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- Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activityPublication . Leimann, Fernanda Vitória; Souza, Luma Borges de; Oliveira, Byanca Pereira Moreira de; Rossi, Bruna Franzon; Silva, Patricia Sabino da; Shiraishi, Carlos Seiti Hurtado; Kaplum, Vanessa; Abreu, Rui M.V.; Pereira, Carla; Barros, Lillian; Peron, Ana Paula; Ineu, Rafael Porto; Oechsler, Bruno Francisco; Sayer, Claudia; Araujo, Pedro Henrique Hermes de; Gonçalves, Odinei Hess; Shiraishi, Carlos S.H.Researchers have concentrated efforts in the search for natural-based reversible inhibitors for cholinesterase enzymes as they may play a key role in the treatment of degenerative diseases. Diverse plant alkaloids can inhibit the action of acetylcholinesterase and, among them, berberine is a promising bioactive. However, berberine has poor water solubility and low bioavailability, which makes it difficult to use in treatment. The solid dispersion technique can improve the water affinity of hydrophobic substances, but berberine solid dispersions have not been extensively studied. Safety testing is also essential to ensure that the berberine-loaded solid dispersions are safe for use. This study investigated the effectiveness of berberine-loaded solid dispersions (SD) as inhibitors of acetylcholinesterase enzyme (AChE). Docking simulation was used to investigate the influence of berberine on AChE, and in vitro assays were conducted to confirm the enzymatic kinetics of AChE in the presence of berberine. Berberine SD also showed improved cytotoxic effects on tumoral cells when dispersed in aqueous media. In vivo assays using Allium cepa were implemented, and no cytotoxicity/genotoxicity was found for the berberine solid dispersion. These results suggest that berberine SD could be a significant step towards safe nanostructures for use in the treatment of neurodegenerative diseases.
- The nanoencapsulation of curcuminoids extracted from: Curcuma longa L. and an evaluation of their cytotoxic, enzymatic, antioxidant and anti-inflammatory activitiesPublication . Santos, Priscila Dayane Freitas dos; Francisco, Cristhian Rafael Lopes; Coqueiro, Aline; Leimann, Fernanda Vitória; Pinela, José; Calhelha, Ricardo C.; Ineu, Rafael P.; Ferreira, Isabel C.F.R.; Bona, Evandro; Gonçalves, Odinei HessCurcumin, bisdemethoxycurcumin and demethoxycurcumin are the main curcuminoids present in Curcuma longa L. and are known for their bioactivity. However, their low water solubility results in poor bioavailability and therapeutic efficacy. This work aimed to investigate the in vitro modulation capacity on the enzymes acetylcholinesterase (AChE) and glutathione S-transferase (GST), as well as the in vitro antioxidant (OxHLIA and TBARS) and anti-inflammatory activities (RAW 264.7 test) of nanoencapsulated curcuminoids. Cytotoxicity on tumor and non-tumor cell lines was also investigated. Curcuminoid nanoparticles significantly inhibited the in vitro activity of AChE (12% inhibition at 50 μM) and GST (30% inhibition at 5 μM). They presented antioxidant activity and toxic effects against breast adenocarcinoma, lung, cervical and hepatocellular carcinoma cells when dispersed in water. Encapsulated curcuminoids exhibited bioactive properties in aqueous medium (no hydrophobic solvent added), exerting antioxidant and cytotoxic effects and acting on the cholinergic and endogenous antioxidant systems.
- Fish protein hydrolysates: bioactive properties, encapsulation and new technologies for enhancing peptides bioavailabilityPublication . Moreira, Thaysa Fernandes Moya; Gonçalves, Odinei Hess; Leimann, Fernanda Vitória; Ribeiro, Ricardo PereiraFish protein hydrolysates (FPHs) can be obtained from substrates such as fish muscle, skin, and wastes and assign value to these fish by-products. Proteolytic enzymes catalyze the hydrolysis of these fish substrates' peptide bonds resulting in smaller peptides that present several bioactive properties. Hydrolysates' bioactive properties are a function of the fish species used as the substrate, the enzyme selectivity or specificity, pH and temperature applied in the reaction, etc. Furthermore, many pre-treatment methods are being applied to fish protein substrates to improve their enzyme susceptibility and increase the number of smaller bioactive peptides. This review addresses the production of FPHs and the main bioactive properties evaluated recently in the literature and emphasizes the substrate treatments by high-pressure processing, microwave, ultrasound, and thermal treatments to achieve better bioactivity making essential amino acids more available in peptides. The bioactive properties most found in FPHs were antioxidants, antimicrobials, anticancer, and antihypertensive. These bioactivities may vary depending on the conditions of hydrolysis, fish species, and fractionation and isolation of specific peptides.New technologies for the treatment of by-products can reduce process losses and achieve better results by cleavage of proteins. Conversely, encapsulation and film utilization can improve bioactivity, bioavailability, and controlled release when applied to foods, resulting in improved health.
