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BACKGROUND: Peripheral nerve injuries negatively impact the quality of life of patients, with no effective treatment available that accelerates sensorimotor recovery and promotes functional improvement and pain relief. The aim of this study was to evaluate the effects of diacerein (DIA) in an experimental mice model of sciatic nerve crush. METHOD: In this study, male Swiss mice were used, randomly separated into six groups as follows: FO (false-operated + vehicle); FO + DIA (false-operated + diacerein 30 mg/kg); SNI (sciatic nerve injury + vehicle); SNI + DIA in doses of 3, 10 and 30 mg/kg (sciatic nerve injury + treatment with diacerein in doses of 3-30 mg/kg). DIA or vehicle was administered 24 h after the surgical procedure, intragastrically, twice a day. The lesion of the right sciatic nerve was generated by crush. RESULTS: We found that the treatment of animals with DIA accelerated sensorimotor recovery of the animal. In addition, animals in the sciatic nerve injury + vehicle (SNI) group showed hopelessness, anhedonia, and lack of well-being, which were significantly inhibited by DIA treatment. The SNI group showed a reduction in the diameters of nerve fibers, axons, and myelin sheaths, while DIA treatment recovered all these parameters. In addition, the treatment of animals with DIA prevented an increase the levels of interleukin (IL)-1ß and a reduction in the levels of the brain-derived growth factor (BDNF). CONCLUSIONS: Treatment with DIA reduces hypersensitivity and depression like behaviors in animals. Furthermore, DIA promotes functional recovery and regulates IL-1ß and BDNF concentrations.
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Traumatismos dos Nervos Periféricos , Neuropatia Ciática , Camundongos , Masculino , Animais , Fator Neurotrófico Derivado do Encéfalo , Traumatismos dos Nervos Periféricos/tratamento farmacológico , Reposicionamento de Medicamentos , Qualidade de Vida , Neuropatia Ciática/tratamento farmacológico , Nervo Isquiático , Modelos Animais de DoençasRESUMO
Introdução: O Diabetes Mellitus Gestacional é uma das síndromes metabólicas mais comuns em gestantes e é caracterizada pela baixa tolerância à glicose, resultando em graves consequências materno-fetais. Objetivo: Traçar o perfil epidemiológico de gestantes atendidas na Atenção Primária à Saúde; elencar os fatores de risco sobre Diabetes Mellitus Gestacional entre gestantes atendidas na Atenção Primária à Saúde e analisar os conhecimentos de gestantes sobre Diabetes Mellitus Gestacional na Atenção Primária à Saúde. Metodologia: Estudo com abordagem quanti- qualitativa, descritiva e exploratória, realizado em uma Unidade de Saúde da Família na Bahia, com 15 gestantes maiores de 18 anos, em qualquer trimestre gestacional e que tivessem realizado ao menos uma consulta de pré-natal. A coleta dos dados foi feita através de um roteiro de entrevista semiestruturada e do acesso ao prontuário físico de cada participante. A análise dos dados do perfil foi feita por estatística descritiva simples e as questões abertas da entrevista pela técnica de conteúdo temática proposta por Bardin. Principais Resultados: Percebe-se que a maioria das gestantes era jovem, negra, possuía ensino médio, tinha mais de três filhos, encontrava-se no segundo trimestre gestacional e detinha baixa renda. Com relação aos fatores de risco, destacam-se o histórico familiar de diabetes mellitus, o sobrepeso/obesidade e o sedentarismo. Aponta-se ainda o desconhecimento total ou insuficiência nas informações sobre diabetes mellitus gestacional entre as participantes. Conclusão: O desconhecimento aliado aos fatores de risco evidenciados e à situação de vulnerabilidade social e econômica pode contribuir para o desenvolvimento do Diabetes Mellitus Gestacional na população estudada, sendo fundamental estratégias multidisciplinares para a sua prevenção e/ou controle.
Introduction: Gestational Diabetes Mellitus is one of the most common metabolic syndromes in pregnant women and is characterized by low glucose tolerance, resulting in severe maternal-fetal consequences. Objective: To trace the epidemiological profile of pregnant women attended in Primary Health Care; to list the risk factors about Gestational Diabetes Mellitus among pregnant women attended in Primary Health Care and to analyze the knowledge of pregnant women about Gestational Diabetes Mellitus in Primary Health Care. Methodology: A study with a quanti-qualitative, descriptive and exploratory approach, carried out in a Family Health Unit in Bahia, with 15 pregnant women over 18 years of age, in any gestational trimester and who had carried out at least one prenatal visit. The data collection was done through a semi-structured interview script and access to the physical records of each participant. The analysis of the profile data was done by simple descriptive statistics and the open questions of the interview by the thematic content technique proposed by Bardin. Main Results: It is noticed that most pregnant women were young, black, had high school, had more than three children, was in the second gestational trimester and had low income. With regard to risk factors, family history of diabetes mellitus, overweight/obesity and sedentary lifestyle are highlighted. It is also pointed out the total lack of knowledge or insufficiency in the information about gestational diabetes mellitus among the participants. Conclusion: The lack of knowledge coupled with the risk factors evidenced and the situation of social and economic vulnerability can contribute to the development of Gestational Diabetes Mellitus in the studied population, being fundamental multidisciplinary strategies for its prevention and/or control.
