RESUMEN
Significant risk factors for atherosclerosis include hyperlipidemia and oxidative stress, which together rank as three of the most significant risk factors for cardiovascular diseases. Securigera securidaca lowers cholesterol levels in diabetic rats' blood. This investigation's objective was to determine how methanolic extracts affected the flowers, leaves, and seeds of plants in rats that were fed a high-fat diet (HFD). Five groups of animals were created (n = 5). A total of 35 days, divided into two intervals, were used for the study. Rats received HFD during the first 15-day interval, while during the second 20-day interval, they also received extracts or the Atorvastatin reference drug. The extract of seeds has a high phenol content as well as DPPH radical antioxidant activity. Extracts were given at a dose of 200 mg/kg; p.o. Methanolic treatment of S. securidaca flowers, leaves, and seeds in HFD-induced hyperlipidemic rats resulted in significant reductions in total cholesterol, triglycerides, LDLC, and VLDL-C levels. HDL-C levels increased significantly because of the leaves. While in hyperlipidemic rats, seeds significantly reduced the activities of the enzymes ALT and ALP. The findings showed that, to a certain extent, seeds, flowers, and leaves may have benefits in reducing hyperlipidemia brought on by HFD in terms of lipid profiles and liver function enzymes. The findings of this study indicate a promising application prospect, but more research is needed to determine the exact mechanism of these novel compounds as antihyperlipidemic agents and to clarify their potential combination effect with synthetic drugs such as Atorvastatin. Combinations can reduce the dose of chemical medications required, which lowers the risk of side effects.
Asunto(s)
Diabetes Mellitus Experimental , Hiperlipidemias , Securidaca , Ratas , Animales , Hiperlipidemias/inducido químicamente , Hiperlipidemias/tratamiento farmacológico , Hipolipemiantes/farmacología , Hipolipemiantes/uso terapéutico , Ratas Wistar , Dieta Alta en Grasa/efectos adversos , Atorvastatina/farmacología , Atorvastatina/uso terapéutico , Atorvastatina/análisis , Diabetes Mellitus Experimental/tratamiento farmacológico , Metanol/análisis , Metanol/uso terapéutico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/química , Semillas , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Antioxidantes/análisis , Flores , ColesterolRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Bocconia arborea S. Watson (Papaveraceae) is known as "palo llora sangre" and is used in Mexican traditional medicine for the treatment of infections, it is also used as anxiolytic, analgesic, and antidiabetic, among others. AIM OF THE STUDY: to evaluate the antinociceptive and gastroprotective activities of extracts from B. arborea and dihydrosanguinarine (DHS) in murine models. MATERIALS AND METHODS: Organic extracts [hexane (HEX), dichloromethane (DCM) and methanol (MeOH)] were obtained by maceration. DHS was isolated and purified from HEX and DCM by precipitation and chromatographic column, respectively. Organic extracts and DHS were evaluated to determine their antinociceptive effect using formalin test in murine model. Also, the ambulatory effect of the HEX and DHS was determined in Open field test. The possible mechanism of action of DHS was explored in the presence of naltrexone (NTX, 1 mg/kg, i.p.), and picrotoxin (PTX, 1 mg/kg, i.p.). Gastric damage as possible adverse effect or gastroprotection were also investigated. Whereas DHS acute toxicological study was done, and 100 mg/kg of DHS was examined by electroencephalographic (EEG) analysis to discard neurotoxic effects. RESULTS: The B. arborea extracts significantly showed effects in both neurogenic and inflammatory phases of the formalin test, where the HEX extract reached the major antinociceptive effect. A significant and dose-response (10, 30, and 100 mg/kg) antinociceptive activity was observed with the HEX (ED50 = 69 mg/kg) and DHS (ED50 = 85 mg/kg) resembling the effect of the reference analgesic drug tramadol (30 mg/kg). The significant effect of DHS was inhibited in the presence of NTX and PTX. Neither the extracts or DHS produced sedative effects or gastric damage per se at antinociceptive doses. The EEG analysis demonstrated central depressant activity but not sedative or neurotoxic effects at the highest antinociceptive dosage tested, and LD50 is higher than 2000 mg/kg. CONCLUSIONS: HEX, DCM, and MeOH extracts showed significant antinociceptive activity, and DHS was identified as one of bioactive compounds without producing sedative, neurotoxic or gastric damage effects, as possible adverse effects reported for analgesic drugs. A role of opioid and GABAA neurotransmission appears to be involved as mechanisms of action of DHS, suggesting its potential for pain therapy and reinforcing the traditional use of B. arborea.
