RESUMO

The effects of adding cochineal carmine and annatto dyes in five mortadella formulations made with curcumin microcrystals were compared, and the preference was evaluated and described sensorially. Based on the optimized formulation obtained with color parameters, two formulations were elaborated: curcumin microcrystals and cochineal carmine were added. During 60 days, pH, objective color, water retention capacity, lipid oxidation, and texture profile analyses were performed. The results demonstrate the possibility of excluding sodium erythorbate from formulations containing curcumin microcrystals. There was no significant difference in lipid oxidation between the samples, presenting at the end of 60 days a value of 0.11 mg and 0.10 mg of MDA kg-1 for the two samples, respectively. There were also no significant differences between the two samples or the evaluated storage times, and the average values obtained for pH, WRC, objective color, and TPA were expected for this type of cooked meat sausage. In the presence of curcumin microcrystals, the synthetic antioxidant, sodium erythorbate, can be eliminated from the formulations, as it does not affect the physical-chemical parameters studied, such as pH, water retention capacity, color objective, and texture profile.

RESUMO

Neurodevelopmental disorders, such as autism spectrum disorder (ASD) and attention deficit hyperactivity disorder (ADHD), are characterized by persistent changes in communication and social interaction, as well as restricted and stereotyped patterns of behavior. The complex etiology of these disorders possibly combines the effects of multiple genes and environmental factors. Hence, exposure to insecticides such as imidacloprid (IMI) has been used to replicate the changes observed in these disorders. Lutein is known for its anti-inflammatory and antioxidant properties and is associated with neuroprotective effects. Therefore, the aim of this study was to evaluate the protective effect of lutein-loaded nanoparticles, along with their mechanisms of action, on Drosophila melanogaster offspring exposed to IMI-induced damage. To simulate the neurodevelopmental disorder model, flies were exposed to a diet containing IMI for 7 days. Posteriorly, their offspring were exposed to a diet containing lutein-loaded nanoparticles for a period of 24 h, and male and female flies were subjected to behavioral and biochemical evaluations. Treatment with lutein-loaded nanoparticles reversed the parameters of hyperactivity, aggressiveness, social interaction, repetitive movements, and anxiety in the offspring of flies exposed to IMI. It also protected markers of oxidative stress and cell viability, in addition to preventing the reduction of Nrf2 and Shank3 immunoreactivity. These results demonstrate that the damage induced by exposure to IMI was restored through treatment with lutein-loaded nanoparticles, elucidating lutein's mechanisms of action as a therapeutic agent, which, after further studies, can become a co-adjuvant in the treatment of neurodevelopmental disorders, such as ASD and ADHD.

Assuntos

Comportamento Animal , Drosophila melanogaster , Luteína , Nanopartículas , Nitrocompostos , Animais , Drosophila melanogaster/efeitos dos fármacos , Luteína/farmacologia , Luteína/administração & dosagem , Comportamento Animal/efeitos dos fármacos , Masculino , Feminino , Nitrocompostos/toxicidade , Neonicotinoides/toxicidade , Estresse Oxidativo/efeitos dos fármacos , Inseticidas/toxicidade , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/administração & dosagem , Transtornos do Neurodesenvolvimento/prevenção & controle , Transtornos do Neurodesenvolvimento/induzido quimicamente , Transtornos do Neurodesenvolvimento/metabolismo , Antioxidantes/farmacologia , Antioxidantes/metabolismo

RESUMO

The present study thus aimed at the development and physicochemical characterization of solid lipid nanoparticles loaded with crude extract of Piper corcovadensis roots (SLN - CEPc) and chitosan - coated solid lipid nanoparticles loaded with crude extract of P. corcovadensis roots (C - SLN - CEPc), as well as the determination of its antimycobacterial activity against Mycobacterium tuberculosis H37Rv, its cytotoxicity against the Vero cell line and evaluation in the hemolysis assay. Both formulat ions containing the encapsulated extract showed high encapsulation efficiency, formed by a monodispersed system with small and spherical particles, and there was no aggregation of particles. In the biological assays, SLN - CEPc and C - SLN - CEPc showed promisin g anti - M. tuberculosis activity with a minimum inhibitory concentration (MIC) of 12.5 µg/mL, whereas the cytotoxic concentrations obtained at 50% (CC 50 ) in Vero cells were 60.0 and 70.0 µg/mL, respectively. Therefore, nanoencapsulation showed satisfactory results, justifying its usage in the development of new products.