Introducción: La diabetes mellitus gestacional es uno de los síndromes metabólicos más comunes en mujeres embarazadas y se caracteriza por una baja tolerancia a la glucosa, lo que tiene graves consecuencias maternofetales. Objetivo: Seguir el perfil epidemiológico de las mujeres embarazadas a las que se presta atención primaria de la salud; enumerar los factores de riesgo de la diabetes mellitus gestacional entre las mujeres embarazadas a las que se presta atención primaria de la salud y analizar los conocimientos de las mujeres embarazadas sobre la diabetes mellitus gestacional en la atención primaria de la salud. Metodología: estudio con enfoque cuantitativo- cualitativo, descriptivo y exploratorio, realizado en una Unidad de Salud Familiar de Bahía, con 15 mujeres embarazadas mayores de 18 años, en cualquier trimestre gestacional y que hayan realizado al menos una consulta prenatal. Los datos se recopilaron mediante una hoja de ruta semiestructurada para las entrevistas y el acceso a los registros físicos de cada participante. El análisis de los datos del perfil se realizó por simple estadística descriptiva y las preguntas abiertas de la entrevista por la técnica de contenido temático propuesta por Bardin. Principales resultados: Se observó que la mayoría de las mujeres embarazadas eran jóvenes, negras, tenían educación secundaria, tenían más de tres hijos, estaban en el segundo trimestre gestacional y tenían bajos ingresos. En cuanto a los factores de riesgo, destacan la historia familiar de diabetes mellitus, sobrepeso/obesidad y estilo de vida sedentario. Además, la información sobre la diabetes mellitus gestacional es totalmente desconocida o insuficiente entre los participantes. Conclusión: El desconocimiento, junto con los factores de riesgo evidenciados y la situación de vulnerabilidad social y económica, puede contribuir al desarrollo de la Diabetes Mellitus Gestacional en la población estudiada, y las estrategias multidisciplinarias son fundamentales para su prevención y/o control.
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PURPOSE: 5'-methoxynobiletin (5'-MeONB), a polymethoxyflavone isolated from A. conyzoides, has shown anti-inflammatory property. Nevertheless, the antinociceptive activity and pre-clinical pharmacokinetics (PK) characteristics of 5'-MeONB remain unknown. Considering the anti-inflammatory potential of the 5'-MeONB, this study aimed to investigate the pre-clinical PK behavior of 5'-MeONB, as well as its time course antinociceptive activity. METHODS: 5'-MeONB plasma concentrations were determined in Wistar rats after intravenous (i.v.) (10 mg/kg) and oral (50 mg/kg) administration, and in Swiss mice after oral administration (100 mg/kg). Plasma samples were deproteinization and 5'-MeONB quantified by a validated UPLC-MS method. Additionally, the antinociceptive activity of 5'-MeONB was evaluated after 15, 30, 60, 180 and 360 min following oral administration on the acute nocifensive behavior of mice induced by formalin. RESULTS: 5'-MeONB rats and mice plasma concentration-time profiles were best one-compartment model. After i.v. administration to rats, a short half-life, a high clearance and moderate volume of distribution at steady state were observed. Similar results were obtained after oral administration. The oral bioavailability ranged from 8 to 11%. Additionally, 5'-MeONB exhibited antinociceptive activity in both formalin phases, especially in the inflammatory phase of the model, inhibiting 68% and 91% of neurogenic and inflammatory responses, respectively, after 30 min of oral administration. CONCLUSIONS: The results described here provide novel insights on 5'-MeONB pharmacokinetics and pharmacodynamic effect, serving as support for future studies to confirm this compound as anti-nociceptive and anti-inflammatory effective agent.
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Ageratum , Administração Oral , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Cromatografia Líquida , Formaldeído , Camundongos , Ratos , Ratos Wistar , Espectrometria de Massas em TandemRESUMO
Ischaemia and reperfusion (I/R)-induced gastrointestinal disorders are caused by free radicals, resulting in organ damage and functional disarrangement. This study aimed to investigate the healing effects of hydroalcoholic extracts from the leaves of Eugenia punicifolia (Kunth) DC. (HEEP) in male and female Wistar rats with I/R-induced peptic injuries, and the role of antioxidants in improving this response. After I/R-induced gastric and duodenal injuries, male and female [intact (INT) and ovariectomized (OVZ)] rats were orally treated with HEEP for 6 days. Biochemical analysis was used to determine the catalase (CAT), superoxide dismutase (SOD), and myeloperoxidase (MPO) activities, as well as malondialdehyde and reduced glutathione levels, to measure the gastric and duodenal healing process. Six days of HEEP treatment significantly decreased the I/R-induced gastric [male (73.68%), INT (52.83%), and OVZ (43.13%)] and duodenal damage [male (57.03%), INT (56.04%), and OVZ (54.83%)] in all groups. In OVZ rats, the healing effect of HEEP occurred because of the increased activity of SOD (2x) and CAT (1.16x) in the gastric mucosa. In the duodenal mucosa of INT rats, the extract reduced MPO (20.83%) activity. The 6-day HEEP treatment improved the healing of I/R-induced peptic ulcer injury, with the system acting differently in males and females. The antioxidant system is an important component of the HEEP activity during post-I/R mucosal recovery. This result revealed the importance of antioxidant compounds in minimizing the severity of I/R-related events.
