RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Rhynchospora nervosa (Vahl) Boeckeler (Cyperaceae), popularly known as "capim-estrela", is a native species widely distributed in Brazil. The whole plant has been used in local traditional medicine in the form of teas or syrups to treat inflammation, flu, nasal congestion, fever, swelling, and venereal disease. This is the first study to investigate the pharmacological properties of this species. AIM OF THE STUDY: The present study aimed to evaluate the in vivo anti-inflammatory, antipyretic and antinociceptive potential of the lyophilized hydroalcoholic extract of R. nervosa in heterogenic Swiss mice. In addition to pharmacological studies, the total phenol and flavonoid contents of the extract were determined. MATERIAL AND METHODS: The anti-inflammatory effect was evaluated through carrageenan-induced paw edema and peritonitis models. For the antinociceptive assay, the number of acetic acid-induced writhing responses in the animals was counted. Antipyretic activity was tested by yeast-induced pyrexia in mice and evaluated for 4 h. Nitric oxide (NO) concentration and leukocyte migration in the peritoneal fluid were quantified. The acute toxicity of the extract was also calculated. Quantitative analyses of total phenols and flavonoids in the extract were performed by spectrophotometric methods. RESULTS: In short, the lyophilized hydroalcoholic extract of R. nervosa showed low acute toxicity in the preclinical tests (LD50 = 3807 mg/kg). A significant anti-inflammatory effect was observed, with an average reduction of carrageenan-induced paw edema of 96.37%. Comparatively, indomethacin inhibited the development of the carrageenin paw edema by 97.52%. In the peritonitis test, a significant reduction in NO levels was recorded. A reduction in the number of white cells, notably monocytes, was also observed, confirming the anti-inflammatory effect. Writhing was reduced by 86.53%, which indicates antinociceptive activity. As for antipyretic activity, no positive effects of the extract were observed. The lyophilized hydroalcoholic extract of R. nervosa presented a high content of phenolic compounds (322.47 µg GAE/mg) and total flavonoids (440.50 µg QE/mg). CONCLUSION: The lyophilized hydroalcoholic extract of R. nervosa showed significant in vivo anti-inflammatory and antinociceptive activity in mice. These preliminary findings support the indication of the use of this species in folk medicine in Brazil for the treatment of inflammation.
Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Antipiréticos/farmacologia , Cyperaceae/química , Fitoterapia , Extratos Vegetais/farmacologia , Analgésicos/administração & dosagem , Animais , Anti-Inflamatórios/administração & dosagem , Antipiréticos/administração & dosagem , Carragenina/toxicidade , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Edema/tratamento farmacológico , Feminino , Masculino , Camundongos , Peritonite/induzido quimicamente , Peritonite/tratamento farmacológico , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Ratos , Ratos WistarRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Hymenaea cangaceira Pinto, Mansano & Azevedo (Fabaceae) is a Brazilian medicinal plant widely known as "Jatobá". In folk medicine, it is used to treat infections, respiratory problems, rheumatism, antitumoral, inflammation and pain, however, no activity has been scientifically validated. AIM OF THE STUDY: This study investigated chemical composition of essential oil from Hymenaea cangaceira (EOHc), antimicrobial, antinociceptive and antioxidant activities besides protection against DNA damage and hemolysis. MATERIAL AND METHODS: The essential oil was obtained by hydrodistillation, and characterized by GC-MS and GC-FID. The evaluation of antimicrobial activity was performed by microdilution method. The evaluation of the antioxidant activity was performed using the radicals DPPH, ABTS, O2- and OH-, and the protection of DNA damage using plasmid pBR322. Different experimental models were used to evaluate the antinociceptive effect (acetic acid and formalin), and evaluate the mechanisms of action involved with pharmacological antagonists (naloxone, atropine and gibenclamide) in mice. The essential oil was evaluated for hemolysis on human erythrocytes. RESULTS: The extraction of EOHc showed a yield of 0.18% on a dry basis, presenting high content of hydrocarbon sesquiterpenes (79.04%), high antioxidant activity and protect DNA from damage, besides presenting antifungal and antibacterial activity against Gram-positive and Gram-negative bacteria in vitro. It was found that the essential oil had no acute toxicity in mice up to 5000â¯mg/kg oral administration (o.a.), in addition to no hemolysis on human erythrocytes. The reduction of antinociceptive activity was 75%, with the opioid system as the mechanism of action. CONCLUSION: Our results validate the main activities by the traditional use attributed to H. cangaceira for antimicrobial and analgesic activity. In addition, the oil has a potent antioxidant activity, protecting the body against oxidative stress damage, adding new value to an endemic species not known to the industry.
