Fruit/microbiology , Lactobacillus acidophilus/growth & development , Lactobacillus acidophilus/metabolism , Lactobacillus acidophilus/physiology , Anacardium/microbiology , Anacardium/growth & development , Psidium/growth & development , Psidium/microbiology , Malpighiaceae/growth & development , Malpighiaceae/microbiology , Freeze Drying , Microbial Viability , Lacticaseibacillus paracasei/growth & development , Lacticaseibacillus paracasei/metabolism , Lacticaseibacillus paracasei/physiology , Fermentation , Food Handling/methods
3.
Pharmaceutics ; 16(7)2024 Jul 09.
Article in English | MEDLINE | ID: mdl-39065609

ABSTRACT

In 2019, the emergence of the seventh known coronavirus to cause severe illness in humans triggered a global effort towards the development of new drugs and vaccines for the SARS-CoV-2 virus. These efforts are still ongoing in 2024, including the present work where we conducted a ligand-based virtual screening of terpenes with potential anti-SARS-CoV-2 activity. We constructed a Quantitative Structure-Activity Relationship (QSAR) model from compounds with known activity against SARS-CoV-2 with a model accuracy of 0.71. We utilized this model to predict the activity of a series of 217 terpenes isolated from the Fabaceae family. Four compounds, predominantly triterpenoids from the lupane series, were subjected to an in vitro phenotypic screening in Vero CCL-81 cells to assess their inhibitory activity against SARS-CoV-2. The compounds which showed high rates of SARS-CoV-2 inhibition along with substantial cell viability underwent molecular docking at the SARS-CoV-2 main protease, papain-like protease, spike protein and RNA-dependent RNA polymerase. Overall, virtual screening through our QSAR model successfully identified compounds with the highest probability of activity, as validated using the in vitro study. This confirms the potential of the identified triterpenoids as promising candidates for anti-SARS-CoV-2 therapeutics.

4.
Clin Nutr ESPEN ; 61: 158-167, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38777429

ABSTRACT

BACKGROUND: Diabetic retinopathy (DR) and limb amputation are frequent complications of diabetes that cannot always be explained by blood glucose control. Metabolomics is a science that is currently being explored in the search for biomarkers or profiles that identify clinical conditions of interest. OBJECTIVE: This study aimed to analyze, using a metabolomic approach, peripheral blood samples from type 2 diabetes mellitus (DM2) individuals, compared with those with diabetic retinopathy and limb amputation. METHODS: The sample consisted of 128 participants, divided into groups: control, DM2 without DR (DM2), non-proliferative DR (DRNP), proliferative DR (DRP), and DM2 amputated (AMP). Metabolites from blood plasma were classified by spectra using nuclear magnetic resonance (NMR), and the metabolic routes of each group using metaboanalyst. RESULTS: We identified that the metabolism of phenylalanine, tyrosine, and tryptophan was discriminant for the DRP group. Histidine biosynthesis, on the other hand, was statistically associated with the AMP group. The results of this work consolidate metabolites such as glutamine and citrulline as discriminating for DRP, and the branched-chain amino acids as important for DR. CONCLUSIONS: The results demonstrate the relationship between the metabolism of ketone bodies, with acetoacetate metabolite being discriminating for the DRP group and histidine being a significant metabolite in the AMP group, when compared to the DM2 group.


Subject(s)
Amputation, Surgical , Biomarkers , Diabetes Mellitus, Type 2 , Diabetic Retinopathy , Metabolomics , Humans , Diabetes Mellitus, Type 2/blood , Diabetic Retinopathy/blood , Male , Female , Middle Aged , Aged , Biomarkers/blood , Magnetic Resonance Spectroscopy
5.
Probiotics Antimicrob Proteins ; 16(1): 308-319, 2024 Feb.
Article in English | MEDLINE | ID: mdl-36708461

