RESUMO
This study evaluated the most appropriate conditions (pH and biopolymers ratio) for the formation of the complex between ß-lactoglobulin (ß-lg) and sodium alginate (NaAlg). Furthermore, we microencapsulated black pepper essential oil (EO) using these biopolymers and transglutaminase as a cross-linking agent, and stability during in vitro digestion and its release in food models were studied. A ratio of 17:1 (ß-lg/NaAlg) at a pH of 4.5 was the optimal condition for the formation of the complex. The encapsulation efficiency (85.01% ± 0.26) and chemical and morphological characteristics suggested that black pepper EO was microencapsulated using polymers and cross-linking agent naturals. The particle size demonstrated that the capsules produced were on micro scale. The black pepper EO microcapsules lost lower release in water, and the Rigger-Peppas model indicated that the Fickian diffusion mechanism occurred. The microcapsules demonstrated a low release of black pepper EO during oral and gastric digestion and a higher release in intestinal digestion. The black pepper EO after digestion presented high stability (84.8% ± 0.07), and bioaccessibility (31.16% ± 0.3). The results suggest that the black pepper EO was microencapsulated and, preserved in aqueous food model and during oral and gastric conditions tested in vitro.
Assuntos
Alginatos/química , Composição de Medicamentos , Lactoglobulinas/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Piper nigrum/química , Biopolímeros/química , Calorimetria , Cápsulas , Digestão , Estabilidade de Medicamentos , Esvaziamento Gástrico/efeitos dos fármacos , Fármacos Gastrointestinais/química , Fármacos Gastrointestinais/farmacologia , Concentração de Íons de Hidrogênio , Tamanho da Partícula , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
Taxifolin possesses gastroprotective property but is characterized by low water solubility, is instabile in alkaline medium, and is degraded by the intestinal bacteria flora. The purpose of the work was therefore to produce a gastroadhesive formulation to prolong taxifolin residence time and release in the stomach. We first demonstrated that taxifolin is stable in simulated gastric fluid with or without pepsin and mucus, and is able to cross pig gastric mucus layer and stomach mucosa. Next, gastromucoadhesive microparticles composed of Syloid® AL-1 mesoporous silica, chitosan and HPMC were produced using spray-drying. Microparticles were characterized by a spherical shape and a mean volume-equivalent diameter around 12 µm. The optimized microparticles were able to release taxifolin and to adhere to pig stomach mucosa for 5 h.
Assuntos
Quitosana/química , Portadores de Fármacos/química , Fármacos Gastrointestinais/química , Quercetina/análogos & derivados , Adesividade , Animais , Liberação Controlada de Fármacos , Excipientes/química , Mucosa Gástrica/metabolismo , Microtecnologia , Mimusops/química , Tamanho da Partícula , Permeabilidade , Quercetina/química , Sementes/química , Dióxido de Silício/química , SuínosRESUMO
Lectins are proteins able to interact specifically and reversibly with carbohydrates. They are present in all living beings, particularly in legume seeds, which have many biological functions. The aim of this study was to isolate, characterize and verify antioxidant, anti-hemolytic, antitumor and gastroprotective activities in a lectin present in seeds of Phaseolus lunatus L. var. cascavel (PLUN). The isolation of lectin was performed by size exclusion chromatography on Sephadex G-100, which was isolated from a protein capable of agglutinating only human erythrocytes type A, being this the only inhibited haemagglutination n-acetyl-d-galactosamine. Its weight was estimated by PAGE is 128kDa. The lectin is thermostable up to 80°C and is active between pH 2-11. As 8M urea was able to denature the lectin. PLUN is a glycoprotein consisting of 2% carbohydrate and has antioxidant action with ascorbic acid equivalent antioxidant capacity (µMAA/g) of 418.20, 326 and 82.9 for total antioxidant activity, ABTS radical capture and capture of DPPH radical, respectively. The lectin has antitumor activity against melanoma derived cells at doses of 100 and 50mg/ml, reducing up to 83% tumor cells, and gastroprotective action, reducing up to 63% damaged area of ââthe stomach induced by ethanol.