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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.
- Functionalization of yogurts with Agaricus bisporus extracts encapsulated in spray-dried maltodextrin crosslinked with citric acidPublication . Francisco, Cristhian Rafael Lopes; Heleno, Sandrina A.; Fernandes, Isabel P.; Barreira, João C.M.; Calhelha, Ricardo C.; Barros, Lillian; Gonçalves, Odinei Hess; Ferreira, Isabel C.F.R.; Barreiro, M.F.Mushroom extracts contain bioactive compounds potentially useful to functionalize foodstuffs. Herein, alcoholic extracts of Agaricus bisporus were studied for their bioactivity and viability as functional ingredients in a food product with high water content (yogurt). Extracts were microencapsulated (to improve their stability and hydrophilicity) by spray-drying, using maltodextrin crosslinked with citric acid as encapsulating material. The effect of thermal treatment (after atomization) on crosslinking and bioactivity of microspheres was tested. The incorporation of free and thermally untreated forms resulted in yogurts with higher initial antioxidant activity (EC 50 values: 214 and 272 mg.mL −1 ) that decreased after 7 days (EC 50 values: 248 and 314 mg.mL −1 ). Contrarily, thermally treated microencapsulated extracts showed higher antioxidant activity after the same period (EC 50 values, 0 days: 106 mg.mL −1 ; 7 days: 48.7 mg.mL −1 ), in result of an effective protection provided by microencapsulation with crosslinked maltodextrin and citric acid. Functionalized yogurts showed an overall maintenance of nutritional properties.
- 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.
- Bioactive properties of dairy beverages functionalized with pure ergosterol and mycosterol extracts: a comparative study with phytosterol counterpartsPublication . Heleno, Sandrina A.; Rudke, Adenilson; Calhelha, Ricardo C.; Barros, Lillian; Gonçalves, Odinei Hess; Rodrigues, Alírio; Barreiro, M.F.; Ferreira, Isabel C.F.R.Agaricus bisporus L. is the most consumed mushroom worldwide exhibiting a high content of ergosterol in its sterol’s fraction (~90%). Some studies have demonstrated the health benefits of this molecule related to its antioxidant, antitumor and also hypocholesterolemic effects, similar to the ones exhibited by phytosterols. Functional foods containing phytosterols, or their derivatives, can be found at commercial level bearing the European Food Safety Authority approved health claim “able to lower cholesterol levels in serum”. Therefore, this work aims to present the use of mycosterols as an innovative alternative to phytosterols. A. bisporus bioresidues obtained from mushroom’s industry were used to obtain mycosterols by ultrasound assisted extraction. Pure ergosterol and the obtained mycosterol extracts were added to dairy beverages, in a similar amount to the one used in the commercial ones incorporated with phytosterols. All the beverages were analysed immediately (T0) and after seven days of storage at 4ºC (T1) regarding nutritional parameters, antioxidant activity and cytotoxic properties against human tumor cell lines and a non‐tumor porcine liver primary culture. The beverages functionalized with the mycosterols extract revealed an antioxidant activity similar to the commercial beverages with phytosterols. However, beverages with pure ergosterol revealed twice this antioxidant activity. Moreover, only the samples functionalized with pure ergosterol or the mycosterols extract have shown an increase in the antioxidant activity from T0 to T1, meaning that the compound/extracts were able to protect the dairy drink from oxidation, increasing the product shelf life. Samples with pure ergosterol also revealed the highest cytotoxicity for tumor cell lines, while the beverages with phytosterols showed the lowest activity with no significant differences between T0 and T1. All the samples revealed a similar nutritional composition, and none of them revealed toxicity for normal cells. Studies on the hypocholesterolemic effects of the developed beverages are being carried out.
- Caracterização dos resíduos de Brassica oleracea L. para obtenção de um potencial ingrediente naturalPublication . Pepinelli, Ana Luísa; Oliveira, Tatiane C.G.; Junior, Eleomar Pires; Caleja, Cristina; Dias, Maria Inês; Kostić, Marina; Soković, Marina; Calhelha, Ricardo C.; Mandim, Filipa; Gonçalves, Odinei Hess; Oliveira, Beatriz; Pereira, Eliana; Barros, LillianA comunidade cientifica, em parceria com a indústria alimentar, tem vindo a estudar diferentes matrizes naturais, a fim de obter ingredientes funcionais com potencial aplicação neste setor industrial. Nesse sentido, este trabalho pretendeu fazer a caracterização de Brassica oleracea var. Acephala (popularmente conhecida como couve galega) quanto ao seu perfil fenólico e ação biológica, com o objetivo de identificar compostos fenólicos com potencial conservante e/ou bioativo para incorporação na indústria alimentar. O perfil fenólico individual foi obtido através de um sistema de HPLC-DAD/ESI-MSn e o potencial bioativo foi avaliado através de ensaios in vitro. A atividade citotóxica foi avaliada em linhas celulares tumorais humanas (AGS, CaCo2, MCF-7, NCI-H460) e a toxicidade em uma linha celular não tumoral (VERO), através do método colorimétrico da sulforodamina B. A atividade anti-inflamatória foi estudada em macrófagos de rato (RAW 264.7); a atividade antimicrobiana foi testada usando o método de microdiluição; e a atividade antioxidante foi avaliada através dos ensaios de TBARS (inibição da peroxidação lipidica) e CAA (atividade antioxidante celular). O perfil fenólico dos bioresíduos de couve galega revelou a presença de moléculas com elevado interesse em concentrações promissoras. Em relação ao potencial bioativo da amostra, foi possível observar uma interessante atividade antioxidante pela análise de TBARS, onde na concentração de 19 μg/mL foi possível oferecer 50% da atividade, porém pela análise de CAA os resultados foram moderados, com uma concentração de 2000 μg/mL com uma inibição de 40%. A atividade antimicrobiana revelou resultados muito satisfatórios, destacando-se as bactérias Bacillus cereus e Enterobacter cloacae e os fungos Aspergillus fumigatus e Penicillium fumiculosum como as estirpes mais suscetíveis ao efeito do extrato da couve. Em relação à atividade citotóxica e antiinflamatória, o extrato da couve não apresentou capacidade antiproliferativa na concentração máxima testada (400 μg/mL), revelando a ausência de potencial antitumoral e anti-inflamatório, mas também, provando a ausência de toxicidade do extrato. Considerando esses resultados, os bioresíduos da couve apresentam uma composição rica em compostos de elevado interesse, nomeadamente com potencial antioxidante, o que pode ser interessante para o desenvolvimento de ingredientes funcionais com possíveis aplicação na indústria. Para além disso, a reutilização de subprodutos permitirá não só diminuir o desperdício alimentar, como também criar soluções estratégicas no setor agroindustrial de crescimento económico e sustentabilidade.
- 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.