ABSTRACT

This study evaluated the effects of simulated gastrointestinal conditions (SGIC) on combined potentially probiotic Limosilactobacillus fermentum 296 (~ 10 log CFU/mL), quercetin (QUE, 160 mg), and/or resveratrol (RES, 150 mg) as the bioactive components of novel nutraceuticals. Four different nutraceuticals were evaluated during exposure to SGIC and analyzed the plate counts and physiological status of L. fermentum 296, contents and bioaccessibility of QUE and RES, and antioxidant capacity. Nutraceuticals with QUE and RES had the highest plate counts (4.94 ± 0.32 log CFU/mL) and sizes of live cell subpopulations (28.40 ± 0.28%) of L. fermentum 296 after SGIC exposure. An index of injured cells (Gmean index, arbitrary unit defined as above 0.5) indicated that part of L. fermentum 296 cells could be entered the viable but nonculturable state when the nutraceuticals were exposed to gastric and intestinal conditions while maintaining vitality. The nutraceuticals maintained high contents (QUE ~ 29.17 ± 0.62 and RES ~ 23.05 mg/100 g) and bioaccessibility (QUE ~ 41.0 ± 0.09% and RES ~ 67.4 ± 0.17%) of QUE and RES, as well as high antioxidant capacity (ABTS assay ~ 88.18 ± 1.16% and DPPH assay 75.54 ± 0.65%) during SGIC exposure, which could be linked to the protective effects on L. fermentum 296 cells. The developed nutraceuticals could cross along the gastrointestinal tract with high concentrations of functioning potentially probiotic cells and bioavailable phenolic compounds to exert their beneficial impacts on consumer health, being an innovative strategy for the co-ingestion of these bioactive components.


Subject(s)
Gastrointestinal Diseases , Limosilactobacillus fermentum , Probiotics , Humans , Quercetin , Resveratrol , Antioxidants , Probiotics/pharmacology
6.
Food Res Int ; 174(Pt 2): 113658, 2023 Dec.
Article in English | MEDLINE | ID: mdl-37981375

ABSTRACT

This study investigated the potential impacts of the flour from Cereus jamacaru cactus cladodes (CJF), a cactus native to the Brazilian Caatinga biome, on the growth and metabolism of different potentially probiotic strains, as well as on the abundance of selected intestinal bacterial populations and microbial metabolic activity during in vitro colonic fermentation with a pooled human fecal inoculum. Cultivation of the probiotics in a medium with C. jamacaru cladodes flour (20 g/L) resulted in viable cell counts of up to 9.8 log CFU/mL, positive prebiotic activity scores (0.73-0.91), decreased pH and sugar contents, and increased lactic, acetic, and propionic acid production over time, indicating enhanced probiotic growth and metabolic activity. CJF overall increased the relative abundance of Lactobacillus spp./Enterococcus spp. (2.12-3.29%) and Bifidobacterium spp. (4.08-4.32%) and decreased the relative abundance of Bacteroides spp./Prevotella spp. (8.35-6.81%), Clostridium histolyticum (6.91-3.59%), and Eubacterium rectale/Clostridium coccoides (7.70-3.95%) during 48 h of an in vitro colonic fermentation using a pooled human fecal inoculum. CJF stimulated the microbial metabolic activity, with decreased pH, sugar consumption, lactic and short-chain fatty acid production, alterations in overall metabolic profiling and phenolic compound contents, and maintenance of high antioxidant capacity during colonic fermentation. These results show that CJF stimulated the growth and metabolic activity of distinct potential probiotics, increased the relative abundance of beneficial intestinal bacterial groups, and stimulated microbial metabolism during in vitro colonic fermentation. Further studies using advanced molecular technologies and in vivo experimental models could forward the investigation of the potential prebiotic properties of CJF.


Subject(s)
Cactaceae , Gastrointestinal Microbiome , Humans , Flour , Fermentation , Metabolomics
7.
Nat Prod Res ; : 1-7, 2023 Nov 22.
Article in English | MEDLINE | ID: mdl-37991440

ABSTRACT

Pink pepper (Schinus terebinthifolius Raddi) is a native species native from Central and South America that produces an essential oil (EOpp) with promising applications. This work aimed to investigate the chemical composition and cytotoxic activity of EOpp extracted from unripe (U-EOpp) and ripe (R-EOpp) pink pepper fruits. U-EOpp and R-EOpp were extracted using the hydrodistillation technique and analysed using NMR and GC-MS. U-EOpp and R-EOpp cytotoxic activity was assessed using HL-60 (acute promyelocytic leukemia) and SK-MEL-28 (malignant melanoma) cell lines by MTT assay. Results showed that α-pinene (29.16%), dl-Limonene (20.65%), and ρ-cymene (15.86%) were U-EOpp major components. In addition, l-phellandrene (38.91%), Sylvestrene (23.02%), and α-pinene (21.62%) were R-EOpp major components. U-EOpp showed cytotoxic activity at 37.5 and 18.7 µg/mL for SK-MEL-28 and HL-60, respectively. R-EOpp showed cytotoxic activity for HL-60 at 100 µg/mL. Therefore, EOpp may represent a remarkable source of active natural compounds used in traditional Brazilian medicine.