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Fármacos Gastrointestinais/farmacologia , Phaseolus/química , Lectinas de Plantas/farmacologia , Úlcera Gástrica/tratamento farmacológico , Acetilgalactosamina/química , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Benzotiazóis/antagonistas & inibidores , Benzotiazóis/química , Compostos de Bifenilo/antagonistas & inibidores , Compostos de Bifenilo/química , Linhagem Celular Tumoral , Eritrócitos/efeitos dos fármacos , Etanol , Fármacos Gastrointestinais/química , Fármacos Gastrointestinais/isolamento & purificação , Testes de Hemaglutinação , Humanos , Masculino , Camundongos , Peso Molecular , Picratos/antagonistas & inibidores , Picratos/química , Lectinas de Plantas/química , Lectinas de Plantas/isolamento & purificação , Desnaturação Proteica , Sementes/química , Extração em Fase Sólida/métodos , Estômago/efeitos dos fármacos , Estômago/patologia , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/patologia , Ácidos Sulfônicos/antagonistas & inibidores , Ácidos Sulfônicos/química , Ureia/químicaRESUMO
Pancreatin is a biotechnological product containing an enzyme complex, obtained from porcine pancreas, that is employed in treating pancreatic diseases. Experiments regarding the stability of the pharmaceutical formulation containing pancreatin were performed using standard binary mixtures with 6 excipients in a 1:1 ratio (m/m) and a commercial formulation. To accomplish these goals, samples were stored for 1, 3 and 6 months at 40 ± 1 °C and 75 ± 5 % relative humidity (RH) and 40 ± 1 °C and 0 % RH. Stress testing was also performed. All samples were analyzed to evaluate the α-amylase, lipase and protease activities through UV/Vis spectrophotometry. The results revealed that the excipient proprieties and the storage conditions affected enzyme stability. Humidity was a strong influencing factor in the reduction of α-amylase and protease activities. Stress testing indicated that pH 9.0 and UV light did not induce substantial alterations in enzyme activity.
Assuntos
Excipientes/química , Fármacos Gastrointestinais/metabolismo , Pancreatina/metabolismo , Animais , Brasil , Química Farmacêutica , Estabilidade de Medicamentos , Armazenamento de Medicamentos , Estabilidade Enzimática , Fármacos Gastrointestinais/química , Guias como Assunto , Temperatura Alta/efeitos adversos , Umidade/efeitos adversos , Concentração de Íons de Hidrogênio , Lipase/química , Lipase/metabolismo , Oxirredução , alfa-Amilases Pancreáticas/química , alfa-Amilases Pancreáticas/metabolismo , Pancreatina/química , Peptídeo Hidrolases/química , Peptídeo Hidrolases/metabolismo , Pós , Sus scrofa , Raios Ultravioleta/efeitos adversosRESUMO
Peppermint (Mentha piperita) infusions represent an important source of bioactive compounds with health benefits, which can be enhanced by applying salicylic acid (SA) during plant cultivation. The aim of this study was to evaluate the effect of SA (0, 0.5 and 2 mM) during peppermint cultivation on the chemical profile of saponins and alkaloids, as well as the anti-diabetic properties of the resulting infusions. The results showed that a 2 mM SA treatment significantly improved the chemical profiles of the infusions. Furthermore, the administration of 2 mM SA-treated peppermint infusions for 4 weeks to a high-fat diet/streptozotocin-induced diabetic rats decreased serum glucose levels (up to 25%) and increased serum insulin levels (up to 75%) as compared with the diabetic control. This can be related to the observed protection on pancreatic ß-cells. Furthermore, 0.5 and 2 mM SA-treated peppermint infusions decreased LDL (24 and 47%, respectively) and increased HDL levels (18 and 37%, respectively). In addition, all groups treated with peppermint infusions had lower serum and liver triglyceride contents, where 2 mM SA peppermint infusion showed the highest effect (44% and 56%, respectively). This is probably caused by its higher capacity to inhibit pancreatic lipase activity and lipid absorption. Moreover, SA-treated peppermint infusions improved the steatosis score in diabetic rat liver and decreased serum transaminase levels, probably as a result of the increase in steroidal saponins and alkaloids, such as trigonellin. Therefore, the application of 2 mM SA during cultivation of peppermint could be used to improve the anti-diabetic properties of peppermint infusions.