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Eugenia , Úlcera Péptica , Traumatismo por Reperfusão , Úlcera Gástrica , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Eugenia/química , Eugenia/metabolismo , Feminino , Mucosa Gástrica , Isquemia/metabolismo , Masculino , Úlcera Péptica/tratamento farmacológico , Úlcera Péptica/metabolismo , Extratos Vegetais , Ratos , Ratos Wistar , Reperfusão , Traumatismo por Reperfusão/tratamento farmacológico , Traumatismo por Reperfusão/metabolismo , Úlcera Gástrica/induzido quimicamente , Superóxido Dismutase/metabolismoRESUMO
The emergence of multidrug-resistant bacteria stimulates the search for new substitutes to traditional antimicrobial agents, especially molecules with antivirulence properties, such as those that interfere with quorum sensing (QS). This study aimed to evaluate the potential of phenolic compounds for QS inhibition in a QS biosensor strain (Chromobacterium violaceum) and three foodborne bacterial species (Aeromonas hydrophila, Salmonella enterica serovar Montevideo, and Serratia marcescens). Initially, an in silico molecular docking study was performed to select the compounds with the greatest potential for QS inhibition, using structural variants of the CviR QS regulator of C. violaceum as target. Curcumin, capsaicin, resveratrol, gallic acid, and phloridizin presented good affinity to at least four CviR structural variants. These phenolic compounds were tested for antimicrobial activity, inhibition of biofilm formation, and anti-QS activity. The antimicrobial activity when combined with kanamycin was also assessed. Curcumin, capsaicin, and resveratrol inhibited up to 50% of violacein production by C. violaceum. Biofilm formation was inhibited by resveratrol up to 80% in A. hydrophila, by capsaicin and curcumin up to 40% in S. Montevideo and by resveratrol and capsaicin up to 60% in S. marcescens. Curcumin completely inhibited swarming motility in S. marcescens. Additionally, curcumin and resveratrol increased the sensitivity of the tested bacteria to kanamycin. These results indicate that curcumin and resveratrol at concentrations as low as 6µM are potential quorum sensing inhibitors besides having antimicrobial properties at higher concentrations, encouraging applications in the food and pharmaceutical industries.
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O tema evoca um conflito de paradigmas entre os fundamentos da civiliação judaico-cristã, a evolução dos costumes na pós-modernidade, a psicanálise como uma prática relativa à regulação do gozo no campo da psicopatologia e o discurso do Direito que regula a distribuição do gozo no laço social. A psicanálise nasce sob o paradigma da modernidade. Freud desvela a origem perversa e polimorfa da sexualidade, que é posteriormente submetida à lei por meio da função do Nome-do-Pai. Muitos filósofos pós-modernos rejeitam o primado da diferença anatômica entre os sexos, da fantasia infantil da castração e da ficção que atribui ao pai o protagonismo na interdição do incesto. Vamos contrastar os conceitos de diferença, diversidade e autodefinição sexual.
The title evokes a conflict of paradigms between the foundations of Judeo-Christian civilization, the evolution of customs in postmodernity, psychoanalysis as a practice related to the regulation of enjoyment in the field of psychopathology and the discourse of Law that regulates the distribution of enjoyment in social bonding. Psychoanalysis was born under the paradigm of modernity. Freud unveiled the perverse and polymorphic origin of sexuality, which is subsequently subjected to law through the function of the Name of the Father. Many postmodern philosophers reject the primacy of the anatomical difference between the sexes, the infantile fantasy of castration and the fiction that bestows the leading role upon the father in the prohibition of incest. As a result, this article contrasts the concepts of difference and diversity and sexual self-definition.
Le thème évoque un conflit de paradigmes entre les fondements de la civilisation judéo-chrétienne, l'évolution des coutumes dans la postmodernité, la psychanalyse en tant que pratique liée à la régulation de la jouissance dans le domaine de la psychopathologie et le discours du Droit qui règle la répartition de la jouissance dans le lien social. La psychanalyse est née sous le paradigme de la modernité. Freud dévoile l'origine perverse et polymorphe de la sexualité, qui est ensuite soumise à la loi par la fonction du Nom du Père. De nombreux philosophes postmodernes rejettent la primauté de la différence anatomique entre les sexes, du fantasme infantile de castration et de la fiction qui attribue au père le protagonisme dans l'interdiction de l'inceste. Nous comparons les concepts de différence et de diversité et d'autodéfinition sexuelle.
El tema evoca un conflicto de paradigmas entre los fundamentos de la civilización judeocristiana, la evolución de las costumbres en la postmodernidad, el psicoanálisis como práctica relacionada a la regulación del goce en el campo de la psicopatología y el discurso del Derecho que regula la distribución del goce en el vínculo social. El psicoanálisis nace bajo el paradigma de la modernidad. Freud revela el origen perverso y polimórfico de la sexualidad que, posteriormente, se somete a la ley a través de la función del Nombre del Padre. Muchos filósofos postmodernos rechazan la primacía de la diferencia anatómica entre los sexos, de la fantasía infantil de la castración y de la ficción que atribuye al padre el protagonismo en la interdicción del incesto. Comparemos los conceptos de diferencia, diversidad y autodefinición sexual.