8.
Pharmaceuticals (Basel) ; 16(11)2023 Nov 02.
Article in English | MEDLINE | ID: mdl-38004419

ABSTRACT

The characterization and cytotoxicity of the essential oil from Conyza bonariensis (L.) aerial parts (CBEO) were previously conducted. The major compound was (Z)-2-lachnophyllum ester (EZ), and CBEO exhibited significant ROS-dependent cytotoxicity in the melanoma cell line SK-MEL-28. Herein, we employed the Molegro Virtual Docker v.6.0.1 software to investigate the interactions between the EZ and Mitogen-Activated Protein Kinases (MAPKs), the Nuclear Factor kappa B (NF-κB), and the Protein Kinase B (PKB/AKT). Additionally, in vitro assays were performed in SK-MEL-28 cells to assess the effect of CBEO on the cell cycle, apoptosis, and these signaling pathways by flow cytometry and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay using MAPKs inhibitors. CBEO induced a significant increase in the sub-G1 peak, as well as biochemical and morphological changes characteristic of apoptosis. The in-silico results indicated that EZ interacts with Extracellular Signal-Regulated Kinase 1 (ERK1), c-Jun N-terminal Kinase 1 (JNK1), p38α MAPK, NF-κB, and PKB/AKT. Moreover, CBEO modulated the ERK1/2, JNK, p38 MAPK, NF-κB, and PKB/AKT activities in SK-MEL-28 cells. Furthermore, CBEO's cytotoxicity against SK-MEL-28 cells was significantly altered in the presence of MAPKs inhibitors. These findings support the in vitro antimelanoma effect of CBEO through apoptosis induction, and the modulation of ERK, JNK, p38 MAPK, NF-κB, and PKB/AKT activities.

9.
Physiol Behav ; 272: 114360, 2023 Dec 01.
Article in English | MEDLINE | ID: mdl-37778453

ABSTRACT

The aim of this research was to evaluate the effect of cactus flour on the anxious-like behavior and cerebral lipid peroxidation in elderly rats (18 months of life). The rats were divided into four groups (n=10). control (CG) - received the AIN-93M ration. P5%. P10% and P15%. treated with the AIN-93M ration with the addition of 5, 10 and 15% of cactus flour respectively. In the elevated plus maze (EPM) groups P5%, P10% and P15% remained longer in the open arms. P15% remained longer in this region and less time in the closed arms. No significant differences were observed between the groups regarding the time the rats remained in the center of the apparatus. P5%. P10% and P15% performed a greater number of head dips. Regarding the open field animals P5%. P10% and P15% performed a greater number of rearing and stayed for a longer time in the center of the apparatus with P15% being the group that remained for the longest time when compared to the other groups. There was no difference in locomotion and grooming. As for the light-dark box. P15% spent more time in the light part. less time in the dark part and performed a smaller number of transitions. P5%. P10% and P15% had the lowest concentrations of brain lipid peroxidation. Our data demonstrated that consumption of cactus flour by rats promoted anxiolytic effects and minimized brain lipid peroxidation in aging. Given the above, it can be deduced that cactus pear can contribute to the prevention and/or treatment of anxiety in the aging phase.Due to its concentrations of mono and polyunsaturated fatty acids, soluble fibers and antioxidant contents such as vitamin E and selenium.


