Production of mucic acid from pectin-derived D-galacturonic acid: a review / 生物工程学报

Mucic acid is a hexaric acid that can be biosynthesized by oxidation of D-galacturonic acid, which is the main constituent of pectin. The structure and properties of mucic acid are similar to that of glucaric acid, and can be widely applied in the preparation of important platform compounds, polymers and macromolecular materials. Pectin is a cheap and abundant renewable biomass resource, thus developing a process enabling production of mucic acid from pectin would be of important economic value and environmental significance. This review summarized the structure and hydrolysis of pectin, the catabolism and regulation of D-galacturonic acid in microorganisms, and the strategy for mucic acid production based on engineering of corresponding pathways. The future application of mucic acid are prospected, and future directions for the preparation of mucic acid by biological method are also proposed.

Preparação e caracterização de nanocarreadores de beta-lactose à base de pectina e lisozima / Preparation and characterization of beta-lactose nanocarriers based on pectin and lysozyme

O objetivo deste trabalho foi preparar e caracterizar nanocarreadores via auto-organização a partir da pectina de citros e lisozima para o encapsulamento da ß-lactose. Foram estudadas três condições de interação entre os biopolímeros variando a razão molar pectina/lisozima (3:1, 2:1, 1:1, 1:2 e 1:3), o pH e o tempo de aquecimento. A confirmação da interação foi determinada por espectroscopia no infravermelho por transformada de Fourier (FTIR) e por calorimetria de varredura diferencial (DSC). Os espectros de infravermelho evidenciaram que ligações de hidrogênio foram as principais forças envolvidas na formação dos nanocarreadores e sugeriram a ausência de ß-lactose livre na superfície das nanopartículas. Os termogramas evidenciaram que as nanopartículas formadas na presença de ß-lactose têm maior estabilidade térmica do que as nanopartículas sem ß-lactose. Para ambas as formulações estudadas, na presença e na ausência de ß-lactose, a formação das nanopartículas ocorreu entre os valores de pKa e ponto isoelétrico (pI) da pectina e lisozima, respectivamente, sendo a melhor razão de interação pectina/lisozima 1:2, em pH 10, a 80 ºC por 30 min. As nanopartículas foram formadas via auto-organização e todos as partículas apresentaram distribuição de tamanho homogênea, formato esférico, diâmetro inferior a 100 nm e carga superficial negativa. A morfologia e o tamanho das partículas pouco alteraram com a incorporação da -lactose. A eficiência de encapsulação (EE) da ß-lactose foi superior a 96% para as concentrações estudadas. Ensaios preliminares in vitro, em células epiteliais de câncer de cólon (HCT-116), evidenciaram que as nanopartículas formadas são capazes de adentrar no meio intracelular, possivelmente, por via endocitose

This work aimed to prepare and characterize nanocarriers via self-assembly using citrus pectin and lysozyme for ß-lactose encapsulation. Three interaction conditions between the biopolymers were studied, varying the pectin/lysozyme molar ratio (3:1, 2:1, 1:1, 1:2 and 1:3), pH and heating time. Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) determined the interaction's confirmation. The infrared spectra showed that hydrogen bonds were the main forces involved in the formation of nanocarriers and suggested the absence of free ß-lactose on the surface of the nanoparticles. The thermograms showed that nanoparticles formed in the presence of ß-lactose have greater thermal stability than nanoparticles without ß-lactose. For both formulations studied, in the presence and absence of lactose, the formation of nanoparticles occurred between the pKa and isoelectric point (pI) values of pectin and lysozyme, respectively, with the best pectin/lysozyme interaction molar ratio 1:2, at pH 10, at 80 °C for 30 min. Nanoparticles were formed via self-assembly, and all particles presented homogeneous size distribution, spherical shape, diameter less than 100 nm, and negative surface charge. The morphology and size of the particles changed little with the incorporation of ß-lactose. The encapsulation efficiency (EE) of ß-lactose was higher than 96% for the concentrations studied. Preliminary in vitro assays in colon cancer epithelial cells (HCT-116) showed that the nanoparticles formed are capable of entering the intracellular medium, possibly via endocytosis

Optimization of pectin extraction from selected Philippine fruit peel wastes using Box-Behnken design

Background@#Pectin is a pharmaceutically relevant excipient that can be upcycled from selected Philippine fruit peel wastes. Method optimization of pectin extraction leads to maximizing yields from limited resources, while also reducing environmental wastes, and providing local alternative sources. @*Objectives@#This study aimed to optimize the method of extracting pectin from selected Philippine fruit peel wastes using the Box-Behnken design, by varying the acid extraction solvent, treatment time, and working temperature. @*Methodology@#The three-level (-1, 0, 1) Box-Behnken design (15 set-ups) was used to optimize the pectin extraction in each of the fruit peel samples (C. maxima; A. heterophyllus; ripe and unripe M. indica; D. zibethinus; and H. undatus). The three experimental factors were the type of 3N acid used as extracting solvent (HNO₃, H₂SO₄, and HCl); duration of treatment in minutes (60, 90, and 120); and temperature of treatment in C 60, 75, and 90). The %yield was computed in each set-up, and the projected yields were generated using multiple linear regression. The pectin samples obtained from the optimized conditions were subjected to the physicochemical characterization, with apple pectin as the standard. Degree of esterification (DE), equivalent weight (EW), methoxy content (MC), alkalinity of ash (AA), and anhydrouronic acid content (AUA) were performed. @*Results@#Maximum yields were extracted from C. maxima (28.96%), A. heterophyllus (20.12%), ripe M. indica (26.23%), and unripe M. indica (25.89%), using 3N H₂SO₄, for a treatment duration of 60 minutes, at a working temperature of 90 C, and H. undatus (25.03%) at 60 C, for a treatment duration of 120 minutes. @*Conclusion@#Optimum conditions were identified to extract pectin in each of the fruit peel samples. The 3N H₂SO₄ produced the highest pectin yields in all of the set-ups, while the treatment time and working temperature vary per fruit peel sample. Pectin extract from C. maxima, A. heterophyllus, and M. indica was comparable to the standard.