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BACKGROUND: Healthcare professionals need to know the degree of disability and severity of their patients to determine actions and therapy needed to minimize potential harm, improve their patient condition, and maximize clinical outcomes. OBJECTIVES: To evaluate the occurrence and severity of neck disability in individuals with muscular, joint, and mixed temporomandibular disorder (TMD). MATERIALS AND METHODS: Cross-sectional study with individuals divided into four groups: muscular TMD (n=20), joint TMD (n=20), mixed TMD (n=20) and control (n=20). For diagnosis and classification of TMD, it was used the Research Diagnostic Criteria (RDC) and to assess the severity of neck dysfunction the Neck Disability Index (NDI). RESULTS: Moderate neck disability was frequent in all individuals with TMD; high scores of neck disability index were evidenced in the mixed and joint TMD groups; there was a moderate positive correlation between the severity of neck disability and TMD severity (r=0.7; CI=0.32-0.78; p<0.03). CONCLUSION: The gravity of neck disability and the severity of TMD are directly proportional in the group of individuals with mixed TMD.
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Transtornos da Articulação Temporomandibular , Estudos Transversais , Dor Facial , HumanosRESUMO
The emergence of bacterial strains resistant to different antibiotics has prompted the search for new sources of antimicrobial compounds. Studies have shown that jambolan [Syzygium cumini (L.) Skeels], a tropical fruit from the Mirtaceae family, contains a great variety of phytochemical compounds with high antioxidant and antimicrobial activity. This study aimed to determine the centesimal composition and physicochemical characteristics of the pulp and seed of S. cumini (L.) Skeels, as well as the content of total phenolic compounds and the antioxidant, antibacterial, antibiofilm and anti-quorum sensing (QS) activities of the phenolic extracts obtained from the pulp and the seeds of this fruit. The in vitro antibacterial and anti-QS activities of active films incorporating phenolic extracts were also evaluated. Additionally, we performed molecular docking of phenolic compounds present in jambolan with the CviR QS regulator of Chromobacterium violaceum. The composition and physicochemical characteristics of the samples presented similar values to those found for the species. However, the seed phenolic extract had a higher content of phenolic compounds and antioxidant activity than the pulp. Both phenolic extracts presented antibacterial activity against Aeromonas hydrophila, C. violaceum, Escherichia coli, Pseudomonas aeruginosa, Salmonella enterica serovar Typhimurium, Serratia marcescens, Listeria monocytogenes, and Staphylococcus aureus. The seed phenolic extract was particularly inhibitory against S. aureus. The pulp phenolic extract inhibited swarming motility and biofilm formation of A. hydrophila, E. coli, and S. marcescens in sub-MIC concentrations. The pulp and seed phenolic extracts inhibited violacein production in C. violaceum. Films incorporating both phenolic extracts inhibited the growth of bacteria, particularly Pseudomonas fluorescens, L. monocytogenes, and S. aureus, as well as QS in C. violaceum. Molecular docking showed that a variety of compounds found in pulp and seed extracts of jambolan, particularly chlorogenic acid and dihydroquercetin, potentially bind CviR protein and may interfere with QS. Our results indicate that pulp and seed of jambolan are good sources of antibacterial, antibiofilm, and anti-QS compounds that can be used in the development of natural preservatives and for application in antibacterial active films.
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ETHNOPHARMACOLOGICAL RELEVANCE: Eugenia punicifolia (Kunth) DC. (Myrtaceae), an Amazonian medicinal plant known as "pedra-ume-caá," is popularly used as a natural remedy for inflammation, wounds, infections, diabetes, fever, and flu. Its anti-inflammatory, antinociceptive, and gastroprotective effects have already been characterized. We evaluated the gastric healing effect of the hydroalcoholic extract of the leaves of E. punicifolia (HEEP) in male and female Wistar rats against nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol. MATERIALS AND METHODS: The healing effect of HEEP on the gastric mucosa of adult male and female Wistar rats was measured after the chronic application of aggressive factors such as NSAIDs or 80% ethanol. Male, and intact and ovariectomized (OVZ) female rats were treated with HEEP for two days (NSAIDs) or one, two, four, and six days (80% ethanol). The stomachs were analyzed macroscopically for ulcerative lesions (mm2), and the healing process was measured using biochemical analysis with anti-inflammatory and antioxidant parameters. RESULTS: Macroscopic evaluation of the gastric mucosa showed that gastric lesions induced by NSAIDs were significantly healed (66%) and pro-inflammatory interleukin 5 cytokine level was decreased after two-day oral treatment with HEEP compared with those in the negative control group (pâ¯<â¯0.05). However, the gastric lesions induced by NSAIDs did not heal in HEEP-treated female rats (pâ¯>â¯0.05). In addition, four-day treatment with HEEP significantly healed the gastric lesions induced by ethanol in male and female rats (63% and 78%, respectively) compared to those of the negative control group (pâ¯<â¯0.05). However, the OVZ group required six days of HEEP treatment to heal gastric ulcers (67% compared to the control group). HEEP exerts the healing effect against ethanol by significantly reducing neutrophil infiltration into the gastric mucosa by decreasing myeloperoxidase activity in male and OVZ rats after four and six days of treatment, respectively (pâ¯<â¯0.05). Four-day treatment with HEEP also increased the level of a non-enzymatic antioxidant, reduced glutathione in intact females compared to that of the negative control group (pâ¯<â¯0.05). CONCLUSION: These findings indicated that HEEP was effective in promoting the healing of gastric ulcers induced by NSAIDs or ethanol. The gastric healing effects of this extract could be affected by female sex hormone interference; in future, comprehensive studies should be performed by considering sex differences.
