Effects of Fish Oil Supplementation on Oxidative Stress Biomarkers and Liver Damage in Hypercholesterolemic Rats.

Metabolic syndrome, especially its component related to dyslipidemia, is related to the development of nonalcoholic fatty liver disease (NAFLD), which is a disease with a significant global prevalence. Supplementation with omega-3 polyunsaturated fatty acids emerged as a complementary therapeutic possibility for dyslipidemia, but its benefits are questioned. This paper aims at evaluating the effects of fish oil supplementation in rats with hypercholesterolemia induced by hypercholesterolemic diet (HD). The study design is based on an experimental model in which the animals were randomly divided into 3 groups: G1 (standard commercial feed + saline solution); G2 (hypercholesterolemic diet + saline solution) and G3 (hypercholesterolemic diet + fish oil) over a period of 16 weeks. Metabolic control parameters and oxidative stress biomarkers were evaluated according to standardized methodologies. The G3 group showed significantly lower values of plasma concentrations of TG, and hepatic myeloperoxidase as well as higher erythrocyte superoxide dismutase activity (p < 0.05). Regarding histopathological analysis, there was lipid accumulation in the liver of animals from group G2; meanwhile, hepatocytes reorganization and expressive reduction of lipid vacuoles and hepatic TG content was observed in group G3. This study demonstrated how fish oil supplementation reduced the plasma concentration and hepatic content of triglycerides, as well as liver tissue damage in histopathological analysis.

Bio-Availability, Anticancer Potential, and Chemical Data of Lycopene: An Overview and Technological Prospecting.

The purpose of this review was to collect relevant chemical data about lycopene and its isomers, which can be extracted using different non-polar or polar aprotic solvents by SC-CO2 or biosynthesis as a friendly technique. Lycopene and other carotenoids can be identified and quantified by UV-Vis and HPLC using a C18 or C30 column, while their characterization is possible by UV-Vis, Fluorescence, FTIR, MS, NMR, and DSC assays. Among these techniques, the last four can compare lycopene isomers and identify cis or all-trans-lycopene. FTIR, MS, and NMR techniques are more suitable for the verification of the purity of lycopene extracts due to the signal complexity generated for each isomer, which enables identification by subtle differences. Additionally, some biological activities of lycopene isolated from red vegetables have already been confirmed, such as anti-inflammatory, antioxidant, and cytotoxic activity against cancer cells, probably by activating several pathways. The encapsulation of lycopene in nanoparticles demonstrated an improvement in oral delivery, and ex vivo assessments determined that these nanoparticles had better permeation and low cytotoxicity against human cells with enhanced permeation. These data suggest that lycopene has the potential to be applied in the food and pharmaceutical industries, as well as in cosmetic products.

Effects of ω-3 PUFA-Rich Oil Supplementation on Cardiovascular Morphology and Aortic Vascular Reactivity of Adult Male Rats Submitted to an Hypercholesterolemic Diet.

Atherosclerosis is a cardiovascular disease associated with abnormalities of vascular functions. The consumption of mono- and polyunsaturated fatty acids can be considered a strategy to reduce clinical events related to atherosclerosis. In the present study, we investigated the effects of supplementation with 310 mg of ω-3 PUFAs (2:1 eicosapentaenoic/docosahexaenoic acids) for 56 days on rats with hypercholesterolemia induced by a diet containing cholesterol (0.1%), cholic acid (0.5%), and egg yolk. Serum biochemical parameters were determined by the enzymatic colorimetric method. Assessment of vascular effects was performed by analysis of histological sections of the heart and aortic arch stained with hematoxylin and eosin and vascular reactivity of the aorta artery. We observed that treatment with ω-3 PUFAs did not promote alterations in lipid profile. On the other hand, we documented a favorable reduction in liver biomarkers, as well as contributions to the preservation of heart and aortic arch morphologies. Interestingly, the vascular reactivity of rat thoracic aortic preparations was improved after treatment with ω-3 PUFAs, with a decrease in hyperreactivity to phenylephrine and increased vasorelaxation promoted by acetylcholine. Our findings suggest that the supplementation of hypercholesterolemic rats with ω-3 PUFAs promoted improvement in liver and vascular endothelial function as well as preserving heart and aortic tissue, reinforcing the early health benefits of ω-3 PUFAs in the development of atherosclerotic plaque and further related events.