Supplementation with different non-fiber carbohydrate sources in dairy cow diets with high or low rumen-undegradable protein content / Suplementação com diferentes fontes de carboidratos não fibrosos em dietas para vacas leiteiras com alto ou baixo teor de proteína não degradável no rúmen

The objective for this study was to evaluate the supplementation with different non-fibrous carbohydrate (NFC) sources for grazing dairy cows in diets with high or low concentrations of rumen undegradable protein (RUP). Twelve multiparous cows averaging 30kg/d of milk production and 45±23 days in milk in a 4x4 Latin square design with 2 × 2 factorial arrangement were used. The difference in NFC content of the diets was achieved using ground corn (GC) or dried citrus pulp (DCP). Dietary RUP was altered by the partial replacement of soybean meal (LRUP) by roasted whole soybean and corn gluten meal (HRUP). Greater dry matter intake (DMI) was observed in DCP treatments compared to GC treatments (19.2 and 17.7kg/day of DM, respectively). Milk fat concentration was lower for LRUP treatments (3.4%) when compared to HRUP (3.6%). The milk protein concentration was greater for GC treatments (2.9%) in relation to DCP treatments (2.8%). Lower milk ureic nitrogen was observed when DCP diets were fed compared to those with GC (17.8 and 21.2mg/dL, respectively). The use of DCP as CNF source increased dry matter intake as well as milk fat concentration, although no differences in milk production were observed for RUP level.(AU)

Objetivou-se avaliar a suplementação com diferentes fontes de carboidratos não fibrosos (CNF) em vacas manejadas a pasto em dietas com alta ou baixa concentração de proteína não degradável no rúmen (PNDR). Doze vacas multíparas com média de 30kg leite/ dia e 45±23 dias em lactação foram utilizadas em delineamento quadrado latino 4x4 com arranjo fatorial 2 × 2. As fontes de CNF foram milho moído (MM) e polpa cítrica seca (PC). A PNDR da dieta foi alterada pela substituição parcial do farelo de soja da dieta de baixa PNDR (BPNDR) por grão de soja tostado e farelo de glúten de milho dieta de alta PNDR (APNDR). Foi observado maior consumo de matéria seca (CMS) nos tratamentos com PC quando comparado aos tratamentos com MM (19,2 e 17,7kg / dia de MS, respectivamente). O teor de gordura do leite foi menor para os tratamentos com BPNDR (3,4%) em comparação aos tratamentos com APNDR (3,6%). O teor de proteína do leite foi maior nos tratamentos com MM (2,9%) em relação aos tratamentos com PC (2,8%). Foram observados menores teores de nitrogênio ureico no leite dos animais alimentados com PC em relação aos com MM (17,8 e 21,2mg / dL, respectivamente). O uso de PC como fonte de CNF aumentou o consumo de matéria seca, bem como o teor de gordura do leite, embora não tenham sido observadas diferenças na produção de leite relacionada a alteração nos teores de PNDR.(AU)

Avaliação da atividade imunomoduladora das pectinas in natura e modificadas obtidas de goiabas / Evaluation of immunomodulatory activity of non-modified and modified pectins from guava fruit

As pectinas presentes nas frutas, assim como sua versão modificada, estão entre as biomoléculas mais promissoras no campo da imunomodulação. Este estudo teve como objetivo avaliar o potencial imunomodulador de pectinas obtidas de goiabas verdes e maduras, bem como suas versões modificadas. As goiabas cv. Tailandesas foram avaliadas ao longo do amadurecimento, sendo acompanhadas as alterações da cor da polpa e casca, firmeza, produção de etileno e respiração, perda de massa e o teor de açúcares solúveis. Após a caracterização dos frutos, foram extraídas as pectinas e estas foram caracterizadas quanto ao conteúdo monossacarídico, peso molecular, presença de oligossacarídeos e grau de esterificação. As pectinas in natura de goiaba madura e verde, bem como a versão modificada desta última apresentaram frações de alto e baixo peso molecular, alta proporção de ácido galacturônico e alto teor de esterificação. Por outro lado, as pectinas modificadas derivadas de goiaba madura apresentaram maior desesterificação, com perda de frações de menor peso molecular, menor proporção de ácido galacturônico e baixo teor de esterificação. As pectinas foram incubadas com células THP-1 e RAW 264.7, e apesar da alta viabilidade celular e ausência de efeito citotóxico, resultou em expressiva produção de espécies reativas de oxigênio. De modo geral, as pectinas in natura de goiaba verde e madura, e pectina modificada de goiaba verde promoveram estímulo da produção de citocinas diversas, em especial inflamatórias, como IL-1ß, IL-12, CCL5, CXCL10 e CXCL9, para células THP-1 e IL-10 (antiinflamatória), TNF-α e MCP-1, demonstrando seu potencial imunomodulador, já para células RAW 264.7 as pectinas estimularam a produção de IL-10, TNF-α e MCP-1, demonstrando seu potencial imunomodulador. A pectina modificada derivada da goiaba madura não promoveu a indução significativa de nenhuma citocina. Estes resultados sugerem que as pectinas obtidas a partir de goiabas têm potencial imunomodulador e devem ser estudadas em outros modelos celulares e / ou em concentrações mais altas e modelos in vivo, para que esses benefícios possam realmente ser comprovados