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Antiulcerosos/farmacologia , Eugenia/química , Extratos Vegetais/farmacologia , Úlcera Gástrica/tratamento farmacológico , Animais , Anti-Inflamatórios não Esteroides/toxicidade , Antiulcerosos/isolamento & purificação , Antioxidantes/metabolismo , Modelos Animais de Doenças , Etanol/toxicidade , Feminino , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/patologia , Masculino , Folhas de Planta , Ratos , Ratos Wistar , Fatores Sexuais , Úlcera Gástrica/patologia , Cicatrização/efeitos dos fármacosRESUMO
OBJECTIVES: The route of administration is an important factor in determining the action of some drugs. We previously demonstrated that subcutaneous monosodium glutamate (MSG) accelerated cortical spreading depression (CSD) in the rat and that treadmill exercise attenuated this effect. This study evaluated whether other routes of administration exert the same action by testing orogastric (gavage) and topical cortical MSG administration in treadmill-exercised and sedentary rats. Additionally, in the orogastric treatment we tested anxiety-like behavior. METHODS: Exercised and sedentary rats received per gavage water or MSG (1 or 2 g/kg) daily from postnatal (P) day 7 to 27. Behavioral tests (open field and elevated plus-maze) occurred at P53 ± 3. At P56 ± 3, we analyzed CSD parameters (velocity, amplitude, and duration of the negative potential change). Other three groups of rats received an MSG solution (25, 50 or 75â mg/ml) topically to the intact dura mater during CSD recording. RESULTS: MSG-gavage increased anxiety-like behavior and the CSD velocities compared with water-treated controls (P < 0.05). Exercise decelerated CSD. In contrast to gavage, which accelerated CSD, topical MSG dose-dependently and reversibly impaired CSD propagation, reduced CSD amplitude and increased CSD duration (P < 0.05). CONCLUSIONS: The exercise-dependent attenuation of the effects of MSG confirms our previous results in rats treated subcutaneously with MSG. CSD results suggest two distinct mechanisms for gavage and topical MSG administration. Additionally, data suggest that exercise can help protect the developing and adult brain against the deleterious actions of MSG.
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Ansiedade/induzido quimicamente , Depressão Alastrante da Atividade Elétrica Cortical/efeitos dos fármacos , Condicionamento Físico Animal , Glutamato de Sódio/administração & dosagem , Administração Tópica , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/fisiopatologia , Feminino , Masculino , Ratos Wistar , Comportamento SedentárioRESUMO
AIM: To evaluate the sex-specific effects of a hydroalcoholic extract from Eugenia punicifolia (HEEP) leaves on gastric ulcer healing. METHODS: In this rat study involving males, intact (cycling) females, and ovariectomized females, gastric ulcers were induced using acetic acid. A vehicle, lansoprazole, or HEEP was administered for 14 d after ulcer induction. Body weight was monitored throughout the treatment period. At the end of treatment, the rats were euthanized and the following in vivo and in vitro investigations were performed: macroscopic examination of the lesion area and organ weights, biochemical analysis, zymography, and evaluation of protein expression levels. Additionally, the concentration-dependent effect of HEEP was evaluated in terms of subacute toxicity and cytotoxicity. RESULTS: Compared to the vehicle, HEEP demonstrated a great healing capacity by substantially reducing the ulcerative lesion area in males (52.44%), intact females (85.22%), and ovariectomized females (65.47%), confirming that HEEP accelerates the healing of acetic acid-induced gastric lesions and suggesting that this effect is modulated by female sex hormones. The antiulcer effect of HEEP was mediated by prostaglandin E2 only in male rats. Overall, the beneficial effect of HEEP was the highest in intact females. Notably, HEEP promoted the expression of vascular endothelial growth factor (intact vs ovariectomized females) and decreased the expression of Caspase-8 and Bcl-2 (intact female vs male or ovariectomized female). Additionally, HEEP enhanced fibroblast proliferation and migration into a wounded area in vitro, confirming its healing effect. Finally, no sign of subacute toxicity or cytotoxicity of HEEP was observed. CONCLUSION: In gastric ulcers, HEEP-induced healing (modulated by female sex hormones; in males, mediated by prostaglandin) involves extracellular matrix remodeling, with gastric mucosa cell proliferation and migration.
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Eugenia/química , Extratos Vegetais/farmacologia , Reepitelização/efeitos dos fármacos , Úlcera Gástrica/tratamento farmacológico , Ácido Acético/toxicidade , Animais , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos , Feminino , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/patologia , Humanos , Masculino , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Ratos , Ratos Wistar , Fatores Sexuais , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/patologia , Testes de Toxicidade Subaguda , Resultado do TratamentoRESUMO
Myrcia bella Cambess., Myrcia fallax (Rich.) DC. and Myrcia guianensis (Aubl.) DC. (Myrtaceae) are trees found in Brazilian Cerrado. They have been widely used in folk medicine for the treatment of gastrointestinal disorders, hemorrhagic and infectious diseases. Few reports have been found in the literature connecting their phenolic composition and biological activities. In this regard, we have profiled the main phenolic constituents of Myrcia spp. leaves extracts by ESI(−)Q-TOF-MS. The main constituents found were ellagic acid (M. bella), galloyl glucose isomers (M. guianensis) and hexahydroxydiphenic (HHDP) acid derivatives (M. fallax). In addition, quercetin and myricetin derivatives were also found in all Myrcia spp. extracts. The most promising antioxidant activity, measured by 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity, was found for M. fallax extracts (EC50 8.61 ± 0.22 µg·mL−1), being slightly less active than quercetin and gallic acid (EC50 2.96 ± 0.17 and 2.03 ± 0.02 µg·mL−1, respectively). For in vitro antiproliferative activity, M. guianensis showed good activity against leukemia (K562 TGI = 7.45 µg·mL−1). The best antimicrobial activity was observed for M. bella and M. fallax to Escherichia coli (300 and 250 µg·mL−1, respectively). In conclusion, the activities found are closely related to the phenolic composition of these plants.