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El presente estudio apuntó al desarrollo y caracterización fisicoquímica de na nopartículas lípidas en estado sólido, cargadas con extracto crudo de raíz de Piper c orcovadensis (SLN - CEPc) y nanopartículas lípidas en estado sólido cubiertas con quitosano cargadas co n extracto crudo de raíz de P. corcovadensis (C - SLN - CEPc), así como la determinación de su actividad antimico bacterial contra Mycobacterium tuberculosis H37Rv, su citotoxicidad contra la línea celular Vero y su evaluación en ensayo de hemólisis. Ambas formulaciones que contenían el extracto encapsulado mostraron alta eficien cia de encapsulación, formado por un sistema monodispersado con pequeñas partículas esféricas, y no hubo agregación de partículas. En los ensayos biológicos, SLN - CEPc y C - SLN - CEPc mostraron un a prometedora actividad anti - M. tuberculosis con una mínima conc entración inhibitoria (MIC) de 12,5 µg/mL, mientras que las concentraciones citotóxicas obtenidas al 50% (CC 50 ) en células Vero estuvo en 60,0 y 70,0 µg/mL, respectivamente. Por lo tanto, la nanoencapsulación mostró resultados satisfactorios, justificando su uso en el desarrollo de nuevos productos.

Assuntos

Extratos Vegetais/administração & dosagem , Sistemas de Liberação de Medicamentos , Piper/química , Antibacterianos/administração & dosagem , Mycobacterium tuberculosis/efeitos dos fármacos , Temperatura , Portadores de Fármacos , Cromatografia Líquida de Alta Pressão , Raízes de Plantas , Quitosana , Nanopartículas , Lipídeos

RESUMO

ß-carotene-loaded nanoparticles improves absorption by increasing bioavailability. The Drosophila melanogaster model of Parkinson's disease must be helpful in investigating potential neuroprotective effects. Four groups of four-day-old flies were exposed to: (1) control; (2) diet containing rotenone (500 µM); (3) ß-carotene-loaded nanoparticles (20 µM); (4) ß-carotene-loaded nanoparticles and rotenone for 7 days. Then, the percentage of survival, geotaxis tests, open field, aversive phototaxis and food consumption were evaluated. At the end of the behaviors, the analyses of the levels of reactive species (ROS), thiobarbituric acid reactive substances (TBARS), catalase (CAT) and superoxide dismutase (SOD) activity was carried out, as well as an evaluation of the levels of dopamine and acetylcholinesterase (AChE) activity, in the head of flies. Nanoparticles loaded with ß-carotene were able to improve motor function, memory, survival and also restored the oxidative stress indicators (CAT, SOD, ROS and TBARS), dopamine levels, AChE activity after exposure to rotenone. Overall, nanoparticles loaded with ß-carotene showed significant neuroprotective effect against damage induced by the Parkinson-like disease model, emerging as a possible treatment. Overall, ß-carotene-loaded nanoparticles presented significant neuroprotective effect against damage induced by model of Parkinson-like disease, emerging as a possible treatment.

Assuntos

Nanopartículas , Fármacos Neuroprotetores , Doença de Parkinson , Animais , Doença de Parkinson/tratamento farmacológico , Doença de Parkinson/prevenção & controle , Drosophila melanogaster , beta Caroteno/farmacologia , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Dopamina , Rotenona , Espécies Reativas de Oxigênio , Fármacos Neuroprotetores/farmacologia , Substâncias Reativas com Ácido Tiobarbitúrico , Acetilcolinesterase/metabolismo , Estresse Oxidativo , Superóxido Dismutase/metabolismo , Modelos Animais de Doenças

RESUMO

Fish 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.