- Lipid composition optimization in spray congealing technique and testing with curcumin-loaded microparticlesPublication . Sorita, Guilherme Dallarmi; Santamaria-Echart, Arantzazu; Gozzo, Ângela Maria; Gonçalves, Odinei Hess; Leimann, Fernanda Vitória; Bona, Evandro; Manrique, Yaidelin A.; Fernandes, Isabel P.; Ferreira, Isabel C.F.R.; Barreiro, M.F.Spray-congealing, a technique based on the fast solidification of sprayed molten lipids, is considered a novel strategy to encapsulate natural products. Among others, it is a safe, low cost, fast and reproducible technique, with rising interest for several applications (e.g. food applications). One of the key parameters for the application of this technique is the lipid solidification temperature, which can be modulated by optimizing the lipid composition. In this work, three lipid components (beeswax, carnauba wax, and medium-chain triglycerides (Miglyol 812)) were selected, and the mixture composition modelled using a simplex-centroid experimental design. Three different lipid compositions were chosen to validate the proposed model, then tested in the preparation of curcumin-loaded microparticles (1.5%, w/w). The produced microparticles were analysed in terms of colour, morphology, particle size, encapsulation efficiency and load, physicochemical, crystalline, and thermal properties. Results evidenced that microparticle's properties, including encapsulation efficiency, vary according to the used lipid mixture, supporting their tailoring role. This fact brings advantages in the design of microencapsulation systems based on spray congealing processes, broadening their applicability. Moreover, lipid composition optimisation was proved to be an important tool to precede the development of spray-congealing applications.
- Influence of nanoencapsulated lutein on acetylcholinesterase activity: In vitro determination, kinetic parameters, and in silico docking simulationsPublication . Miranda, Cristiane Grella; Santos, Priscila Dayane Freitas dos; Silva, Jéssica Thaís do Prado; Leimann, Fernanda Vitória; Borges, Bianca Ferreira; Abreu, Rui M.V.; Ineu, Rafael P.; Gonçalves, Odinei HessLutein is a bioactive found in dark leafy vegetables that may be used as a nutraceutical agent in foodstuff and an inhibitor of key enzymes of the human body such as those involved in the cholinergic system. However, its high hydrophobicity leads to low bioavailability and must be overcome if lutein is to be added in foods. The objective of this study was to evaluate the influence of nanoencapsulated lutein in the activity of the acetylcholinesterase enzyme. The in vitro study was carried out using water in order to evaluate the impact of encapsulation on the hydrophilicity of lutein. In vitro assays showed that lutein, both free and nanoencapsulated, presented a mixedtype inhibition behavior, and encapsulated lutein was able to inhibit acetylcholinesterase activity even in an aqueous medium. Inhibition was also showed by the in silico docking results which show that lutein interacted with the pocket region of the enzyme.