The pectin present in fruits and their modified version are the most promising biomolecules in the immunomodulatory field. This study aimed to evaluate the immunomodulatory potential of pectins obtained from unripe and ripe guavas (Psidium guajava L.) cv. Thailandesa as well as their modified versions. The guavas were characterized during ripening regarding cell wall solubilization, sugar content, firmness, mass loss and ethylene production rate and respiration during 10th following harvest. After fruit characterization, pectins were extracted and characterized for monosaccharide content, molecular weight, presence of oligosaccharides and degree of esterification. Pectins from unripe and ripe guava as well as the modified versions of pectins had high and low molecular weight fractions, a high proportion of galacturonic acid and high esterification content. On the other hand, modified pectins derived from ripe guava showed higher de-esterification, with loss of lower molecular weight fractions, a lower proportion of galacturonic acid and low esterification content. The pectins were incubated with THP-1 and RAW 264.7 cells, and despite the high cell viability and absence of cytotoxic effect, the treatment resulted in the expressive production of reactive oxygen species. In general, pectins from ripe and unripe guava and modified pectin from unripe guava stimulated the production of diverse cytokines, especially inflammatory cytokines, such as IL-1ß, IL 12, CCL5, CXCL10, and CXCL9, for THP-1, while IL-10 (anti-inflammatory), TNF-α and MCP-1 were stimulated in RAW 264.7 cells, demonstrating their immunomodulatory potential. Modified pectin derived from ripe guava did not promote any significant induction of the cytokines investigated. These results suggest that pectins obtained from guavas have immunomodulatory potential and deserve a more in-depth investigation using other cellular models and/or use of higher concentrations and in vivo models tests so their immunomodulatory benefits can be prove

Research progress in structure and function of pectin methylesterase / 生物工程学报

Pectin methylesterase (PME) is an important pectinase that hydrolyzes methyl esters in pectin to release methanol and reduce the degree of methylation of pectin. At present, it has broad application prospects in food processing, tea beverage, paper making and other production processes. With the in-depth study of PME, the crystal structures with different sources have been reported. Analysis of these resolved crystal structures reveals that PME belongs to the right-hand parallel β-helix structure, and its catalytic residues are two aspartic acids and a glutamine, which play the role of general acid-base, nucleophile and stable intermediate, in the catalytic process. At the same time, the substrate specificity is analyzed to understand the recognition mechanism of the substrate and active sites. This paper systematically reviews these related aspects.

Wet citrus pulp in finishing diets for feedlot lambs: performance and hepatic enzyme concentration / Polpa cítrica úmida na terminação de cordeiros confinados: desempenho e concentração de enzimas hepáticas

Pectin industry generates a citrus pulp residue compounded by peduncle, endocarp, juice vesicles, columella, seeds and tiny fractions of epicarp and mesocarp of citrus fruits, denominated Wet Citrus Pulp (WCP), which has not yet been tested as food for lamb's nutrition. Thus, this study aimed to determine the effect of partial replacement of ground corn by WCP in high-concentrate diets on the performance and hepatic enzyme concentration of feedlot lambs. Forty-two male lambs (15 Santa Inês and 27 ½ Dorper × Santa Inês), with 24.7 ± 1.5 kg of BW and 60 ± 5 d of age was assigned to a randomized complete block design. Within blocks (n = 14), lambs were randomly assigned to 1 of 3 treatments: 0WCP (control) ­ diet containing 75.5% ground corn without WCP; 20WCP ­ diet containing 20% WCP in replacement of ground corn, and 40WCP ­ diet containing 40% WCP in replacement of ground corn. The experiment lasted 70 days, which was split in 3 experimental periods (14 days of diets' adaptation and 2 sub-periods of 28 days each). Statistical analyses were performed using the MIXED procedure of the SAS. Orthogonal polynomials for diet response were determined by linear and quadratic effects. There was a quadratic effect for DM, CP, ash, ether extract and NFC intake The highest DM and CP intake was observed for lambs fed 20WCP, however, the control diet increased the ash, ether extract and NFC intake. The increased levels of WCP decreased the ADG and feed efficiency (FE) during the adaptation period, however, did not affect the ADG and FE on periods 1 and 2. Consequently, the increased levels of WCP inclusion decreased linearly the BW. There was no effect of WCP inclusion in diets on Gamma-Glutamyl Transferase (GGT) concentration. However, there was a linear increase for Aspartate Aminotransferase (AST) concentration during the adaptation period, but without difference in other periods. In conclusion, adding up to 40% of WCP in finishing diets for feedlot lambs decrease performance during adaptation period, compromising the final body weight, but without damages effects on liver enzymes.(AU)