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Anti-Infecciosos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Myrtaceae/química , Extratos Vegetais/farmacologia , Anti-Infecciosos/química , Antineoplásicos Fitogênicos/química , Antioxidantes/química , Linhagem Celular Tumoral , Sinergismo Farmacológico , Flavonóis/química , Flavonóis/farmacologia , Humanos , Redes e Vias Metabólicas , Testes de Sensibilidade Microbiana , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/química , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por MatrizRESUMO
BACKGROUND: Eugenia spp. are used in popular medicine in the treatment of pain, diabetes, intestinal disorders and cough. The aim of the work is to evaluate, ex vivo and in vivo, the anti-inflammatory activity of the hydroethanolic extracts of the leaves of Eugenia aurata (EA) and Eugenia punicifolia HBK (EP) upon neutrophils. METHODS: Ex vivo, isolated human neutrophils were sensitized by Eugenia extracts (0.1-1000 µg/mL) and stimulated by PMA. In these conditions, different neutrophil activities related to inflammatory process were measured: adhesion, degranulation and NET release. Neutrophil viability and tumor line cells were monitored. In vivo, neutrophil influx was evaluated by peritonitis model performed in mice pretreated with different concentrations of Eugenia extracts. Phytochemical profile was assessed by mass spectrometry. RESULTS: Ex vivo, EA and EP (1000 µg/mL) reduced cell adhesion and degranulation, respectively. NET release was inhibited by EA and EP. Anti-inflammatory activities occurred in the absence of cytotoxicity. In vivo, both EA as EP inhibited neutrophil migration. The phytochemical profile revealed that EA contains myricitrin, rutin, quinic acid and quercetin derivatives. EP presents gallic acid, quercetin derivatives, syringic acid, ellagic acid, monogalloyl-glucose, glycosyringic acid, mudanoside B, HHDP glucose isomer and digalloylglucose isomer. EA and EP inhibit neutrophil migration by different pathways. CONCLUSION: Different chemical compositions may explain the anti-inflammatory effects described herein for EA and EP. Both extracts inhibit NET release but only EA reduces cell adhesion whereas EP decreases elastase secretion. This work contributes to the elucidation of cellular mechanisms related to the anti-inflammatory activity for leaves of E. aurata and E. punicifolia HBK.
Assuntos
Anti-Inflamatórios/farmacologia , Adesão Celular/efeitos dos fármacos , Degranulação Celular/efeitos dos fármacos , Eugenia/química , Armadilhas Extracelulares/efeitos dos fármacos , Neutrófilos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/química , Sobrevivência Celular/efeitos dos fármacos , Inflamação/metabolismo , Masculino , Camundongos , Extratos Vegetais/químicaRESUMO
Natural rubber latex biomembranes (NRL), obtained from rubber tree Hevea brasiliensis (Willd. ex A. Juss.) Mull. Arg., have been used as sustained drug release of drugs and plant extracts with medicinal properties. The Stryphnodendron obovatum Bench (Fabaceae), popularly known as "barbatimão" has anti-inflammatory and healing properties already described in literature. Thus, the aim of this work were to study the release behavior of the hydroethanolic extract from the leaves of S. obovatum loaded in the NRL by ultravioletvisible spectroscopy (UV-VIS). The release followed a biexponential pattern and the mechanism of release was Super Case II (n > 1). FTIR analyses did not show reaction between NRL and extract, only intermolecular interaction. From SEM was possible to observe the extract at the surface, responsible for the initial fast release, which the concentrations at 5.0 mg/mL released 2.4% and at 0.1 mg/mL released 96.8%; both reached the plateau in 7 days.