- Progesterone-loaded solid lipid nanoparticles for use in the regulation of the estrous cycle in female ratsPublication . Fogolari, Odinei; Leimann, Fernanda Vitória; Ineu, Rafael Porto; Rudy, Marcia; Ludwig, André Franco; Salles, Fernando Marques; Amorim, João Paulo de Arruda; Franci, Celso Rodrigues; Sagae, Sara Cristina; Sayer, Claudia; Araújo, Pedro Henrique Hermes de; Gonçalves, Odinei HessProtocols used for artificial insemination involve the effective synchronization of the estrous cycle by the administration of exogenous hormones including progesterone analogs. Although widespread in the world, the current techniques present many disadvantages that need to be overcome such as the time dependency of progesterone levels in the blood and the need to remove the release dispositive. Nanotechnology may offer the tools for it, and solid lipid nanoparticles (SLN) are a promising candidate to be used as nanocarriers for progesterone. In this work, progesterone-loaded SLNs were investigated in the regulation of the estrous cycle in female rats. First, the obtention of the SLN was investigated to determine how experimental parameters may affect the encapsulation efficiency of progesterone and the morphology of the nanoparticles. Also, in vitro release profiles of progesterone were also evaluated. Sexual receptivity, mutagenicity, hepatic inflammation and steatosis, hormone measurement, and biometric parameters of pups were also determined. Progesterone-loaded SLN induced estrous cycle synchronization and were able to maintain the estrous phase of the estrous cycle while inducing a greater latency release for its onset. Progesterone induced an increase in the sexual receptivity of the females and did not alter the biometric parameters like the body weight of the mothers and puppies, until weaning. Results gathered here demonstrated that encapsulation of progesterone may be a promising alternative to the conventional methods for synchronization of the estrous cycle of female animals in artificial insemination procedures.
- Antiinflammatory activity of carnauba wax microparticles containing curcuminPublication . Rocha, Bruno Ambrósio da; Francisco, Cristhian Rafael Lopes; Almeida, Mariana; Ames, Franciele Queiroz; Bona, Evandro; Leimann, Fernanda Vitória; Gonçalves, Odinei Hess; Bersani-Amado, Ciomar AparecidaThe pharmacokinetic of curcumin has posed a challenge to its therapeutic efficacy. Drug encapsulation systems, particularly microparticles, are promising due to their ability to protect compounds against both physical and chemical degradation and to improve their bioactivity. The aim of the present study was to prepare curcumin loaded solid lipid microparticles from carnauba wax and evaluate its antiinflammatory efficacy. Microparticles were obtained by hot homogenization technique and characterized by scanning electron microscopy, differential scanning calorimetry, infrared spectroscopy and X-ray diffraction demonstrating the effective encapsulation of curcumin. Antiinflammatory efficacy was evaluated comparing free curcumin and curcumin encapsulated by carrageenan-induced paw edema in rats. Additionally, myeloperoxidase (MPO) activity and concentration of nitric oxide (NO) were evaluated in plantar tissue of rats. Microparticles showed regular and spherical morphology with 20 μm diameter. Thermal, spectroscopic, X-ray and images analysis demonstrated the encapsulation of curcumin in the lipid matrix. The evaluation of antiinflammatory activity showed that encapsulated curcumin at doses of 25 and 50 mg kg 1 were more effective than free curcumin at lower doses of 25 and 50 mg. kg 1 and had similar efficacy to free curcumin at dose a 400 mg.kg 1 , inhibiting the development of edema, myeloperoxidase (MPO) activity, and the increase in nitric oxide (NO) levels. Overall, curcumin microparticles were obtained with high encapsulation efficiency and antiinflammatory efficacy 16-fold better than free curcumin.
- Bioactivity screening of pinhão (Araucaria Angustifolia (Bertol.) Kuntze) seed extracts: the inhibition of cholinesterases and α-amylases, and cytotoxic and anti-inflammatory activitiesPublication . Oliveira, Anielle; Moreira, Thaysa Fernandes Moya; Pepinelli, Ana Luísa; Costa, Luis Gustavo Médice Arabel; Leal, Luana Eloísa; Silva, Tamires Barlati Vieira; Gonçalves, Odinei Hess; Ineu, Rafael P.; Dias, Maria Inês; Barros, Lillian; Abreu, Rui M.V.; Ferreira, Isabel C.F.R.; Bracht, Lívia; Leimann, Fernanda VitóriaThe objective of this work was to determine the potential bioactive properties of extracts from bio-residues of pinhão (Araucaria angustifolia (Bertol.) Kuntze) seeds, namely the α-amylase and cholinesterase inhibition, cytotoxicity, and anti-inflammatory properties. The pinhão extracts evaluated were obtained from cooking water (CW) and as an ethanolic extract from residual pinhão seed shells (PS). Catechin was the major compound found in both extracts. The PS extract presented higher antioxidant levels and the better inhibition of human salivary and porcine pancreatic α-amylases when compared to the CW extract. Also, based on in vivo evaluations, the PS extract did not differ significantly from acarbose when compared to a control group. The most potent inhibitor of cholinesterases was the CW extract. No cytotoxicity toward normal cells was detected, and neither extract showed anti-inflammatory activity. The PS extract presented cytotoxic activity toward non-small-cell lung, cervical, hepatocellular and breast carcinoma cell lines. Overall, the results demonstrated the potential bioactivity of extracts obtained from pinhão bioresidues.