Assuntos

Peixes , Hidrolisados de Proteína , Animais , Hidrolisados de Proteína/química , Hidrolisados de Proteína/metabolismo , Disponibilidade Biológica , Peixes/metabolismo , Peptídeos/química , Anti-Hipertensivos/química , Hidrólise , Antioxidantes/química

RESUMO

The present study prepared, optimized, and characterized solid lipid microparticles that contained trans-anethole (SLMAN), evaluated their antiinflammatory activity in acute and chronic inflammation models, and investigated their effects on the gastric mucosa in arthritic rats. The microparticles were obtained by a hot homogenization process and characterized by physicochemical analyses. The acute inflammatory response was induced by an intradermal injection of 0.1 ml of carrageenan solution (200 µg) in the hind paw. The rats were treated orally with a single dose of SLMAN 1 h before induction of the inflammatory response. The chronic inflammatory response was induced by the subcutaneous application of 0.1 ml of complete Freund's adjuvant suspension (500 µg) in the hind paw. SLMAN was orally administered, starting on the day of arthritis induction, and continued for 21 days. The results showed that SLMAN was obtained with good encapsulation efficiency. Treatment with SLMAN at doses of 25 and 50 mg/kg was as effective as trans-anethole (AN) at a dose of 250 mg/kg on acute and chronic inflammatory responses. Histological analyses showed that treatment with SLMAN did not aggravate lesions in the gastric mucosa in arthritic rats. These results indicated that treatment with SLMAN at a dose that was 5-10 times lower than non-encapsulated AN exerted an inhibitory effect on acute and chronic inflammatory responses, suggesting the better bioavailability and efficacy of microencapsulated AN without aggravating lesions in the gastric mucosa in arthritic rats.

Assuntos

Artrite Experimental , Ratos , Animais , Artrite Experimental/induzido quimicamente , Artrite Experimental/tratamento farmacológico , Artrite Experimental/patologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Inflamação/tratamento farmacológico , Inflamação/patologia , Lipídeos

RESUMO

The 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 bio-residues.

Assuntos

Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Araucaria/química , Inibidores da Colinesterase/farmacologia , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , Animais , Antioxidantes/farmacologia , Catequina/análise , Linhagem Celular Tumoral , Colinesterases/metabolismo , Humanos , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Extratos Vegetais/análise , Sementes/química , alfa-Amilases/metabolismo

RESUMO

Pathogenic and deteriorating bacteria are a great concern to food safety. In this sense, the present study evaluated the fight against microbial contamination through the use of nanoparticles containing curcumin, in addition to analyzing the physical properties of these nanoparticles. Efficient curcumin encapsulation was determined by Fourier transform infrared spectra evaluation and differential scanning calorimetry. Transmission electron microscopy images showed irregular shaped nanoparticles with broad size distribution (20-250 nm). The antibacterial activity was considered satisfactory, since curcumin in the form of nanoparticles demonstrated antimicrobial and antibacterial activity superior to curcumin in its free form, against both pathogenic bacteria, such as Staphylococcus aureus (MIC 125 µg/mL), and deteriorates, such as Alicyclobacillus acidoterrestris (MIC 62.5 µg/mL). Since curcumin nanoparticles may be consumed as a food additive, the bioactive properties of the nanoencapsulated curcumin were also evaluated in relation to antioxidant capacity (Thiobarbituric acid reactive substances (TBARS) and oxidative hemolysis inhibition assays) and cytotoxicity against four carcinoma cell lines, as well as two non-tumor cells. As a proof of concept, nanoparticles were incorporated in orange juice, with the juice maintaining satisfactory pH, °Brix, and color stability, during three days of storage (8 °C).

Assuntos

Alicyclobacillus , Citrus sinensis , Curcumina , Curcumina/farmacologia , Esporos Bacterianos

RESUMO

AIMS: Quercetin has been investigated as an agent to treat rheumatoid arthritis. At high doses it improves inflammation and the antioxidant status of arthritic rats, but it also exerts mitochondriotoxic and pro-oxidant activities. Beneficial effects of quercetin have not been found at low doses because of its chemical instability and low bioavailability. In the hope of overcoming these problems this study investigated the effects of long-term administration of quercetin-loaded pectin/casein microparticles on the oxidative status of liver and brain of rats with adjuvant-induced arthritis. MAIN METHODS: Particle morphology was viewed with transmission electron microscopy and the encapsulation efficiency was measured indirectly by X-ray diffraction. Quercetin microcapsules (10 mg/Kg) were orally administered to rats during 60 days. Inflammation indicators and oxidative stress markers were measured in addition to the respiratory activity and ROS production in isolated mitochondria. KEY FINDINGS: Quercetin was efficiently encapsulated inside the polymeric matrix, forming a solid amorphous solution. The administration of quercetin microparticles to arthritic rats almost normalized protein carbonylation, lipid peroxidation, the levels of reactive oxygen species as well as the reduced glutathione content in both liver and brain. The paw edema in arthritic rats was not responsive, but the plasmatic activity of ALT and the mitochondrial respiration were not affected by quercetin, indicating absence of mitochondriotoxic or hepatotoxic actions. SIGNIFICANCE: Quercetin-loaded pectin/casein microcapsules orally administered at a low dose improve oxidative stress of arthritic rats without a strong anti-inflammatory activity. This supports the long-term use of quercetin as an antioxidant agent to treat rheumatoid arthritis.