Acetylated cashew gum and fucan for incorporation of lycopene rich extract from red guava (Psidium guajava L.) in nanostructured systems: Antioxidant and antitumor capacity.

Industrial application of lycopene is limited due to its chemical instability and low bioavailability. This study proposes the development of fucan-coated acetylated cashew gum nanoparticles (NFGa) and acetylated cashew gum nanoparticles (NGa) for incorporation of the lycopene-rich extract from red guava (LEG). Size, polydispersity, zeta potential, nanoparticles concentration, encapsulation efficiency, transmission electron microscopy (TEM) and atomic force microscopy (AFM) were used to characterize nanoparticles. The antioxidant activity was determinated and cell viability was evaluated in the human breast cancer cells (MCF-7) and human keratinocytes (HaCaT) by MTT assay. The toxic effect was evaluated by hemolysis test and by Galleria mellonella model. NFGa showed higher stability than NGa, having a size of 162.10 ± 3.21 nm, polydispersity of 0.348 ± 0.019, zeta potential -30.70 ± 0.53 mV, concentration of 6.4 × 109 nanoparticles/mL and 60% LEG encapsulation. Microscopic analysis revealed a spherical and smooth shape of NFGa. NFGa showed antioxidant capacity by ABTS method and ORAC assay. The NFGa presented significant cytotoxicity against MCF-7 from the lowest concentration tested (6.25-200 µg/mL) and did not affect the cell viability of the HaCaT. NFGa showed non-toxic effect in the in vitro and in vivo models. Therefore, NFGa may have a promising application in LEG stabilization for antioxidant and antitumor purposes.

Anti-Leishmania activity of extracts from Piper cabralanum C.DC. (Piperaceae).

Species of Piperaceae are known by biological properties, including antiparasitic such as leishmanicidal, antimalarial and in the treatment of schistosomiasis. The aim of this work was to evaluate the antileishmania activity, cytotoxic effect, and macrophage activation patterns of the methanol (MeOH), hexane (HEX), dichloromethane (DCM) and ethyl acetate (EtOAc) extract fractions from the leaves of Piper cabralanum C.DC. The MeOH, HEX and DCM fractions inhibited Leishmanina amazonensis promastigote-like forms growth with a half maximal inhibitory concentration (IC50) of 144.54, 59.92, and 64.87 µg/mL, respectively. The EtOAc fraction did not show any relevant activity. The half maximal cytotoxic concentration (CC50) for macrophages were determined as 370.70, 83.99, 113.68 and 607 µg/mL for the MeOH, HEX and DCM fractions, respectively. The macrophage infectivity was concentration-dependent, especially for HEX and DCM. MeOH, HEX and DCM fractions showed activity against L. amazonensis with low cytotoxicity to murine macrophages and lowering infectivity by the parasite. Our results provide support for in vivo studies related to a potential application of P. cabralanum extract and fractions as a promising natural resource in the treatment of leishmaniasis.

Anti-proliferative profile of Anacardium occidentale polysaccharide and characterization by AFM.

This paper explores the application of cashew gum (CG) as an in vitro antiproliferative, firstly by isolating and characterizing the gum using elemental analysis, gel-permeation chromatography, nuclear magnetic resonance (NMR) and atomic force microscopy (AFM). The molar mass of isolated CG was in the order of 103-104 g/mol, with small protein traces present. Polymer characterization by NMR identified key signals correlating to galactose, glucose, rhamnose and acid-related groups. Three distinct conformational stages were observed by AFM. The impact of CG on cell morphology and viability with both tumor and non-tumor cell lines was studied by AFM and 3-(4,5-dimethyl-2-thiazole)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay respectively. Antiproliferative activity was confirmed for HCT116 (colorectal carcinoma), B16F10 (melanoma) and HL60 (promyelocytic leukemia) cancer cell lines. A change in cell morphology was demonstrated as an increased surface roughness for HL60. Considering that a CG does not exhibit cytotoxicity to non-tumor lines, it can be seen that the CG shows selectivity for tumor cells and can be a promising biomaterial for future studies.

Synergistic effects of in vitro combinations of piplartine, epiisopiloturine and praziquantel against Schistosoma mansoni.