Subject(s)
Opuntia , Humans , Rats , Animals , Rats, Wistar , Lipid Peroxidation , Flour , Brain , Anxiety/drug therapy
10.
Biomolecules ; 13(10)2023 09 24.
Article in English | MEDLINE | ID: mdl-37892120

ABSTRACT

The essential oil from Conyza bonariensis (Asteraceae) aerial parts (CBEO) was extracted by hydrodistillation in a Clevenger-type apparatus and was characterized by gas chromatography-mass spectrometry. The antitumor potential was evaluated against human tumor cell lines (melanoma, cervical, colorectal, and leukemias), as well as non-tumor keratinocyte lines using the MTT assay. The effect of CBEO on the production of Reactive Oxygen Species (ROS) was evaluated by DCFH-DA assay, and a protection assay using the antioxidant N-acetyl-L-cysteine (NAC) was also performed. Moreover, the CBEO toxicity in the zebrafish model was assessed. The majority of the CBEO compound was (Z)-2-lachnophyllum ester (57.24%). The CBEO exhibited selectivity towards SK-MEL-28 melanoma cells (half maximal inhibitory concentration, IC50 = 18.65 ± 1.16 µg/mL), and induced a significant increase in ROS production. In addition, the CBEO's cytotoxicity against SK-MEL-28 cells was reduced after pretreatment with NAC. Furthermore, after 96 h of exposure, 1.5 µg/mL CBEO induced death of all zebrafish embryos. Non-lethal effects were observed after exposure to 0.50-1.25 µg/mL CBEO. Additionally, significant alterations in the activity of enzymes associated with oxidative stress in zebrafish larvae were observed. These results provide evidence that CBEO has a significant in vitro antimelanoma effect by increasing ROS production and moderate embryotoxicity in zebrafish.


Subject(s)
Asteraceae , Conyza , Melanoma , Oils, Volatile , Animals , Humans , Conyza/chemistry , Zebrafish , Reactive Oxygen Species , Oils, Volatile/pharmacology , Oils, Volatile/chemistry
11.
Article in English | MEDLINE | ID: mdl-37561381

ABSTRACT

This study evaluated the impacts of novel nutraceuticals formulated with freeze-dried jabuticaba peel (FJP) and three potentially probiotic Limosilactobacillus fermentum strains on the abundance of bacterial groups forming the human intestinal microbiota, metabolite production, and antioxidant capacity during in vitro colonic fermentation. The nutraceuticals had high viable counts of L. fermentum after freeze-drying (≥ 9.57 ± 0.09 log CFU/g). The nutraceuticals increased the abundance of Lactobacillus ssp./Enterococcus spp. (2.46-3.94%), Bifidobacterium spp. (2.28-3.02%), and Ruminococcus albus/R. flavefaciens (0.63-4.03%), while decreasing the abundance of Bacteroides spp./Prevotella spp. (3.91-2.02%), Clostridium histolyticum (1.69-0.40%), and Eubacterium rectale/C. coccoides (3.32-1.08%), which were linked to positive prebiotic indices (> 1.75). The nutraceuticals reduced the pH and increased the sugar consumption, short-chain fatty acid production, phenolic acid content, and antioxidant capacity, besides altering the metabolic profile during colonic fermentation. The combination of FJP and probiotic L. fermentum is a promising strategy to produce nutraceuticals targeting intestinal microbiota.

12.
Article in English | MEDLINE | ID: mdl-36417111

ABSTRACT

This study evaluated the stability of a novel nutraceutical formulation composed of the probiotic Limosilactobacillus fermentum 296, quercetin (QUE), and resveratrol (RES) (LFQR) under different storage conditions. The effects of different relative humidities (RH; 11, 22, and 33%) and storage temperatures (refrigeration temperature -4 °C and room temperature -25 °C) on the stability of LFQR were evaluated through the determination of thermal stability, viable cell counts, bacterial physiological status, antioxidant capacity, and contents of QUE and RES during long-term storage. RH did not affect endothermic reactions and mass reduction in LFQR. After a 15-day-humidification period, L. fermentum 296 had higher viable cell counts in LFQR under refrigeration temperature storage when compared to room temperature storage regardless of the RH. The physiological status of L. fermentum 296 in LFQR was overall similar during 90 days of storage (11% RH) under refrigeration and room temperature. L. fermentum 296 had the highest viable cell counts (> 6 log CFU/g) in LFQR up to day 90 of refrigeration storage (11% RH). LFQR kept high contents of QUE and RES and maintained antioxidant capacity during 90 days of storage under refrigeration and room temperature. The results showed that the higher stability and functionality of LFQR during long-term storage should be guaranteed under 11% RH and refrigeration temperature.