A indústria de produção de pectina gera um resíduo composto por pedúnculo, endocarpo, vesículas de suco, columela, sementes e minúsculas frações de epicarpo e mesocarpo de frutas cítricas, denominada Polpa Cítrica Úmida (WCP), que ainda não foi testada como alimento na nutrição de ovinos. Sendo assim, este estudo teve como objetivo avaliar o efeito da substituição parcial do milho pela WCP em dietas contendo elevado teor de concentrado sobre o desempenho e a concentração de enzimas hepáticas de cordeiros confinados. Quarenta e dois cordeiros machos (15 Santa Inês e 27 ½ Dorper x Santa Inês), com 24,7 ± 1,5 kg de peso corporal e 60 ± 5 dias de idade foram distribuídos em delineamento de blocos completos casualizados. Dentro de cada bloco (n = 14), os cordeiros foram distribuídos aleatoriamente entre os tratamentos: 0WCP ­ dieta contendo 75,5% de milho moído, sem a inclusão de WCP; 20WCP ­ dieta contendo 20% de WCP em substituição ao milho moído; e 40WCP ­ dieta contendo 40% de WCP em substituição ao milho moído. O experimento teve duração de 70 dias, sendo dividido em 3 períodos experimentais (14 dias de adaptação as dietas e 2 períodos de 28 dias cada). As análises estatísticas foram realizadas utilizando o procedimento MIXED do SAS. Os polinômios ortogonais lineares e quadráticos foram utilizados para avaliar o efeito das dietas. Houve efeito quadrático para o consumo de matéria seca, PB, cinzas, extrato etéreo e CNF. A maior ingestão de MS e PB foi observada para os cordeiros alimentados com 20WCP, entretanto, a dieta controle aumentou o consumo de cinzas, extrato etéreo e CNF. O aumento na inclusão de WCP diminuiu o ganho médio diário e a eficiência alimentar durante o período de adaptação, entretanto, não afetou essas variáveis durante os períodos 1 e 2. Consequentemente, a inclusão de WCP reduziu o peso corporal ao final do período experimental. Não houve efeito das dietas na concentração de gama-glutamil transferase (GGT). Entretanto, houve aumento linear na concentração de aspartato aminotransferase (AST) durante o período de adaptação. Em conclusão, a inclusão de até 40% de WCP nas dietas de terminação para cordeiros confinados diminuiu o desempenho durante o período de adaptação, comprometendo o peso corporal ao final do período experimental, entretanto, não comprometeu a afetou as enzimas hepáticas.(AU)

Desenvolvimento de geléia de frutas para uso em queijo tipo coalho trufado / Fruit jelly development for use in cheese type coalho truffle

O trabalho foi realizado com o objetivo de desenvolver geleias de jenipapo e acerola, produzidas com 0,5 e 1,0% de pectina metoxilada, para recheio de queijo tipo coalho trufado. Foram avaliadas as características físico químicas, como pH, acidez total titulável, sólidos solúveis totais, umidade, cinzas e, ácido ascórbico. Após confecção dos queijos estes foram submetidos à análise sensorial através da aparência, cor, sabor e textura, bem como intenção de compra. A metodologia abordada para demonstração dos dados foi a estatística descritiva. O uso de geleias para recheio de queijo tipo coalho trufado tem potencial para exploração comercial, visto a manutenção das características organolépticas e de aceitabilidade pelo consumidor, sendo que o uso do queijo trufado com geleia de acerola demonstrou maior potencial de vida de prateleira.

Endophytic Actinomycetes as Potential Producers of Hemicellulases and Related Enzymes for Plant Biomass Degradation

Abstract Tailor made enzymatic preparation must be design to hydrolyze efficiently plant biomass, once that each plant biomass possesses a distinct cell wall composition. Most of actinomycetes used for plant cell wall degradation are focused on the cellulases and xylanases production. However, a wide range of enzymes must be produced for an efficient degradation of lignocellulose materials. During the last decade several unusual environments were studied to obtain strains that produce glycohydrolases with innovator characteristics. In this context, the present work concerned the selection of endophytic actinomycetes as producers of hemicellulases and related enzymes with different enzymatic profiles, for use in the deconstruction of lignocellulosic biomass. A total of 45 Brazilian actinomycetes previously isolated from plants (endophytics) and soil were prospected for hemicellulases and β-glucosidase production. Four strains highlighted for hemicellulase production (DR61, DR63, DR69 and DR66) and were selected for cultivation under other inductors substrates (xylan and pectin). All strains belong to Streptomyces genera and have their extracts tested for degradation of several hemicellulolytic substrates. The strains presented different glicohydrolyse enzymes profiles mainly for xylans and glucans that can be used for specific formulations of enzymes applied on the biomass deconstruction, principally on sugar cane bagasse.