Assuntos

Artrite Experimental/patologia , Caseínas/química , Microesferas , Estresse Oxidativo , Pectinas/química , Quercetina/farmacologia , Alanina Transaminase/sangue , Animais , Antioxidantes/farmacologia , Artrite Experimental/sangue , Encéfalo/efeitos dos fármacos , Encéfalo/patologia , Varredura Diferencial de Calorimetria , Respiração Celular/efeitos dos fármacos , Edema/patologia , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Mitocôndrias Hepáticas/efeitos dos fármacos , Mitocôndrias Hepáticas/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Oxirredutases/metabolismo , Ratos , Espécies Reativas de Oxigênio/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X

RESUMO

Vitamin D is a water-insoluble compound presented in two main forms (D2 and D3), susceptible to environmental conditions. Microencapsulation is an alternative to supplements and preserve vitamin D properties in foods. Entrapment efficiency (EE) is the main property to evaluate the encapsulation effectiveness and therefore it is of interest the study of analytical methods for the identification and quantification of this compound within the particle. This paper describes a low cost UV-Vis methodology validation to the identification and quantification of vitamin D3 in microparticles produced by hot homogenization. The method was validated following the International Conference on Harmonization (ICH) guidelines. To guarantee safe application in foodstuff, microparticles toxigenicity was evaluated with Allium cepa L. in vivo model, showing no cytotoxic nor genotoxic potential. High entrapment efficiency was obtained, the results also demonstrated that the concentration of vitamin D3 in microparticles can be safely accessed by the validated method.

Assuntos

Colecalciferol/análise , Colecalciferol/toxicidade , Suplementos Nutricionais/análise , Análise de Alimentos/métodos , Microesferas , Colecalciferol/química , Contaminação de Alimentos/análise , Cebolas/química

RESUMO

Curcuminoids found in turmeric have attracted attention due to their remarkable biological activity. Nanoencapsulation may improve their technological properties, but extraction and encapsulation procedures could be time-consuming and expensive when carried out separately. This work aimed to combine extraction and nanoencapsulation steps to obtain curcuminoids-polyvinylpyrrolidone (PVP) nanoparticles directly from plant rhizomes. This single-step procedure was evaluated by a Rotatable Central Composite Design (RCCD) and optimized using desirability functions, resulting in the optimal conditions of temperature (29.9°C), ethanol (99%), and PVP (15.38 mg). Nanoencapsulation allowed curcuminoids to exert scavenging activity against superoxide anions donors and hydrogen peroxide in an aqueous medium, despite their poor water solubility. Curcuminoids-PVP nanoparticles could be used to formulate nutraceutical foods as an adjuvant to the endogenous antioxidant defense systems protecting against cellular damage. PRACTICAL APPLICATION: Simultaneous extraction and nanoencapsulation of curcuminoids from turmeric (Curcuma longa L.) was studied in this work. The combination of two processes in one single step reduces production time and costs, enhancing the feasibility of curcuminoids microparticles application into foodstuff. Moreover, since most foodstuff presents water in their composition, increase of curcuminoids water dispersibility could facilitate their incorporation into food matrices and improve the use of their health benefits, as results from this research demonstrated that encapsulated curcuminoids were able to scavenge reactive oxygen species in aqueous medium, even though they are lipophilic compounds.