13.
Bionanoscience ; 12(4): 1166-1171, 2022.
Article in English | MEDLINE | ID: mdl-35967762

ABSTRACT

Quillaja saponins have an intrinsic capacity to interact with membrane lipids that self-assembles in nanoparticles (immunostimulating complexes or ISCOM-matrices) with outstanding immunoadjuvant activity and low toxicity profile. However, the expensive and laborious purification processes applied to purify Quillaja saponins used to assemble ISCOM-matrices show an important drawback in the large-scale use of this vaccine adjuvant. Thus, in this study, we describe a protocol to appropriately formulate ISCOM-matrices using the raw aqueous extract (AE) of Quillaja lancifolia leaves. In the presence of lipids, AE was able to self-assemble in nanostructures that resembles immunostimulating complexes (ISCOM). These negatively charged nanoparticles of approximately 40 nm were characterized by transmission electron microscopy and dynamic light scattering. In addition, well-known saponins with remarkable immunoadjuvant activity, as QS-21, were detected into nanoparticles. Thus, the easier, robust, cheaper, and environmentally friendly method developed here may be an alternative to the classical methods for ISCOM-matrices production that use high-purified saponins.

14.
Nutrients ; 14(10)2022 May 18.
Article in English | MEDLINE | ID: mdl-35631239

ABSTRACT

Background: This study assessed the effects of Baru (Dipteryx alata Vog.) almond oil supplementation on vascular function, platelet aggregation, and thrombus formation in aorta arteries of Wistar rats. Methods: Male Wistar rats were allocated into three groups. The control group (n = 6), a Baru group receiving Baru almond oil at 7.2 mL/kg/day (BG 7.2 mL/kg, n = 6), and (iii) a Baru group receiving Baru almond oil at 14.4 mL/kg/day (BG 14.4 mL/kg, n = 6). Baru oil was administered for ten days. Platelet aggregation, thrombus formation, vascular function, and reactive oxygen species production were evaluated at the end of treatment. Results: Baru oil supplementation reduced platelet aggregation (p < 0.05) and the production of the superoxide anion radical in platelets (p < 0.05). Additionally, Baru oil supplementation exerted an antithrombotic effect (p < 0.05) and improved the vascular function of aorta arteries (p < 0.05). Conclusion: The findings showed that Baru oil reduced platelet aggregation, reactive oxygen species production, and improved vascular function, suggesting it to be a functional oil with great potential to act as a novel product for preventing and treating cardiovascular disease.


Subject(s)
Dipteryx , Thrombosis , Animals , Aorta , Arteries , Male , Plant Oils , Platelet Aggregation , Rats , Rats, Wistar , Reactive Oxygen Species/pharmacology , Thrombosis/drug therapy
15.
Food Chem ; 342: 128264, 2021 Apr 16.
Article in English | MEDLINE | ID: mdl-33041168

ABSTRACT

This study developed and carried out an in vitro evaluation of nutraceutical formulations composed of potentially probiotic Limosilactobacillus fermentum (L. fermentum 139, L. fermentum 263 or L. fermentum 296), quercetin and/or resveratrol. L. fermentum strains had counts of >9 log CFU/g and contents of QUE and RES of >200 µg/mg in formulations after freeze-drying. Formulations with QUE and RES protected L. fermentum during exposure to in vitro acidic stomach conditions. L. fermentum strains had counts of >6 log CFU/g on day 60 and/or 90 of refrigeration storage. Contents of QUE (>29%) and RES (>50%) in formulations were potentially bioaccessible. Higher counts of L. fermentum and higher contents of QUE and RES were found in formulations stored under refrigerated rather than under room temperature. All nutraceutical formulations had antioxidant properties. Combinations of probiotic L. fermentum and QUE and/or RES should be an innovative strategy to develop added-value nutraceutical formulations.


