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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.
- Propriedades bioativas de formulações hidrofílicas de curcumina: aplicação em iogurtePublication . Leimann, Fernanda Vitória; Almeida, Heloísa H.S.; Roriz, Custódio Lobo; Barros, Lillian; Barreira, João C.M.; Calhelha, Ricardo C.; Barreiro, M.F.; Ferreira, Isabel C.F.R.A curcumina tem reconhecidas propriedades bioativas e corantes. Porém, a sua aplicação em produtos alimentares é dificultada pela sua baixa solubilidade em meios hidrofílicos. De forma a ultrapassar esta limitação, foram preparadas nanopartículas de poli(vinil-pirrolidona) (PVP, 40.000g/mol)/curcumina com base na técnica de dispersão sólida, utilizando Tween 80 como estabilizante e etanol como solvente. As nanopartículas foram caracterizadas quanto à morfologia (microscopia eletrónica de transmissão) indicando forma esférica e tamanho (dispersão dinâmica de luz) com índice de polidispersão = 0,050±0,009 e diâmetro médio em intensidade = 377±15 nm. As propriedades térmicas (análise termogravimétrica, TG), interações químicas (Espectroscopia de Infravermelho com Transformada de Fourier, FTIR). As análises por TG revelaram que as nanopartículas não apresentaram perda de humidade (não se observou nenhuma transição antes dos 100 ºC), justificada pelo facto de os pontos de ligação da PVP à água terem dado origem a interações com a curcumina na sequência da encapsulação [1]. A análise por FTIR comprovou este facto dado a ausência da banda característica a 3510 cm-1 na zona do estiramento dos OHs. As propriedades bioativas (atividade antioxidante, atividade anti-inflamatória e citotoxicidade) das nanopartículas de PVP/curcumina (NC) foram comparadas às da curcumina pura utilizada no procedimento de nanoencapsulação (PC) (Sigma Aldrich) e às de uma amostra comercial dispersável (DC) (CHR Hansen, Vegex Tumeric WS5). Os valores de EC50 (μg/mL) para a atividade antioxidante (DPPH, poder redutor, β-caroteno e TBARS) evidenciaram o seguinte perfil de atividade: PC>NC>DC, similarmente à resposta anti-inflamatória (concentração responsável por 50% da inibição da produção de óxido nítrico em comparação com o controlo negativo). Quanto à citotoxicidade, a PC revelou uma atividade superior em todas as linhas celulares, tendo os valores de GI50 (μg/mL) indicado atividade NC>DC apenas nos casos das linhas HeLa, HepG2 e PLP2 e indistinta nas MCF-7 e NCI-H460. Na etapa seguinte, as formulações PC, NC e DC foram aplicadas em iogurtes, para os quais se avaliou o perfil nutricional (humidade, cinzas, gordura, proteínas, hidratos de carbono e energia) e os parâmetros de cor (L*, a* e b*) ao longo do tempo de armazenamento (TA = 0, 7 e 15 dias, 4 ºC). Independentemente de TA, os iogurtes com DC apresentaram os teores de cinza, gordura, energia e L* superiores, enquanto os valores a* e b* foram superiores para os com PC. O teor máximo de proteína foi registado para os iogurtes com NC e o teor máximo de hidratos de carbono para as amostras controlo. Quanto a TA, as amostras armazenadas durante 7 dias caracterizaram-se por teores superiores de proteína, cinza (tal como as amostras armazenadas durante 15 dias), hidratos de carbono e energia, enquanto as amostras analisadas no dia de preparação registaram os valores mais elevados para gordura e a*. O efeito do tempo de armazenamento não foi significativo nos parâmetros L* e b*. Em síntese, e apesar de se terem observado algumas diferenças significativas nos indicadores nutricionais e parâmetros de cor, pode concluir-se que as nanopartículas de PVP/curcumina são uma boa estratégia para coloração do iogurte, não se tendo registado sem alterações relevantes do seu valor nutricional e aparência. Adicionalmente, e dado a bioatividade evidenciada, a sua utilização resultará em benefícios adicionais não conseguidos com a PC (baixa solubilidade em meio hidrofílico).
- 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.
- Efeito do teor de etanol na composição de compostos fenólicos extraídos da casca de sementes de pinhãoPublication . Santos, Carlos Henrique Koslinski; Dias, Maria Inês; Barros, Lillian; Baqueta, Michel Rocha; Coqueiro, Aline; Barreiro, M.F.; Gonçalves, Odinei Hess; Bona, Evandro; Silva, Marcos Vieira da; Ferreira, Isabel C.F.R.; Leimann, Fernanda VitóriaAs sementes de Araucaria angustifolia (Bertol.) Kuntze, designadas por pinhão, são normalmente consumidas após cozedura, sendo as cascas descartadas. Contudo, estes bioresíduos podem ser aproveitados como fonte de compostos antioxidantes. Neste trabalho, procedeu-se à extração e caracterização de antioxidantes a partir da casca de pinhão, previamente submetida a cozedura. As cascas, secas e trituradas, foram submetidas a extração (8,75 gcascas/100 mLsolvente) com misturas etanol:água (97% e 38%; v/v etanol) em homogeneizador Ultra-Turrax (a 12.000 rpm, 15 min e temperatura controlada num banho termostático a 42,5ºC). Os extratos foram posteriormente analisados quanto ao perfil fenólico (HPLC-DAD-ESI/MS), de acordo com um procedimento previamente otimizado por alguns dos autores [1]. Adicionalmente, foi avaliado o rendimento em volume de extrato obtido em relação ao volume inicial de solvente utilizado na extração, e analisada a microestrutura (Microscopia Eletrónica de Varrimento, MEV) das amostras após o processo de extração. Foram identificados treze compostos fenólicos, dez proantocianidinas (catequina e derivados de epicatequina), dois ácidos fenólicos (ácido protocatéquico e derivados de ácido ferúlico), um flavonol (quercetina-3-O-glucósido) e uma flavona (eriodictiol-O-hexósido). A extração usando um teor superior de etanol (97%) conduziu a uma concentração de compostos fenólicos extraídos superior (60,66±0,83 mg/gextrato), comparativamente com a extração efetuada com 38% de etanol (22,28±0,13 mg/gextrato). Quanto ao rendimento em volume foram obtidos os seguintes resultados: 44% e 62% para 97% e 38% de etanol, respetivamente. Com as imagens de MEV concluiu-se que um teor superior de água no solvente de extração favoreceu o inchamento e o dilaceramento das amostras. Em conclusão, a utilização de teores superiores em etanol favoreceu a extração de compostos fenólicos e conduziu à recuperação de um volume de extrato final superior.
- 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.