Assuntos
Analgésicos/farmacologia , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Hymenaea/química , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Ácido Acético/toxicidade , Analgésicos/química , Analgésicos/isolamento & purificação , Animais , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Brasil , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos , Etanol/química , Etnofarmacologia , Formaldeído/toxicidade , Humanos , Medicina Tradicional/métodos , Camundongos , Testes de Sensibilidade Microbiana , Nociceptividade/efeitos dos fármacos , Óleos Voláteis/química , Óleos Voláteis/uso terapêutico , Dor/induzido quimicamente , Dor/diagnóstico , Dor/tratamento farmacológico , Medição da Dor , Óleos de Plantas/química , Óleos de Plantas/isolamento & purificação , Testes de Toxicidade AgudaRESUMO
Schistosomiasis mansoni is a tropical disease and remains as an important public healthy problem in Northeast - Brazil, where it is highly endemic. This disease has the liver as the major focus of its histological lesions, physiopathological alterations and clinical manifestations. Previous studies have shown alteration on lipid metabolism in the hepatosplenic form of Schistosomiasis. One of the main alterations is the reduction on lecithin: cholesterol acyltransferase (LCAT) activity, an hepatic enzyme that catalyze the esterification of cholesterol in plasma In this work, we evaluate the LCAT activity in plasma from patients with hepatosplenic Schistosomiasis mansoni who were subjected to a new surgical treatment, which consists of splenectomy followed by auto-transplantation of spleen tissue. LCAT activity was detected by using a radioactive substrate. Both [14C]free and esterified cholesterol produced by the LCAT reaction were separated by thin layer chromatography, and the sample radioactivity was counted in a liquid scintilation analyzer. LCAT activity from plasma of patients subjected to splenectomy and spleen tissue implantation were reduced by 32 %, in comparison to the control group. However, in Schistosoma mansoni patients who were only clinically treated the reduction on LCAT activity was twice (64%) as much as that found in plasma of patients subjected to splenectomy and spleen tissue implantation. These results suggest a significant improvement on LCAT activity after the surgical treatment of patients with the hepatosplenic form of Schistosomiasis mansoni.
A esquistossomose mansônica é uma doença tropical que constitui um importante problema de saúde pública, na Região Nordeste do Brasil, onde é encontrada em alta endemicidade. Essa parasitose tem o fígado como principal alvo de suas lesões histológicas, alterações fisiopatológicas e manifestações clínicas. Estudos anteriores reportam alterações no metabolismo lipídico associadas à forma hepatoesplênica da esquistosomose.Uma das principais alterações consiste na redução da atividade da enzima hepática LCAT, responsável pela esterificação do colesterol no plasma. Neste trabalho, avaliamos a atividade da LCAT no plasma de pacientes portadores da esquistossomose mansônica hepatoesplênica, os quais foram submetidos a esplenectomia e reimplante de parte de tecido do baço. A atividade enzimática da LCAT foi determinada com substrato radioativo. O [14C]colesterol livre e esterificado, formados por ação da LCAT, foram separados por cromatografia em camada delgada e a radioatividade das amostras foi contada em analisador de cintilação líquida. A atividade da LCAT nos pacientes submetidos a esplenectomia e reimplante de tecido do baço apresentou redução de 32 %, em relação ao grupo controle. Contudo, nos portadores da doença que não foram submetidos ao procedimento cirúrgico a redução na atividade da LCAT foi o dobro (64%) da observada em pacientes esplenectomizados e com reimplante de parte do tecido do baço. Esses resultados sugerem haver uma melhora significativa no efeito da forma grave da esquistossomose mansônica sobre a atividade da LCAT.
RESUMO
Schistosomiasis mansoni is a tropical disease and remains as an important public healthy problem in Northeast - Brazil, where it is highly endemic. This disease has the liver as the major focus of its histological lesions, physiopathological alterations and clinical manifestations. Previous studies have shown alteration on lipid metabolism in the hepatosplenic form of Schistosomiasis. One of the main alterations is the reduction on lecithin: cholesterol acyltransferase (LCAT) activity, an hepatic enzyme that catalyze the esterification of cholesterol in plasma In this work, we evaluate the LCAT activity in plasma from patients with hepatosplenic Schistosomiasis mansoni who were subjected to a new surgical treatment, which consists of splenectomy followed by auto-transplantation of spleen tissue. LCAT activity was detected by using a radioactive substrate. Both [14C]free and esterified cholesterol produced by the LCAT reaction were separated by thin layer chromatography, and the sample radioactivity was counted in a liquid scintilation analyzer. LCAT activity from plasma of patients subjected to splenectomy and spleen tissue implantation were reduced by 32 %, in comparison to the control group. However, in Schistosoma mansoni patients who were only clinically treated the reduction on LCAT activity was twice (64%) as much as that found in plasma of patients subjected to splenectomy and spleen tissue implantation. These results suggest a significant improvement on LCAT activity after the surgical treatment of patients with the hepatosplenic form of Schistosomiasis mansoni.