Subject(s)
Dietary Supplements/analysis , Dietary Supplements/microbiology , Limosilactobacillus fermentum , Quercetin/chemistry , Resveratrol/chemistry , Drug Compounding , Freeze Drying , Probiotics/chemistry
16.
Vaccine ; 39(3): 571-579, 2021 01 15.
Article in English | MEDLINE | ID: mdl-33339669

ABSTRACT

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.


Subject(s)
Saponins , Zika Virus Infection , Zika Virus , Adjuvants, Immunologic , Animals , Immunity , Mice , Quillaja , Quillaja Saponins , Zika Virus Infection/prevention & control
17.
Toxins (Basel) ; 13(1)2020 Dec 23.
Article in English | MEDLINE | ID: mdl-33374495

ABSTRACT

This study evaluated the efficacy of potentially probiotic fruit-derived Lactobacillus isolates, namely, L. paracasei 108, L. plantarum 49, and L. fermentum 111, to remove aflatoxin M1 (AFM1) from a phosphate buffer solution (PBS; spiked with 0.15 µg/mL AFM1). The efficacy of examined isolates (approximately 109 cfu/mL) as viable and non-viable cells (heat-killed; 100 °C, 1 h) to remove AFM1 was measured after 1 and 24 h at 37 °C. The recovery of AFM1 bound to bacterial cells after washing with PBS was also evaluated. Levels of AFM1 in PBS were measured with high-performance liquid chromatography. Viable and non-viable cells of all examined isolates were capable of removing AFM1 in PBS with removal percentage values in the range of 73.9-80.0% and 72.9-78.7%, respectively. Viable and non-viable cells of all examined Lactobacillus isolates had similar abilities to remove AFM1. Only L. paracasei 108 showed higher values of AFM1 removal after 24 h for both viable and non-viable cells. Percentage values of recovered AFM1 from viable and non-viable cells after washing were in the range of 13.4-60.6% and 10.9-47.9%, respectively. L. plantarum 49 showed the highest AFM1 retention capacity after washing. L. paracasei 108, L. plantarum 49, and L. fermentum 111 could have potential application to reduce AFM1 to safe levels in foods and feeds. The cell viability of examined isolates was not a pre-requisite for their capacity to remove and retain AFM1.


Subject(s)
Aflatoxin M1/chemistry , Lacticaseibacillus paracasei/physiology , Lactobacillus plantarum/physiology , Limosilactobacillus fermentum/physiology , Food Contamination , Fruit/microbiology , Microbial Viability , Probiotics
18.
Molecules ; 25(23)2020 Nov 26.
Article in English | MEDLINE | ID: mdl-33256223

ABSTRACT

This study evaluated the effect of Mucuna pruriens (MP) administration on neuroinflammation and behavioral and murinometric parameters in obese rats. Proximate composition, oligosaccharide and phenolic compound profile of MP were determined. Wistar adult male rats were randomized into healthy (HG) and obese group (OG). The HG consumed a control chow diet while OG consumed a cafeteria diet for eight weeks. Then, they were subdivided into: Healthy (HG); Healthy with MP administration (HGMP); Obese (OG); Obese with MP administration (OGMP), with the consumption of the respective diets remaining for another eight weeks, in addition to gavage with MP extract to supplemented groups (750 mg/kg weight). MP presented a composition rich in proteins and phenolic compounds, especially catechin, in addition to 1-kestose and levodopa. Supplementation reduced food intake, body weight, and thoracic and abdominal circumferences in obese rats. MP showed anxiolytic and antidepressant effects and reduced morphological damage and expression of interleukin 6 in the hippocampus of obese rats. MP treatment showed satietogenic, slimming, anxiolytic and antidepressant effects, besides to minimizing hippocampal neuroinflammation in obese rats. Our results demonstrated the potential anti-obesity of MP which are probably related to the high content of bioactive compounds present in this plant extract.