Pectin lyase overproduction by Penicillium griseoroseum mutants resistant to catabolite repression

Abstract Expression of pectinolytic genes is regulated by catabolic repression limiting the production of pectin lyase (PL) if the natural inducer, pectin, is missing from the growth medium. Here, we report the isolation of Penicillium griseoroseum mutants resistant to 2-deoxy-d-glucose (DG) that show resistance to catabolite repression and overproduce PL. Three spontaneous and nine UV-induced mutants were obtained. Some mutants produced sectors (segments morphologically different) that were also studied. The mutants were analyzed for pectinases production on pectinase-agar plates and five mutants and two sectors showing larger clearing zones than the wild type were selected for quantitative assay. Although PL production higher than the wild type has been found, phenotype instability was observed for most of the mutants and, after transfers to nonselective medium, the DG resistance was no longer present. Only mutants M03 and M04 were stable maintaining the DG-resistance phenotype. When growing for 120 h in liquid medium containing glucose with or without pectin, both mutants showed higher PL production. In the presence of glucose as sole carbon source, the mutant M03 produced 7.8-fold more PL than the wild type. Due its phenotypic stability and PL overproduction, the mutant M03 presents potential for industrial applications.

Draft genome sequence of pectic polysaccharide-degrading moderate thermophilic bacterium Geobacillus thermodenitrificans DSM 101594

Abstract Geobacillus thermodenitrificans DSM 101594 was isolated as a producer of extracellular thermostable pectic polysaccharide degrading enzymes. The completely sequenced genome was 3.6 Mb in length with GC content of 48.86%. A number of genes encoding enzymatic active against the high molecular weight polysaccharides of potential biotechnological importance were identified in the genome.

Desenvolvimento e caracterização de filmes e comprimidos bucais a base de pectina e goma gelana para liberação tópica de triancinolona / Development and characterization of films and buccal tablets based on pectin and gellan gum for the topical release of triamcinolone

O tratamento farmacológico de patologias bucais é conduzido, geralmente, por via de administração local. No entanto, devido ao pouco tempo de permanência do fármaco no local de ação, esse tratamento pode ser bastante comprometido. Assim, este trabalho teve por objetivo o desenvolvimento de formas farmacêuticas que proporcionem a liberação local de triancinolona na cavidade oral. Foram produzidos filmes e comprimidos mucoadesivos a partir de polímeros naturais como gelana e pectina. Os filmes bucais foram preparados por meio de evaporação do solvente (solvent casting) utilizando diferentes quantidades de polímeros. As matérias-primas e os filmes foram caracterizados fisico quimicamente utilizando espectroscopia vibracional (in-infravermelho com transformada de Fourier e Raman) e difração de raios X. As propriedades físicas e mecânicas dos filmes também foram avaliadas. Além disso, realizou-se os ensaios de mucoadesividade e de dissolução do fármaco. Os comprimidos foram preparados por com-pressão direta usando como base os polímeros naturais. Diferentes parâmetros em relação as misturas e as formulações foram avaliados tais como as propriedades de fluxo dos pós constituintes, peso médio, dureza, friabilidade e desintegração. Em relação aos filmes bucais, estes foram obtidos com sucesso através de um método simples, sem a utilização de agentes reticulantes, ácidos ou solventes orgânicos. Todos apresentaram bons resultados nas propriedades avaliadas, no entanto as formulações com quantidades intermediarias de polímeros foram as melhores. Dentre as formulações de comprimidos preparadas, apenas 4 apresentaram boas características, no entanto, os resultados dos ensaios de dissolução mostraram que estas formulações têm capacidade de agir como sistema de liberação controlada de fármacos

Pharmacological treatment of oral pathologies is usually conducted by local administration. However, due to the short time the drug stays in the site of action, this treatment can be quite compromised. Thus, the objective of this work was to develop pharmaceutical forms that pro-vide the local release of triamcinolone in the oral cavity. Mucoadhesive films and tablets were made from natural polymers such as gellan and pectin. The buccal films were prepared by sol-vent casting using different amounts of polymers. The raw materials and films were characte-rized physically chemically using vibrational spectroscopy (FTIR and Raman) and X-ray diffraction. The physical and mechanical properties of the films were also evaluated. In addi-tion, the mucoadhesive and drug dissolution tests were performed. The tablets were prepared by direct pressing with the natural polymers. Different parameters in relation to mixtures and formulations were evaluated such as the flow properties of the constituent powders, average weight, hardness, friability and disintegration. In relation to oral films, these were successfully obtained by a simple method, without the use of crosslinking agents, acids or organic solvents. All presented good results in the evaluated properties, however the formulations with interme-diate amounts of polymers were the best. Among the tablet formulations prepared, only 4 sho-wed good characteristics, however, the dissolution test results showed that these formulations have the ability to act as a controlled drug delivery system

Desenvolvimento e caracterização de filmes e comprimidos bucais a base de pectina e goma gelana para liberação tópica de triancinolona / Development and characterization of films and buccal tablets based on pectin and gellan gum for the topical release of triamcinolone