A esquistossomose mansônica é uma doença tropical que constitui um importante problema de saúde pública, na Região Nordeste do Brasil, onde é encontrada em alta endemicidade. Essa parasitose tem o fígado como principal alvo de suas lesões histológicas, alterações fisiopatológicas e manifestações clínicas. Estudos anteriores reportam alterações no metabolismo lipídico associadas à forma hepatoesplênica da esquistosomose.Uma das principais alterações consiste na redução da atividade da enzima hepática LCAT, responsável pela esterificação do colesterol no plasma. Neste trabalho, avaliamos a atividade da LCAT no plasma de pacientes portadores da esquistossomose mansônica hepatoesplênica, os quais foram submetidos a esplenectomia e reimplante de parte de tecido do baço. A atividade enzimática da LCAT foi determinada com substrato radioativo. O [14C]colesterol livre e esterificado, formados por ação da LCAT, foram separados por cromatografia em camada delgada e a radioatividade das amostras foi contada em analisador de cintilação líquida. A atividade da LCAT nos pacientes submetidos a esplenectomia e reimplante de tecido do baço apresentou redução de 32 %, em relação ao grupo controle. Contudo, nos portadores da doença que não foram submetidos ao procedimento cirúrgico a redução na atividade da LCAT foi o dobro (64%) da observada em pacientes esplenectomizados e com reimplante de parte do tecido do baço. Esses resultados sugerem haver uma melhora significativa no efeito da forma grave da esquistossomose mansônica sobre a atividade da LCAT.
RESUMO
Objective: To evaluate the lipid metabolism in a population of young people, with the hepatesplenic form of schistosomiasis mansoni, associated with bleeding esophageal varices. Methods: 20 young patients were selected, at random, and compared to a control group of 20 healthy young people with the same social, economical and environmental conditions. The patients had undergone splenectomy, ligature of the left gastric vein and auto implantation of spleen tissue into the major omentum. From these two groups were obtained plasma and erythrocytes, and it were extracted, separated and determinated the neutral lipids, free cholesterol and ester, phospholipids and triglicerides levels. Results: The results appointed that the total molar concentration of total, cholesterol was similar to the group of the patients, which was similar to the control group. Similar results were observed with the fractions of ester and free cholesterol. There was a reduction on the concentration of plasmatic triglicerides, but without significance. The individual's phospholipids presented relative concentration, similar to the control group, but there was significant reduction (p 0,01) in the patient's phosphatidilethanolamine fraction, however, there was no significantly reduction of molar concentration of total plasmatic phospholipids, compared to the controls. In the erythrocyte membrane, the total cholesterol and. total phospholipids levels do not suffered significant alterations. Conclusion: The obtained data indicated a similarity of the lipids levels in the plasma and in the erythrocyte membrane of the patients submitted to the surgical treatment.
Objetivo: Avaliar o metabolismo lipídico em uma população de jovens portadores de esquistossomose na forma hepatoesplênica associada a varizes sangrentas de esôfago. Métodos: Foram selecionados, aleatoriamente, 20 jovens com estas anormalidades, submetidos a esplenectomia, ligadura da veia gástrica esquerda e auto-implante de tecido esplênico no omento maior. Como controle foram selecionados 20 adolescentes saudáveis, com a mesma condição sócio-econômico ambiental do grupo estudo. Destes dois grupos, obtiveram-se plasma e eritrócitos de onde foram extraídos, separados e dosados os lipídios neutros, colesterol livre e esterificado, fosfolipídios e triglicerídios. Resultados: A concentração molar de colesterol total do grupo de pacientes foi discretamente reduzida quando comparada ao grupo de indivíduos controles. Resultados similares foram observados com as frações de colesterol esterificado e colesterol livre. Houve redução na concentração de triglicerídios plasmáticos mas não significativa. Os fosfolipídios individuais apresentarem concentração relativa similar aos do grupo controle, entretanto houve redução significativa (p 0,01) na fração fosfatidiletanolamina dos pacientes, cuja redução não alterou significatvamente os fosfolipídios totais plasmáticos. Na membrana eritrocitária, os níveis de colesterol total e fosfolipídio total, não sofreram alterações significativas. Conclusão: Os dados sugerem haver normalização nos níveis lipídicos no plasma e na membrana eritrocitária dos pacientes submetidos ao tratamento efetuado.