Assuntos
Diabetes Mellitus Experimental/dietoterapia , Suplementos Nutricionais , Fertilizantes , Hipoglicemiantes/uso terapêutico , Mentha piperita/química , Extratos Vegetais/uso terapêutico , Ácido Salicílico/metabolismo , Animais , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/complicações , Diabetes Mellitus Experimental/patologia , Suplementos Nutricionais/análise , Inibidores Enzimáticos/química , Inibidores Enzimáticos/uso terapêutico , Fármacos Gastrointestinais/química , Fármacos Gastrointestinais/uso terapêutico , Hiperlipidemias/complicações , Hiperlipidemias/prevenção & controle , Hipoglicemiantes/química , Insulina/agonistas , Insulina/sangue , Insulina/metabolismo , Secreção de Insulina , Ilhotas Pancreáticas/metabolismo , Ilhotas Pancreáticas/patologia , Lipase/antagonistas & inibidores , Lipase/metabolismo , Fígado/patologia , Masculino , Mentha piperita/crescimento & desenvolvimento , Mentha piperita/metabolismo , México , Hepatopatia Gordurosa não Alcoólica/complicações , Hepatopatia Gordurosa não Alcoólica/prevenção & controle , Obesidade/complicações , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/crescimento & desenvolvimento , Folhas de Planta/metabolismo , Distribuição Aleatória , Ratos WistarRESUMO
The therapeutic action of phosphorylated mannanoligosaccharides (MOS) was investigated regarding its prebiotic activity on enteropathogenic Escherichia coli (EPEC). Diarrhea was induced in dogs by experimental infection with EPEC strains. Then MOS was supplied once a day, in water for 20 days. Immunological (IgA and IgG), hematological (lymphocytes, neutrophils and monocytes) and bacteriological variables (PCR detection of the eae gene of EPEC recovered from stool culture), as well as occurrence of diarrhea were evaluated. All strains caused diarrhea at 24, 48 and 72 h after infection. PCR results indicated that E. coli isolated from stool culture of all infected animals had the eae gene. There was no significant difference among groups as to number of blood cells in the hemogram and IgA and IgG production. MOS was effective in recovering of EPEC-infected dogs since prebiotic-treated animals recovered more rapidly from infection than untreated ones (p < 0.05). This is an important finding since diarrhea causes intense dehydration and nutrient loss. The use of prebiotics for humans and other animals with diarrhea can be an alternative for the treatment and prophylaxis of EPEC infections.
Assuntos
Sangue/imunologia , Diarreia/microbiologia , Escherichia coli Enteropatogênica/imunologia , Fezes , Fármacos Gastrointestinais/metabolismo , Oligossacarídeos/metabolismo , Prebióticos , Animais , Anticorpos Antibacterianos/sangue , Fenômenos Químicos , Modelos Animais de Doenças , Cães , Escherichia coli , Fármacos Gastrointestinais/administração & dosagem , Fármacos Gastrointestinais/química , Imunoglobulina A/sangue , Imunoglobulina G/sangue , Leucócitos/imunologia , Oligossacarídeos/administração & dosagem , Oligossacarídeos/químicaRESUMO
The therapeutic action of phosphorylated mannanoligosaccharides (MOS) was investigated regarding its prebiotic activity on enteropathogenic Escherichia coli (EPEC). Diarrhea was induced in dogs by experimental infection with EPEC strains. Then MOS was supplied once a day, in water for 20 days. Immunological (IgA and IgG), hematological (lymphocytes, neutrophils and monocytes) and bacteriological variables (PCR detection of the eae gene of EPEC recovered from stool culture), as well as occurrence of diarrhea were evaluated. All strains caused diarrhea at 24, 48 and 72 h after infection. PCR results indicated that E. coli isolated from stool culture of all infected animals had the eae gene. There was no significant difference among groups as to number of blood cells in the hemogram and IgA and IgG production. MOS was effective in recovering of EPEC-infected dogs since prebiotic-treated animals recovered more rapidly from infection than untreated ones (p < 0.05). This is an important finding since diarrhea causes intense dehydration and nutrient loss. The use of prebiotics for humans and other animals with diarrhea can be an alternative for the treatment and prophylaxis of EPEC infections.