Schistosomiasis is a world health problem, and praziquantel is the only drug currently used for the treatment. There is some evidence that extensive monotherapy of praziquantel may be leading to drug resistance in the parasite. In order to find alternative treatments, the effects of the combination of epiisopiloturine (EPI), piplartine (PPT) and praziquantel (PZQ) were evaluated. Similarity analysis of these compounds was performed using optimized molecular structures to compare the shape and the charge modeling of combinations between PZQ and EPI or PPT. Supported by this data, in vitro association of PZQ-PPT, PZQ-EPI, and EPI-PPT was carried out, and the activity of these combinations against Schistosoma mansoni was assessed. The results showed synergistic activity with a combination index (CI) of 0.42 for the treatment with PZQ-PPT. Both PZQ-EPI and EPI-PPT combinations also showed synergistic effects, with CI values of 0.86 and 0.61, respectively. Surface alterations in the tegument of adult schistosomes after the treatments were observed using laser confocal microscopy and scanning electron microscopy. Additionally, the association of EPI-PPT decreased the cytotoxicity when compared with both isolated compounds in three different lines of mammalian cells. Thus, synergistic combinations of PZQ-PPT, PZQ-EPI, and EPI-PPT create the possibility of reduced doses to be used against Schistosoma mansoni.

Thaulin-1: The first antimicrobial peptide isolated from the skin of a Patagonian frog Pleurodema thaul (Anura: Leptodactylidae: Leiuperinae) with activity against Escherichia coli.

Patagonia's biodiversity has been explored from many points of view, however, skin secretions of native amphibians have not been evaluated for antimicrobial peptide research until now. In this sense, Pleurodema thaul is the first amphibian specie to be studied from this large region of South America. Analysis of cDNA-encoding peptide in skin samples allowed identification of four new antimicrobial peptides. The predicted mature peptides were synthesized and all of them showed weak or null antimicrobial activity against Klebsiella pneumoniae, Staphylococcus aureus and Escherichia coli with the exception of thaulin-1, a cationic 26-residue linear, amphipathic, Gly- and Leu-rich peptide with moderate antimicrobial activity against E. coli (MIC of 24.7µM). AFM and SPR studies suggested a preferential interaction between these peptides and bacterial membranes. Cytotoxicity assays showed that thaulin peptides had minimal effects at MIC concentrations towards human and animal cells. These are the first peptides described for amphibians of the Pleurodema genus. These findings highlight the potential of the Patagonian region's unexplored biodiversity as a source for new molecule discovery.

Antibacterial, antibiofilm and cytotoxic activities of Terminalia fagifolia Mart. extract and fractions.

BACKGROUND: The methicillin resistance of bacteria from the genus Staphylococcus and its ability to form biofilms are important factors in pathogenesis of these microorganisms. Thus, the search for new antimicrobials agents, especially from plants, has been intensified. In this context, Terminalia species have been the subject of research for many pharmacological activities. In this study we evaluated the antibacterial, antibiofilm and cytotoxic activities of the ethanol extract (EtE) from Terminalia fagifolia stem bark as well as that of three fractions of the extract (AqF, HaF and WSF). METHODS: We determined the minimum inhibitory concentration (MIC) by microdilution in 96-well plates, where the strains were exposed to serial dilutions of the ethanol extract and fractions, ranging from 12.5 to 400 µg/mL. We then determined the minimum bactericidal concentration (MBC), seeding the inoculum (10 µL) with concentrations equal to or greater than the MIC in Mueller-Hinton agar. To test the antibiofilm activity biofilm formation was induced in the presence of concentrations equivalent to 1/2, 1/4 and 1/8 of the MIC extract or fraction tested. In addition, the effect of the EtE and the fractions on cell viability was tested by the MTT assay on human MCF-7 breast cancer and mouse fibroblast NIH/3T3. To obtain high-resolution images of the effect of the aqueous fraction on the bacterial morphology, atomic force microscopy (AFM) imaging of treated S. aureus cells was performed. RESULTS: We observed antibacterial activity of EtE and fractions with MICs ranging from 25-200 µg/mL and MBCs ranging from 200-400 µg/mL. Regarding antibiofilm activity, both the EtE as the AqF, HaF and WSF fractions showed significant inhibition of the biofilm formation, with inhibition of biofilms formation of over 80% for some strains. The EtE and fractions showed a moderate cytotoxicity in cell line NIH/3T3 viability and potential antitumoral activity on human breast cancer cell line MCF-7. The microscopic images obtained revealed morphological changes to the S. aureus ATCC 29213 surface caused by AqF, as well as significant size alterations. CONCLUSIONS: The results show potential antibacterial, antibiofilm and antitumoral activities of the ethanol extract and fractions of T. fagifolia.