O tratamento farmacológico de patologias bucais é conduzido, geralmente, por via de adminis-tração local. No entanto, devido ao pouco tempo de permanência do fármaco no local de ação, esse tratamento pode ser bastante comprometido. Assim, este trabalho teve por objetivo o de-senvolvimento de formas farmacêuticas que proporcionem a liberação local de triancinolona na cavidade oral. Foram produzidos filmes e comprimidos mucoadesivos a partir de polímeros naturais como gelana e pectina. Os filmes bucais foram preparados por meio de evaporação do solvente (solvent casting) utilizando diferentes quantidades de polímeros. As matérias-primas e os filmes foram caracterizados fisico quimicamente utilizando espectroscopia vibracional (in-fravermelho com transformada de Fourier e Raman) e difração de raios X. As propiedades físicas e mecânicas dos filmes também foram avaliadas. Além disso, realizou-se os ensaios de mucoadesividade e de dissolução do fármaco. Os comprimidos foram preparados por com-pressão direta usando como base os polímeros naturais. Diferentes parâmetros em relação as misturas e as formulações foram avaliados tais como as propriedades de fluxo dos pós consti-tuintes, peso médio, dureza, friabilidade e desintegração. Em relação aos filmes bucais, estes foram obtidos com sucesso através de um método simples, sem a utilização de agentes reticu-lantes, ácidos ou solventes orgânicos. Todos apresentaram bons resultados nas propriedades avaliadas, no entanto as formulações com quantidades intermediarias de polímeros foram as melhores. Dentre as formulações de comprimidos preparadas, apenas 4 apresentaram boas ca-racterísticas, no entanto, os resultados dos ensaios de dissolução mostraram que estas formula-ções têm capacidade de agir como sistema de liberação controlada de fármacos.

Pharmacological treatment of oral pathologies is usually conducted by local administration. However, due to the short time the drug stays in the site of action, this treatment can be quite compromised. Thus, the objective of this work was to develop pharmaceutical forms that pro-vide the local release of triamcinolone in the oral cavity. Mucoadhesive films and tablets were made from natural polymers such as gellan and pectin. The buccal films were prepared by sol-vent casting using different amounts of polymers. The raw materials and films were characte-rized physically chemically using vibrational spectroscopy (FTIR and Raman) and X-ray diffraction. The physical and mechanical properties of the films were also evaluated. In addi-tion, the mucoadhesive and drug dissolution tests were performed. The tablets were prepared by direct pressing with the natural polymers. Different parameters in relation to mixtures and formulations were evaluated such as the flow properties of the constituent powders, average weight, hardness, friability and disintegration. In relation to oral films, these were successfully obtained by a simple method, without the use of crosslinking agents, acids or organic solvents. All presented good results in the evaluated properties, however the formulations with interme-diate amounts of polymers were the best. Among the tablet formulations prepared, only 4 sho-wed good characteristics, however, the dissolution test results showed that these formulations have the ability to act as a controlled drug delivery system.

Pectina e cloreto de potássio na produção de presunto cozido / Pectin and potassium chloride in the production of cooked ham

No Brasil, as Doenças Cardiovasculares são as principais causas de morte, fenômeno que ocorre mundialmente. Dentre os fatores de risco considerados de maior importância para a aterosclerose estão: hipertensão arterial, dislipidemias,obesidade, diabetes mellitus e alguns hábitos relacionados ao estilo de vida, como dieta pobre em fibras e rica em calorias, gorduras saturadas, colesterol e sal (NaCl). A pectina é uma fibra dietética solúvel, podendo também ser classificada como fibra funcional, ou seja, que possui benefícios adicionais à saúde humana. Na fabricação de produtos cárneos, a pectina vem sendo avaliada em razão da capacidade de associação com moléculas de água, favorecendo a capacidade de retenção de água, aumentando o rendimento dos processos e melhorando a textura dos produtos. O cloreto de potássio (KCl) tem sido amplamente estudado como principal substituto do sal comum (NaCl), a fim de garantir alimentos voltados à população portadora de desordens no aparelho circulatório.

In Brazil, cardiovascular diseases are major causes of death, a phenomenon that occurs worldwide. Among the risk factors considered most important for atherosclerosis are hypertension, dyslipidemia, obesity, diabetes mellitus and certain habits related to lifestyle such as diet low in fiber and rich in calories, saturated fat, cholesterol and salt (NaCl). Pectin is a soluble dietary fiber, may also be classified as functional fiber, ie, which has additional benefits to human health. In the manufacture of meat products, the pectin is being evaluated because of the capacity of association with water molecules, by promoting water retention, increasing the efficiency of processes and improving the texture of products. Potassium chloride (KCl) has been widely studied as a main substitute for common salt (NaCl), to ensure foods aimed at people suffering from disorders of the circulatory system.