Assuntos
Borracha , Stryphnodendron barbatimam , TaninosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: An ethnopharmacological survey indicated that leaves from Eugenia punicifolia (Kunth) DC. (Myrtaceae) are popularly used as a natural therapeutic agent to treat pain and inflammation. AIM OF THE STUDY: The overall objective of the present study was to evaluate the antinociceptive, anti-inflammatory and gastroprotective activities of a hydroalcoholic extract of leaves from Eugenia punicifolia (HEEP) in rodents. MATERIAL AND METHODS: The antinociceptive effects of HEEP were evaluated in mice after oral administration in chemical (formalin and glutamate) and thermal (hot-plate) tests. We evaluated the involvement of the glutamatergic, opioidergic and nitrergic pathways in the antinociception of HEEP and the effect of HEEP on the inhibition of p38α MAPK. The anti-inflammatory effect of HEEP was evaluated in mice and rats using xylene-induced ear edema and carrageenan-induced paw edema, respectively. Furthermore, the gastroprotective effect of HEEP was evaluated in rats with acute gastric lesions induced by ethanol or indomethacin. Finally, we performed a phytochemical analysis of HEEP. RESULTS: The oral administration of HEEP (125, 250 and 500mg/kg, p.o.) significantly inhibited the neurogenic and inflammatory phases of formalin-induced licking, and HEEP (250mg/kg, p.o.) also significantly inhibited the nociception caused by glutamate. The antinociceptive effects of HEEP were significantly reversed by l-arginine (500mg/kg, i.p.) but not by naloxone (1mg/kg, i.p.) in the formalin test. HEEP did not affect animal motor performance in the rotarod model. In addition, HEEP also increased the paw withdraw latency in the hot-plate test. HEEP significantly inhibited ear edema induced by xylene (64%) and paw edema induced by carrageenan (50%) compared to the control group. Furthermore, HEEP (3-30mg/mL) also inhibited the phosphorylation of p38α MAPK by approximately 90%. In addition, HEEP (125, 250 and 500mg/kg, p.o.) protected the rats against ethanol (88.4-99.8%) and indomethacin (53-72.3%) and increased the mucus levels of the gastric mucosa without producing an antisecretory effect. The phytochemical profile of HEEP obtained using HPLC-PDA showed secondary metabolites already reported for the genus, mostly flavonoids, gallotannins and proanthocyanidins. CONCLUSIONS: These data show for the first time that HEEP has significant antinociceptive and anti-inflammatory effects, which appear to be related to the inhibition of the glutamatergic system, the synthesis of nitric oxide and the inhibition of the phosphorylation of p38α MAPK. HEEP also has interesting gastroprotective effects related to the maintenance of protective factors, such as mucus production. These results support the use of Eugenia punicifolia in popular medicine and demonstrate that this plant has therapeutic potential for the development of phytomedicines with antinociceptive, anti-inflammatory and gastroprotective properties.
Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Eugenia/química , Extratos Vegetais/farmacologia , Analgésicos/administração & dosagem , Analgésicos/isolamento & purificação , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/isolamento & purificação , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Edema/tratamento farmacológico , Feminino , Ácido Glutâmico/metabolismo , Inflamação/tratamento farmacológico , Masculino , Medicina Tradicional , Camundongos , Dor/tratamento farmacológico , Medição da Dor , Extratos Vegetais/administração & dosagem , Folhas de Planta , Ratos , Ratos WistarRESUMO
The purpose of this study was to determine the Minimum Inhibitory Concentration (MIC) of pure or mixed chemicals for Saccharomyces cerevisiae and Lactobacillus fermentum in the samples isolated from distilleries with serious bacterial contamination problems. The biocides, which showed the best results were: 3,4,4' trichlorocarbanilide (TCC), tested at pH 4.0 (MIC = 3.12 mg/l), TCC with benzethonium chloride (CBe) at pH 6.0 (MIC = 3.12 mg/l) and TCC mixed with benzalkonium chloride (CBa) at pH 6.0 (MIC = 1.53 mg /l). If CBa was used in sugar cane milling in 1:1 ratio with TCC, a 8 times reduction of CBa was possible. This formulation also should be tested in fermentation steps since it was more difficult for the bacterium to develop resistance to biocide. There was no inhibition of S. cerevisiae and there were only antibiotics as an option to bacterial control of fuel ethanol fermentation by S. cerevisiae.
RESUMO
UNLABELLED: In 2002, Spring et al reported a family with an autosomal dominant form of hereditary sensory neuropathy; patients also presented adult onset of gastroesophageal reflux and cough. Since then, no further families have been described. OBJECTIVE: To study a new Portuguese family with these characteristics. METHOD: To describe the clinical and neurophysiologic characteristics of one family with features of sensory neuropathy associated with cough and gastroesophageal erflux. RESULTS: Three of five siblings presented a similar history of paroxysmal cough (5th decade). About a decade later they experienced numbness and paraesthesia in the feet and in all cases there was evidence of an axonal sensory neuropathy. A history of gastroesophageal reflux of variable severity and age of onset was also present. DISCUSSION: Molecular genetic studies have demonstrated genetic heterogeneity between the hereditary sensory neuropathy type 1 subtypes. The identification of these families is of major importance because further work is required to identify the underlying genetic defect.
Assuntos
Tosse/etiologia , Refluxo Gastroesofágico/diagnóstico , Neuropatias Hereditárias Sensoriais e Autônomas/diagnóstico , Idade de Início , Idoso , Idoso de 80 Anos ou mais , Tosse/genética , Tosse/fisiopatologia , Feminino , Refluxo Gastroesofágico/genética , Refluxo Gastroesofágico/fisiopatologia , Neuropatias Hereditárias Sensoriais e Autônomas/genética , Neuropatias Hereditárias Sensoriais e Autônomas/fisiopatologia , Humanos , Masculino , Mutação , Condução Nervosa , Linhagem , PortugalRESUMO
In 2002, Spring et al reported a family with an autosomal dominant form of hereditary sensory neuropathy; patients also presented adult onset of gastroesophageal reflux and cough. Since then, no further families have been described. Objective: To study a new Portuguese family with these characteristics. Method: To describe the clinical and neurophysiologic characteristics of one family with features of sensory neuropathy associated with cough and gastroesophageal erflux. Results: Three of five siblings presented a similar history of paroxysmal cough (5th decade). About a decade later they experienced numbness and paraesthesia in the feets and in all cases there was evidence of an axonal sensory neuropathy. A history of gastroesophageal reflux of variable severity and age of onset was also present. Discussion: Molecular genetic studies have demonstrated genetic heterogeneity between the hereditary sensory neuropathy type 1 subtypes. The identification of these families is of major importance because further work is required to identify the underlying genetic defect. .