Assuntos

Curcuma , Curcumina , Antioxidantes , Diarileptanoides , Rizoma

RESUMO

There is growing interest in the development of biodegradable packaging materials containing natural antioxidant extracts. In this sense, the use of extracts obtained from agro-industrial byproducts has proved to be a sustainable alternative. In this study, Pinhão extract, a byproduct of Pinhão (Araucaria angustifolia (Bertol.) Kuntze) seed consumption, was characterized by HPLC-DAD-ESI/MSn, demonstrating the presence of eight phenolic compounds, (+)-catechin and (-)-epicatechin being the most abundant molecules. TPS/PBAT films containing Pinhão extract were produced by blown extrusion and their properties (tensile properties, thermal characteristics and microstructure) were evaluated in order to determine the effect of the presence of extracts. Results suggested that the interaction between the phenolic compounds of the extract and the polymeric matrix caused the reduction in the crystallinity degree, and an increase in the starch glass transition temperature. The presence of Araucaria angustifolia (Bertol.) Kuntze extract significantly (p < 0.05) affected the color and opacity of the film. Regarding water vapor permeation, no significant difference (p > 0.05) was detected. However, the water solubility and the contact angle with water (polar solvent) and diiodomethane (non-polar solvent) significantly changed due to the extract addition. Moreover, the Pinhão extract conferred significant antioxidant capacity to the TPS/PBAT films as determined by DPPH, suggesting that this material can be applied as an active packaging material.

Assuntos

Araucaria/química , Embalagem de Alimentos/instrumentação , Fenóis/química , Extratos Vegetais/química , Poliésteres/química , Amido/química , Cor , Temperatura Alta , Fenóis/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Polímeros/química , Sementes/química , Resistência à Tração

RESUMO

This research was to compare mortadella elaborated with synthetic antioxidant and microcrystals of curcumin in relation to its physicochemical and sensorial characteristics for a period of 90 days. It was detect no differences between the three evaluated treatments in relation to the pH, color, and texture profile features. The mortadella with curcumin microcrystals showed significantly lower TBARS values at the end of the storage when compared to the other treatments. In the sensory analysis, the addition of curcumin decreased the acceptance of color's sample and the purchase intention, but no significant difference was observed among the other attributes. The color of the sample containing curcumin also became worse than its day-of-production standard during storage. The results obtained suggest the potential of curcumin in replacing synthetic antioxidants in cooked meat sausage, since it practically does not modify its physicochemical characteristics, besides preventing the oxidation of the food.

Assuntos

Antioxidantes/química , Curcumina/química , Produtos da Carne , Ácido Ascórbico/química , Cor , Comportamento do Consumidor , Culinária , Armazenamento de Alimentos , Humanos , Concentração de Íons de Hidrogênio , Produtos da Carne/análise

RESUMO

Curcumin, 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.

Assuntos

Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Curcuma/química , Nanopartículas/química , Extratos Vegetais/química , Acetilcolinesterase , Animais , Anti-Inflamatórios/química , Antineoplásicos Fitogênicos/química , Antioxidantes/química , Encéfalo/enzimologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Glutationa Transferase/antagonistas & inibidores , Humanos , Camundongos , Células RAW 264.7 , Ratos

RESUMO

There is an increasing demand for healthier foodstuff containing specific compounds such as Polyunsaturated Fatty Acids (PUFAs). In the case of PUFAs, protection against oxidative degradation is challengeable and microencapsulation emerges as an alternative. Mayonnaises containing microencapsulated oils could be a source of PUFAs. The objective was to formulate mayonnaises containing microencapsulated chia seeds oil, pumpkin seeds oil or baru oil. Micrometric particles with high encapsulation efficiency were produced and thermal analyses indicated an increased thermal stability of all oils after encapsulation. Rheology studies highlighted an increase in the mayonnaise viscosity when microparticles containing chia and pumpkin seeds oil were added. Mechanical texture was not affected by the presence of microparticles in the mayonnaise in all formulations tested. Nevertheless, samples containing microcapsules up to 5%wt were not distinguished from the base-mayonnaise in the sensorial test. Overall, enriched mayonnaises were successfully produced and encapsulation was efficient in protecting oils from oxidation.