Influencia del tamaño de partícula y la velocidad de agitación sobre el rendimiento de pectina / Influence of the particle size and the stirring speed over the pectin yield

Introducción: el procesamiento de las hojas de sábila (Aloe barbadensis Mill) para la obtención de productos de interés agroalimentario como el gel, genera varios residuos, entre ellos el bagazo que se obtiene de la molienda de la pulpa. El mismo constituye un recurso económico para la obtención de componentes de amplio uso en las industrias alimentaria y farmacéutica, como la pectina, compuesto de interés por su alto poder gelificante, cuyo proceso de extracción más usado a nivel industrial es la hidrólisis ácida. La extracción de pectina a partir del bagazo de sábila se estudió a escala de laboratorio y se establecieron las condiciones de operación (temperatura, pH y tiempo de extracción) requeridas para maximizar el rendimiento de la pectina, sin embargo, falta estudiar la influencia de la velocidad de agitación y el tamaño de partícula. Objetivo: evaluar la influencia del tamaño de la partícula y la velocidad de agitación en el rendimiento de extracción de la pectina al utilizar la hidrólisis ácida. Métodos: se aplicó la técnica de hidrolisis ácida a escala de laboratorio para extraer pectina del bagazo de sábila. Los factores estudiados fueron: velocidad de agitación (300 y 1 000 min-1) y tamaño de partícula (0,250 y 0,600 mm). El resto de los parámetros se mantuvieron constante: tiempo de reacción (60 minutos), temperatura (90 °C), pH (1,5). La relación soluto/solvente fue fijada en 1:15 y 1:20 m/v, teniendo en cuenta el desarrollo experimental de cada tamaño de partícula. Resultados: las condiciones óptimas en el rango estudiado fueron velocidad de agitación de 1 000 min-1 y tamaño de partícula 0,600 mm y se obtiene un rendimiento de 3,80 por ciento de pectina por cada 5 g de muestra de bagazo seco. Conclusiones: es la velocidad de agitación la que ejerce una mayor influencia, aunque ambos factores resultaron significativos con un 95 por ciento de confiabilidad(AU)

Introduction: the processing of sabila leaves (Aloe barbadensis Mill) to obtain products of agricultural interest such as gel, generates various wastes, including bagasse obtained by grinding the pulp. Bagasse is an economic resource for the production of components widely used in the food and pharmaceutical industries like pectin, an interesting compound because of its high gellifying power and the most used extraction process at industrial level is acid hydrolysis. In particular, the pectin extraction from sabila bagasse was studied on a lab scale; and the operating conditions (temperature, pH and extraction time) required to maximize the pectin yield was established. However, the influence of the stirring speed and the particle size remained to be studied. Objective: to assess the influence of the particle size and the stirring speed on the extraction yield of pectin using acid hydrolysis. Methods: the acid hydrolysis technique was applied to extract pectin from the sabila bagasse. The studied factors were stirring rate (300 to 1 000 min-1) and particle size (0,250 to 0,600 mm). The rest of parameters remained unchanged: reaction time (60 minutes), temperature (90 °C) and pH (1.5). The solute/solvent ratio was set at 1:15 and 1:20 w/v, considering experimental behavior of each particle size. Results: the optimal conditions in the studied range were stirring rate 1 000 min-1 and particle size of 0,600 mm, reaching a pectin yield of 3,80 percent per 5 g sample o dry bagasse. Conclusions: the stirring rate the most influential although both factors were significant with 95 percent reliability(AU)

Efeito de polímeros naturais na conservação de banana CV Caturra / Effect of natural polymers in banana CV caturra conservation

Este trabalho teve como objetivo avaliar o efeito de filmes formados por pectina, albúmen de ovo, carragena, gelatina, fécula de batata, xantana e amido de milho na conservação de banana cv. Caturra. As bananas foram sanitizadas e imersas em soluções filmogênicas de pectina (2%), albúmen de ovo (100%), carragena (2%), gelatina (5%), fécula de batata (2%) com glicerol (0,7%), xantana (1%), amido de milho (2%) com glicerol (0,7%) e o controle (0%), sendo armazenadas a 18ºC a 80% de UR por 8 dias. As bananas revestidas foram avaliados de acordo com a perda de massa, taxa de perda de massa, sólidos solúveis totais, cor (luminosidade e croma b*) e firmeza, nos tempos de zero hora, 2, 6, 7 e 8 dias. Ao final do período de armazenamento as bananas cv Caturra revestidas com filmes de pectina promoveram menor perda de massa e se mantiveram dentro do limite permitido (7%) até os 4,9 dias. O revestimento com carragena mostrou menor aumento dos sólidos solúveis totais, já os filmes de albúmen proporcionaram menores reduções da firmeza e variações da coloração amarela e o revestimento com fécula de batata melhorou a luminosidade nos frutos. Este aspecto mostra uma contribuição dos filmes na manutenção da qualidade da banana cv. Caturra. No entanto, outros parâmetros de qualidade devem ser avaliados, buscando conhecer outros efeitos desses filmes sobre a banana.