- Enhancement of fish protein hydrolysates for salad dressing through high shear and sterilization pre‐treatmentsPublication . Moreira, Thaysa F. M.; Oliveira, Anielle; Rodrigues, Vanessa de Carvalho; Carvalho, Amarilis Santos; Quichaba, Michely B.; Peron, Ana P.; Gonçalves, Odinei Hess; Gozzo, Angela M.; Leimann, Fernanda Vitória; Ribeiro, Ricardo P.Thermal and mechanical treatments may affect the structure of hydrolyzed proteins, thus influencing the obtaining of peptides with improved bioactivity. In this work, tila- pia muscle was treated by thermal sterilization or homogenization with ultra-turrax (UT) and hydrolyzed with alcalase to obtain FPHs with antioxidant properties in salad dressing. To evaluate the bioactive potential of FPHs, the acetylcholinesterase inhibi- tion assay was applied, resulting in up to 45.87% inhibition for the UT sample (60 mg/mL). Also, no cytotoxicity was detected by Allium cepa model for all FPHs. The emulsifying activity index and emulsifying stability index of FPHs indicated better emulsifying capacity in basic pH. As a proof of concept, FPHs were used as an emulsi- fying/antioxidant agent to prepare a salad dressing. FPHs increased the formulation's protein content, pseudoplastic behavior, color, and texture. In addition, FPHs aided the oxidative stability of salad dressing (evaluated by oil's extinction coefficient), dem- onstrating potential application in emulsified foods by acting on the elimination of radicals generated in lipid oxidation. Practical applications Fish protein hydrolysates (FPHs) offer diverse bioactive properties such as antioxi- dant, antimicrobial, anticancer, antihypertensive, and acetylcholinesterase (associated with Alzheimer's disease) inhibitory effects. However, optimizing their technological properties poses a challenge, affecting applicability and bioactivity. Industrial pro- cesses such as thermal and mechanical treatments can alter protein structures, influencing peptide bioactivity post enzymatic hydrolysis. This study investigates the impact of substrate pre-treatments, sterilization via thermal heating, and homogeniza- tion using a rotor-stator system (ultra-turrax) on FPHs' technological properties after hydrolysis with alcalase, including emulsifying capacity and acetylcholinesterase inhibitory capacity. In addition, it explores the application of pre-treated FPHs in a real food system (French salad dressing), assessing rheological properties, texture, and oxidative stability. Such evaluations are crucial for ensuring the feasibility of industrial FPHs production and their application.
- Chemometric approaches to evaluate the substitution of synthetic food dyes by natural compounds: The case of nanoencapsulated curcumin, spirulina, and hibiscus extractsPublication . Teixeira, Valéria Maria Costa; Silva, Roberta França Gomes da; Gonçalves, Odinei Hess; Pereira, Carla; Barros, Lillian; Ferreira, Isabel C.F.R.; Bona, Evandro; Leimann, Fernanda VitóriaFinding natural food coloring options from plant-based sources to substitute artificial dyes is a challenging task because natural dyes often present low water-solubility, not very vibrant hues, and instability due to interactions with food ingredients. Chemometric approaches can be used to evaluate color differences and patterns resulting from natural and synthetic dyes when applied to food systems. Here, the Mixture Design and the Principal Component Analysis (PCA) were applied to evaluate the substitution of the following artificial food dyes: yolk yellow, apricot yellow, strawberry red, and tartrazine by natural dyes (water-soluble curcumin, yellow shade; Hibiscus sabdariffa extract, red shade; Spirulina platensis extract, blue/green shade), in three food simulated systems (phosphate buffer, pH 6.9; yogurt, pH 4.0 and citrate buffer, pH 3.0). The color parameters L*, a*, b*, C* and °h were determined and color difference (ΔE*) with artificial dyes resulted in 11 empirical models. PCA yielded a clear map for the identification of the closely matches natural/artificial dyes for the food simulated systems in three subregions. Furthermore, the antioxidant capacity of the natural dyes was determined by OxHLIA and TBARS. It was possible to make an assessment guide that may be useful for other food systems and dyes.