Assuntos

Ácidos Graxos Insaturados/química , Indústria de Processamento de Alimentos/métodos , Alimentos , Óleos de Plantas/química , Cápsulas , Cucurbita/química , Composição de Medicamentos , Oxirredução , Prunus/química , Reologia , Salvia/química , Sementes/química

RESUMO

Curcumin, the main bioactive polyphenolic compound in Curcuma longa L. rhizomes has a wide range of bioactive properties. Curcumin presents low solubility in water and thus limited bioavailability, which decreases its applicability. In this study, cytotoxic effects of curcumin solid dispersions (CurSD) were evaluated against tumor (breast adenocarcinoma and lung, cervical and hepatocellular carcinoma) and non-tumor (PLP2) cells, while cytotoxic and genotoxic effects were evaluated in Allium cepa. The effect of the CurSD on the acetylcholinesterase (AChE), butyrylcholinesterase (BChE), glutathione S-transferase (GST), and monoamine oxidase (MAO A-B) enzymes was determined, as well as its capacity to inhibit the oxidative hemolysis (OxHLIA) and the formation of thiobarbituric acid reactive substances (TBARS). CurSD are constituted by nanoparticles that are readily dispersible in water, and inhibited 24% and 64% of the AChE and BChE activity at 100 µM, respectively. GST activity was inhibited at 30 µM while MAO-A and B activity were inhibited at 100 µM. CurSD showed cytotoxicity against all the tested tumor cell lines without toxic effects for non-tumor cells. No cytotoxic and genotoxic potential was detected with the Allium cepa test. CurSD maintained the characteristics of free curcumin on the in vitro modulation of important enzymes without appreciable toxicity.

Assuntos

Antioxidantes/farmacologia , Carcinógenos/farmacologia , Curcumina/farmacologia , Mutagênicos/farmacologia , Animais , Linhagem Celular Tumoral , Formas de Dosagem , Inibidores Enzimáticos/farmacologia , Hemólise/efeitos dos fármacos , Humanos , Camundongos , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Cebolas/efeitos dos fármacos , Oxirredução , Células RAW 264.7 , Ratos , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo

RESUMO

Beta-carotene is a carotenoid precursor of vitamin A, known for its biological activities. Due to its high hydrophobicity, nanonization processes, i.e. the transformation into nanoparticles, can improve its water affinity, and therefore the activity in aqueous systems. The objective of this study was to produce beta-carotene nanoparticles by the solid dispersion method and to evaluate their effects on the activity of glutathione-S-transferase and acetylcholinesterase enzymes using Drosophila melanogaster (DM) homogenate, the superoxide dismutase- and catalase-like activities under in vitro conditions, and their cytotoxic properties against tumor and non-tumor cells. The formed nanometric beta-carotene particles resulted in stable colloids, readily dispersed in water, able to modulate acetylcholinesterase (AChE) activity, and presenting high potential to control the cholinergic system. Beta-carotene nanoparticles, at concentrations much lower than the pure pristine beta-carotene, presented in vitro mimetic activity to superoxide dismutase and altered glutathione-S-transferase activity in DM tissue. The content of hydrogen peroxide was neither affected by the nanoparticles (in aqueous solution) nor by pristine beta-carotene (in DMSO). In the cytotoxic assays, beta-carotene nanoparticles dispersed in water showed activity against four different tumor cell lines. Overall, beta-carotene nanoparticles presented significant bioactivity in aqueous medium surpassing their high hydrophobicity constraint.

Assuntos

Antioxidantes/farmacologia , Proteínas de Drosophila/metabolismo , Drosophila melanogaster/efeitos dos fármacos , Drosophila melanogaster/enzimologia , beta Caroteno/farmacologia , Animais , Antioxidantes/química , Catalase/metabolismo , Linhagem Celular Tumoral , Drosophila melanogaster/genética , Glutationa Peroxidase/metabolismo , Humanos , Interações Hidrofóbicas e Hidrofílicas , Nanopartículas/química , Superóxido Dismutase/metabolismo , beta Caroteno/química

RESUMO

Food by-products containing bioactive substances have attracted attention due to the possibility of adding values to residues of the food industry. In this work, the extraction of phenolic compounds from pinhão seed coats (Araucaria angustifolia (Bertol.) Kuntze) using a central composite rotatable design was applied to obtain prediction models for the extract volume yield, total phenolic content, total phenolic acids and total flavonoids. Principal component analysis and hierarchical cluster analysis were implemented showing an evident poor effect of the temperature on phenolic compounds extraction, which is in accordance with the prediction model obtained by the experimental design for total phenolic acids. Volume yield presented a high positive correlation with extraction temperature, followed by solvent composition. Scanning electron microscopy showed that higher temperatures and lower ethanol percentages resulted in highly defibrillated pinhão coats that retained more extract after the extraction process, leading to lower volume yield percentages.