Pectinas de plantas medicinais: características estruturais e atividades imunomoduladoras / Pectins of medicinal plants: structural characteristics and immunomodulatory activities

RESUMO As plantas medicinais apresentam várias propriedades terapêuticas, as quais estão relacionadas com a presença de compostos bioativos. Dentre os compostos, destacam-se as pectinas, que compreendem um grupo de polissacarídeos ácidos de relevante importância medicinal e nutracêutica. As pectinas são formadas por unidades de ácido galacturônico, unidas por ligação do tipo α-(1→4), sendo classificadas em homogalacturonanas e ramnogalacturonanas tipo I (RG-I) e tipo II (RG-II). Outros polissacarídeos constituídos por arabinose e/ou galactose têm sido isolados em associação com polissacarídeos pécticos, como as arabinogalactanas (AG) (tipo I e tipo II). As AG-II podem estar associadas a proteínas, denominadas de arabinogalactana-proteínas (AGPs). Inúmeros relatos demonstram que as pectinas, bem como as AG e AGPs, podem atuar como moduladores do sistema imunológico, sendo, por isso, consideradas modificadores da resposta biológica. A imunomodulação pode estar relacionada tanto com a atividade de macrófagos quanto com as vias do sistema complemento. Em geral, os polissacarídeos provocam um estímulo da atividade fagocitária; no aumento da produção de espécies reativas de oxigênio e da secreção de citocinas pró-inflamatórias. Em relação ao sistema complemento, os polissacarídeos podem modular tanto a via clássica como a via alternativa. A presente revisão tem como objetivo principal descrever os aspectos estruturais de pectinas e suas atividades biológicas relacionadas à modulação do sistema imune. Utilizando literatura específica, estão descritas informações de 29 espécies de plantas medicinais, que apresentam como constituintes pectinas, arabinogalactanas e/ou AGPs, correlacionando suas propriedades terapêuticas com as atividades biológicas associadas ao sistema imune. Na maioria dos casos descritos na literatura, é difícil determinar como as características estruturais específicas podem estar envolvidas na modulação da atividade de macrófagos. Porém, em relação à modulação da atividade do sistema complemento fica sugerido que a presença de estruturas tipo AG-II contribuiria mais significativamente para esta atividade. Entretanto, os possíveis mecanismos de modulação de pectinas, AGs e AGPs sobre a atividade de macrófagos e/ou sobre o sistema complemento ainda não estão totalmente esclarecidos, mesmo assim, estes polímeros podem ser considerados potenciais candidatos para estudos que visam ao desenvolvimento de novos agentes terapêuticos com propriedades moduladoras benéficas para o sistema imunológico.

ABSTRACT Medicinal plants have many therapeutic properties that are related to the presence of biologically active compounds. Pectins, a group of acid polysaccharides that have relevant medicinal and nutraceutical properties, are an example of such biological compounds. Pectins contain a main chain with galacturonic acid units that are α-(1→4) linked; they can be classified into homogalacturonans and type I and type II rhamnogalacturonans (RG-I and RG-II). Other polysaccharides containing arabinose, galactose, or both have been isolated in association with pectin-type polysaccharides are known as arabinogalactans (AGs, type I and type II). Arabinogalactan-proteins (AGPs) comprise AG-II associated with proteins. Several studies have reported that pectins, as well as AG and AGPs, can act as modulators of the immune system and can therefore be considered biological response modifiers. The immunomodulation is related to the activity of macrophages as on the complement system pathways. In general, polysaccharides cause stimulation of phagocytic activity, increase production of reactive oxygen species and secretion of pro-inflammatory cytokines. Polysaccharides can modulate the classical and alternative complement pathways. The aim of this review has to describe the structural aspects of pectins and their biological activities related to the modulation of the immune system. Using literature, we reported data of 29 medicinal plant species, which present as constituents pectins, arabinogalactan and/or AGPs, correlating their therapeutic properties with biological activities associated to the immune system. In most cases described in the literature, it is difficult to determine how the specific structural characteristics can be involved in modulation of macrophage activity. However, with respect to the modulation of the activity of the complement system is proposed that the presence of AG-II-type structures would contribute most significantly to this activity. The possible mechanisms of modulation of pectins, AGs and AGPs on macrophage activity and/or the complement system are not yet fully clear, even if, these polymers can be considered potential candidates for studies aimed at the development of new therapeutic agents with modulatory properties beneficial to the immune system.

Characterization of pectinase activity for enology from yeasts occurring in Argentine Bonarda grape

Pectinolytic enzymes are greatly important in winemaking due to their ability to degrade pectic polymers from grape, contributing to enhance process efficiency and wine quality. This study aimed to analyze the occurrence of pectinolytic yeasts during spontaneous fermentation of Argentine Bonarda grape, to select yeasts that produce extracellular pectinases and to characterize their pectinolytic activity under wine-like conditions. Isolated yeasts were grouped using PCR-DGGE and identified by partial sequencing of 26S rRNA gene. Isolates comprised 7 genera, with Aureobasidium pullulans as the most predominant pectinolytic species, followed by Rhodotorula dairenensis and Cryptococcus saitoi. No pectinolytic activity was detected among ascomycetous yeasts isolated on grapes and during fermentation, suggesting a low occurrence of pectinolytic yeast species in wine fermentation ecosystem. This is the first study reporting R. dairenensis and Cr. saitoi species with pectinolytic activity. R. dairenensis GM-15 produced pectinases that proved to be highly active at grape pH, at 12 °C, and under ethanol and SO₂ concentrations usually found in vinifications (pectinase activity around 1.1 U/mL). This strain also produced cellulase activity at 12 °C and pH 3.5, but did not produce β-glucosidase activity under these conditions. The strain showed encouraging enological properties for its potential use in low-temperature winemaking.