Subject(s)
Anti-Anxiety Agents/pharmacology , Antidepressive Agents/chemistry , Antidepressive Agents/pharmacology , Mucuna/chemistry , Plant Extracts/pharmacology , Animals , Anti-Anxiety Agents/administration & dosage , Anti-Anxiety Agents/chemistry , Antidepressive Agents/administration & dosage , Behavior, Animal/drug effects , Disease Models, Animal , Histocytochemistry , Immunohistochemistry/methods , Obesity , Phytochemicals/chemistry , Phytochemicals/pharmacology , Phytotherapy , Plant Extracts/administration & dosage , Plant Extracts/chemistry , Rats
19.
Fitoterapia ; 145: 104632, 2020 Sep.
Article in English | MEDLINE | ID: mdl-32446709

ABSTRACT

This current study presents the phytochemical analysis of Croton velutinus, describing phenylpropanoids obtained from this species. The fractionation of the roots hexane extract led to the isolation of four new phenylpropanoids derivatives, velutines A-D (1-4) and three known (5-7). Their structures were established based on spectroscopic (1D-2D NMR; HRMS and IR) analysis. Cytotoxic, trypanocidal and anti-inflammatory activities of compounds 1-7 were evaluated. Only compounds 2 and 5 showed cytotoxic activity against cancer cell lines (B16F10, HL-60, HCT116, MCF-7 and HepG2), with IC50 values ranging from 6.8 to 18.3 µM and 11.1 to 18.3 µM, respectively. Compounds 2 and 5 also showed trypanocidal activity against bloodstream trypomastigotes with EC50 values of 9.0 and 9.58 µM, respectively. Finally, the anti-inflammatory potential of these compounds was evaluated on cultures of activated macrophages. All compounds exhibited concentration-dependent suppressive activity on the production of nitrite and IL-1ß by macrophages stimulated with LPS and IFN-γ. These results indicate phenylpropanoids esters (2 and 5) from C. velutinus as promising cytotoxic, trypanocidal and anti-inflammatory candidates that warrants further studies.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Antiprotozoal Agents/pharmacology , Croton/chemistry , Phenylpropionates/pharmacology , Animals , Anti-Inflammatory Agents/isolation & purification , Antineoplastic Agents, Phytogenic/isolation & purification , Antiprotozoal Agents/isolation & purification , Brazil , Cell Line, Tumor , Humans , Macrophages/chemistry , Mice , Molecular Structure , Phenylpropionates/isolation & purification , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Plant Roots/chemistry , Trypanosoma cruzi/drug effects
20.
PLoS One ; 14(10): e0224575, 2019.
Article in English | MEDLINE | ID: mdl-31661523

ABSTRACT

Limonoids, quinolone alkaloids and chromones have been reported as constituents of Dictyoloma vandellianum Adr. Juss. (Rutaceae). Although those compounds are known for their biological activities, only the anti-inflammatory activity of chromones isolated from the underground parts has been evaluated. There are no studies of the pharmacological properties of the aerial parts of D. vandellianum. The present study was carried out to determine the phytochemical profile and antinociceptive activity of the methanol extract, fractions and isolated compounds of leaves of D. vandellianum. The phytochemical profile was performed by HLPC-DAD-ESIMSn and pure substances obtained were characterized by MS and NMR spectroscopy. The antinociceptive activity was assessed using the formalin assay in mice, and the motor function in the rotarod test. ME and all the fractions obtained from ME produced antinociceptive effects. Among them, the ethyl ether fraction was the most active. Data from HPLC-DAD-ESIMSn showed that the ethyl ether fraction presented 42 compounds. The major compounds isolated from this fraction-gallic acid, methyl gallate and 1,2,6-tri-O-galloyl-ß-d-glucopyranose-were tested and produced antinociceptive effects. Gallic acid, methyl gallate and 1,2,6-tri-O-galloyl-ß-d-glucopyranose at antinociceptive doses did not affect the motor performance in mice in the rotarod test. This work is the first report of the occurrence of gallotanins in D. vandellianum. In addition, the pharmacological study showed that D. vandellianum leaves present antinociceptive activity, probably induced by gallic acid, methyl gallate and 1,2,6-tri-O-galloyl-ß-d-glucopyranose.


Subject(s)
Analgesics/chemistry , Plant Leaves/chemistry , Rutaceae/chemistry , Alkaloids/chemistry , Animals , Chromatography, High Pressure Liquid/methods , Chromatography, Liquid/methods , Chromones/analysis , Gas Chromatography-Mass Spectrometry/methods , Limonins/analysis , Male , Methanol/analysis , Mice , Phytochemicals/analysis , Plant Extracts/pharmacology , Plant Leaves/metabolism , Rutaceae/genetics
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