Assuntos

Antioxidantes/química , Fracionamento Químico/métodos , Extratos Vegetais/química , Traqueófitas/química , Antioxidantes/análise , Análise por Conglomerados , Etanol/química , Flavonoides/análise , Flavonoides/química , Flavonoides/isolamento & purificação , Fenóis/análise , Fenóis/química , Fenóis/isolamento & purificação , Análise de Componente Principal , Sementes/química , Solventes/química , Temperatura

RESUMO

Curcumin is the main curcuminoid found in turmeric rhizomes and is a strong candidate to formulate foodstuff with specific properties. Among various bioactive properties of curcumin, its antiinflammatory activity is remarkable; on the other hand, its low water solubility leads to low absorption. Thus, new formulations need to be developed to improve its efficacy, and encapsulation is a promising alternative strategy in this regard. The objective of the present study was to obtain curcumin-loaded polyvinylpyrrolidone (PVP) nanoparticles and evaluate their acute in vivo antiinflammatory activity. Nanoparticles were obtained by complexation using the solid dispersion technique, and the characterization of nanoparticles showed that curcumin and PVP formed an amorphous solid solution. Encapsulated curcumin was colloidally stable in distilled water; this was attributed to the formation of hydrogen bonds between curcumin hydroxyl and PVP carbonyl groups. Rats were treated orally with single doses of curcumin and curcumin-loaded PVP nanoparticles, and antiinflammatory activity was evaluated by an experimental model of carrageenan-induced paw edema, myeloperoxidase (MPO) activity, and microcirculation in situ. Treatment with nanoparticles at 12.5 mg kg-1 significantly reduced the intensity of edema and MPO activity, whereas pure curcumin only presented a significant effect at 400 mg kg-1. Curcumin inhibited cell migration since rolling and adherent leukocytes were significantly reduced using nanoparticles at 50 mg kg-1 and curcumin at 400 mg kg-1. Compared to free curcumin, encapsulated curcumin was effective at lower doses; this might be due to the improved water affinity and colloidal stability of curcumin nanoparticles.

Assuntos

Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Curcumina/administração & dosagem , Curcumina/química , Edema/tratamento farmacológico , Animais , Portadores de Fármacos/química , Avaliação Pré-Clínica de Medicamentos , Edema/imunologia , Humanos , Ligação de Hidrogênio , Masculino , Nanopartículas/química , Tamanho da Partícula , Ratos , Ratos Wistar , Solubilidade

RESUMO

Lutein is a xanthophyll carotenoid widely known by its biological properties and low toxicity. When located in the brain, lutein may inhibit damage mechanisms, acting in neural cells maintenance. However, this carotenoid is very sensitive to external agents such as heat, light, pH and oxidation, besides presenting low absorption in gastrointestinal tract due its low solubility in water. Encapsulation procedures have shown promising results to increase lutein stability and bioavailability. In this work, lutein was encapsulated in polyvinylpyrrolidone (PVP) matrix by the dissolution in common solvent method. Nanoparticles were characterized in respect to morphology, water solubility, and interactions between PVP and lutein. In vivo tests were carried out in order to investigate the influence of lutein encapsulation on mice's declarative memory. Ex vivo tests were also carried out to determine if nanoparticles may cause any inflammatory process per se. Results indicated that lutein was successfully encapsulated in PVP while nanoparticles presented spherical shape and uniform size. Encapsulation was able to increase water solubility of lutein by more than 43 times, which may be attributed to the formation of soluble complexes trough hydrogen bonds between lutein hydroxyl group and PVP carbonyl group. In vivo studies showed that the administration of free lutein at 100mg·kg-1 and lutein-loaded PVP nanoparticles at 10 and 1.5mg·kg-1 significantly increased mice's object recognition index, meaning that significant lower doses of lutein were needed to achieve the same effect when lutein was encapsulated. Ex vivo studies showed that lutein-loaded nanoparticles administration did not alter inflammatory parameters in plasma, liver and brain of mice. In this sense, lutein-loaded PVP nanocapsules showed to be an advantageous alternative to increase water solubility and to improve the memory of mice without causing inflammatory damage per se.

Assuntos

Nanopartículas , Animais , Disponibilidade Biológica , Luteína , Camundongos , Povidona , Solubilidade