Em 2002, Spring et al descreveram uma família com uma combinação de polineuropatia sensitiva hereditária, doença do refluxo gastroesofágico e tosse paroxística. Desde então não foram descritos outros casos. Objectivo: Estudar uma nova família portuguesa com essas características. Método: Caracterização clínica e neurofisiológica de uma família com a referida combinação de patologias. Resultados: Três, de cinco irmãos, apresentam uma história semelhante de tosse paroxística com início na 5a década. Cerca de uma década mais tarde iniciam quadro de parestesias em ambos os pés, com evidência de neuropatia sensitiva axonal. Todos os casos apresentam também uma história de doença do refluxo gastroesofágico de gravidade variável. Discussão: Nos últimos anos, os estudos de genética molecular permitiram evidenciar a heterogeneidade genética dos vários subtipos de polineuropatia sensitiva hereditária tipo 1. A identificação das famílias afectadas reveste-se de grande importância, nomeadamente na tentativa de caracterização da alteração genética deste subtipo. .
Assuntos
Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Masculino , Tosse/etiologia , Refluxo Gastroesofágico/diagnóstico , Neuropatias Hereditárias Sensoriais e Autônomas/diagnóstico , Idade de Início , Tosse/genética , Tosse/fisiopatologia , Refluxo Gastroesofágico/genética , Refluxo Gastroesofágico/fisiopatologia , Neuropatias Hereditárias Sensoriais e Autônomas/genética , Neuropatias Hereditárias Sensoriais e Autônomas/fisiopatologia , Mutação , Condução Nervosa , Linhagem , PortugalRESUMO
The present study evaluated the anti-inflammatory and analgesic properties of Agave sisalana Perrine in classic models of inflammation and pain. The hexanic fraction of A. sisalana (HFAS) was obtained by acid hydrolysis followed by hexanic reflux. Anti-inflammatory properties were examined in three acute mouse models (xylene ear oedema, hind paw oedema and pleurisy) and a chronic mouse model (granuloma cotton pellet). The antinociceptive potential was evaluated in chemical (acetic-acid) and thermal (tail-flick and hot-plate test) models of pain. When given orally, HFAS (5, 10, 25 and 50 mg/kg) reduced ear oedema (p < 0.0001; 52%, 71%, 62% and 42%, respectively). HFAS also reduced hind paw oedema at doses of 10 mg/kg and 25 mg/kg (p < 0.05; 42% and 58%, respectively) and pleurisy at doses of 10 mg/kg and 25 mg/kg (41% and 50%, respectively). In a chronic model, HFAS reduced inflammation by 46% and 58% at doses of 10 mg/kg and 25 mg/kg, respectively. Moreover, this fraction showed analgesic properties against the abdominal writhing in an acetic acid model (at doses of 5-25 mg/kg) with inhibitory rates of 24%, 54% and 48%. The HFAS also showed an increased latency time in the hot-plate (23% and 28%) and tail-flick tests (61% and 66%) for the 25 mg/kg and 50 mg/kg doses, respectively. These results suggest that HFAS has anti-inflammatory and analgesic properties.
Assuntos
Agave/química , Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Inflamação/tratamento farmacológico , Dor/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Analgésicos/isolamento & purificação , Animais , Anti-Inflamatórios/isolamento & purificação , Carragenina , Edema/induzido quimicamente , Edema/tratamento farmacológico , Inflamação/induzido quimicamente , Masculino , Camundongos , Dor/induzido quimicamente , Medição da Dor , RatosRESUMO
The present study evaluated the anti-inflammatory and analgesic properties of Agave sisalana Perrine in classic models of inflammation and pain. The hexanic fraction of A. sisalana (HFAS) was obtained by acid hydrolysis followed by hexanic reflux. Anti-inflammatory properties were examined in three acute mouse models (xylene ear oedema, hind paw oedema and pleurisy) and a chronic mouse model (granuloma cotton pellet). The antinociceptive potential was evaluated in chemical (acetic-acid) and thermal (tail-flick and hot-plate test) models of pain. When given orally, HFAS (5, 10, 25 and 50 mg/kg) reduced ear oedema (p < 0.0001; 52%, 71%, 62% and 42%, respectively). HFAS also reduced hind paw oedema at doses of 10 mg/kg and 25 mg/kg (p < 0.05; 42% and 58%, respectively) and pleurisy at doses of 10 mg/kg and 25 mg/kg (41% and 50%, respectively). In a chronic model, HFAS reduced inflammation by 46% and 58% at doses of 10 mg/kg and 25 mg/kg, respectively. Moreover, this fraction showed analgesic properties against the abdominal writhing in an acetic acid model (at doses of 5-25 mg/kg) with inhibitory rates of 24%, 54% and 48%. The HFAS also showed an increased latency time in the hot-plate (23% and 28%) and tail-flick tests (61% and 66%) for the 25 mg/kg and 50 mg/kg doses, respectively. These results suggest that HFAS has anti-inflammatory and analgesic properties.