Assuntos
Animais , Cães , Sangue/imunologia , Diarreia/microbiologia , Escherichia coli Enteropatogênica/imunologia , Fezes , Fármacos Gastrointestinais/metabolismo , Oligossacarídeos/metabolismo , Prebióticos , Anticorpos Antibacterianos/sangue , Fenômenos Químicos , Modelos Animais de Doenças , Escherichia coli , Fármacos Gastrointestinais/administração & dosagem , Fármacos Gastrointestinais/química , Imunoglobulina A/sangue , Imunoglobulina G/sangue , Leucócitos/imunologia , Oligossacarídeos/administração & dosagem , Oligossacarídeos/químicaRESUMO
The essential oil of Eucalyptus tereticornis (EOET) has pharmacological activities but their effects on the gastrointestinal tract are yet unknown. It possesses α- and ß-pinene as minor constituents, isomers largely used as food or drink additives. In this work, we studied their actions on gut motility. After feeding with a liquid test meal, conscious rats received perorally EOET, α-, or ß-pinene, and the fractional dye retention was determined. EOET and its constituents decreased the gastric retention. In anesthetized rats, pinenes increased gastric tonus, while enhancing the meal progression in the small intestine of conscious rats. Both α- and ß-pinene contracted gastric strips IN VITRO but relaxed the duodenum. Conversely, EOET relaxed both the gastric and duodenal strips. In conclusion, EOET accelerates the gastric emptying of liquid, and part of its action is attributed to the contrasting effects induced by α- and ß-pinene on the gut.
Assuntos
Compostos Bicíclicos com Pontes/farmacologia , Eucalyptus/química , Fármacos Gastrointestinais/farmacologia , Motilidade Gastrointestinal/efeitos dos fármacos , Monoterpenos/farmacologia , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Animais , Monoterpenos Bicíclicos , Fármacos Gastrointestinais/química , Fármacos Gastrointestinais/isolamento & purificação , Masculino , Monoterpenos/química , Monoterpenos/isolamento & purificação , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Óleos de Plantas/química , Óleos de Plantas/isolamento & purificação , Ratos , Ratos WistarRESUMO
BACKGROUND: Proton pump inhibitors (PPI) are the drugs of choice for treatment of gastroesophageal reflux disease (GERD). Omeprazole, the first PPI commercialized, is now available in different formulations. OBJECTIVES: To compare the efficacy of different omeprazole formulations on gastric acid secretion measured by intragastric and esophageal pH monitoring in patients with reflux esophagitis. METHODS: Prospective, open, randomized clinical trial involving H. pylori negative patients with typical symptoms of GERD. Patients were submitted to 24-h intragastric and esophageal pH studies during use of six different formulations of compounded and manufactured omeprazole. RESULTS: Thirty patients, 19 female, median age 55 years were studied. The intragastric pH was maintained below 4.0 for a median of 36.7% of total time in compounded group and 47.7% in manufactured group (p>0.05). There was also no statistical difference between the median percentage of time of pH below 4.0 in orthostatic and supine position in compounded and manufactured groups (30.1% and 49.6% and 28.8% and 55.2%, respectively). The esophageal pH was maintained below 4.0 for a median of 0.1% of total time in compounded group and 0.4% in manufactured group (p>0.05). In orthostatic position the median percentage of time of esophageal pH below 4.0 was 0.0% in both groups (p>0.05). In supine position, the median percentage of time of esophageal pH below 4.0 was 0.1% and 0.3% in compounded and manufactured groups, respectively (p>0.05). CONCLUSION: The omeprazole formulations studied (compounded and manufactured) showed similar control of gastric acid secretion and esophageal acid exposure in patients with reflux esophagitis.