Asunto(s)
Dolor , Papaveraceae , Analgésicos/uso terapéutico , Analgésicos/toxicidad , Animales , Benzofenantridinas , Modelos Animales de Enfermedad , Isoquinolinas , Metanol/uso terapéutico , Ratones , Dolor/tratamiento farmacológico , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéuticoRESUMEN
According to the Brazilian folk medicine, the leaves of Plinia edulis (Vell.) Sobral (Myrtaceae), known as cambuca, are indicated in the treatment of gastric disorders. Infusions of P. edulis leaves were previously demonstrated to contain both maslinic (MA) and ursolic acids (UA). Both triterpenes have also been identified in the methanolic extract of peels from P. edulis fruit (MEPPE); however, the antiulcer effects of MEPPE have not yet been studied. This study therefore evaluates the gastroprotective potential of MEPPE, MA, and UA using ethanol/HCl- and indomethacin-induced gastric ulcers in mice. In addition, the in vitro effects of these compounds on the H+, K+-ATPase activity and on the free radical DPPH were measured. When used at concentration of 100 µg/mL, both MEPPE and UA were found to reduce the DPPH radical levels by 78.66 and 60.14%, respectively. However, MA did not reduce DPPH radical levels. Our results illustrated the antiulcer effects of MEPPE, MA, and UA against experimental ulcer models when administered by either the oral or the intraperitoneal routes. In addition, MEPPE reduced the size of ethanol/HCl-induced ulcers in a dose-dependent manner (log half-maximal effective oral dose, LogED50 = 1.09). Interestingly, UA promoted gastroprotection at lower doses than MA by increasing the production of mucin levels at 692%; however, it does not alter the activity of H+, K+-ATPase. In contrast, both MEPPE and MA, when incubated at concentrations of 10 and 100 µg/mL, inhibited H+, K+-ATPase activity in 61.81, 68.37, 54.04, and 70.45%, respectively. These results confirm that MEPPE, MA, and UA display gastroprotective activity through different modes of action; MA inhibits H+, K+-ATPase activity, whereas UA favour the mucus barrier.
Asunto(s)
Frutas , Myrtaceae , Úlcera Gástrica/prevención & control , Triterpenos/uso terapéutico , Animales , Antiulcerosos/aislamiento & purificación , Antiulcerosos/uso terapéutico , Relación Dosis-Respuesta a Droga , Femenino , Metanol/uso terapéutico , Ratones , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patología , Triterpenos/aislamiento & purificación , Ácido UrsólicoRESUMEN
Em função da grande variabilidade na composição da glicerina oriunda do biodiesel, torna-se imprescindível a busca por informações que contribuam estabelecê-la com uma alternativa na alimentação de aves. O objetivo deste estudo foi avaliar o efeito da inclusão de glicerina com alto de teor de metanol em dietas para frangos de corte sobre o desempenho e parâmetros sanguíneos. Foram utilizados 90 pintos de corte machos da linhagem Cobb, com 8 dias de idade, distribuídos em um delineamento inteiramente casualizado com três tratamentos (níveis de inclusão de 0, 6 e 12% de glicerina) e seis repetições de cinco aves cada, totalizando 18 unidades experimentais. As dietas foram formuladas a base de milho e farelo de soja para atender as exigências nutricionais e a glicerina utilizada continha 1,4% de metanol e 3158Kcal/kg de energia metabolizável. Aos 21, 33 e 42 dias de idade as sobras de ração e as aves foram pesadas para determinação do consumo de ração, peso médio, ganho de peso e conversão alimentar. Foram colhidos de 1 a 3mL de sangue venoso das aves, nos últimos dias de cada fase de criação (19-21, 31-33 e 40-42 dias de idade), para determinação do hematócrito, concentração de hemoglobina, reticulócitos, proteínas plasmáticas totais e fibrinogênio. Para avaliação da bioquímica sérica foram colhidos sangue venoso das aves sem anticoagulante, apenas na fase final da criação (40-42 dias). Os dados de desempenho, parâmetros hematológicos e bioquímicos obtidos foram submetidos à análise de variância. Utilizou-se o teste de Tukey com α=0,05 de probabilidade, para comparação das médias. Não foram observadas diferença estatística dos tratamentos sobre as variáveis de desempenho, parâmetros sanguíneos e bioquímicos, exceto para as proteínas plasmáticas entre 19 e 21, que aumentaram com a inclusão de glicerina, e para os reticulócitos que reduziram com a inclusão de glicerina. A inclusão de até 12% de glicerina com 1,4% de metanol residual em dietas de frangos de corte de 8 a 42 pode ser realizada sem prejuízos no desempenho e saúde dos mesmos.(AU)
Due to the great variability in the composition of glycerin derived from the biodiesel, it is essential to search for information which helps establish it with an alternative in poultry feed. The aim of this study was to evaluate the effect of inclusion of glycerin with high methanol content in diets for broilers on performance and blood parameters. They used 90 Cobb male broiler chicks with 8 days old, distributed in a completely randomized design with three treatments (0, 6 and 12% glycerin inclusion levels) and six replications of five birds each, a total of 18 experimental units. Diets were formulated based on corn and soybean meal to meet the nutritional requirements and glycerin used contained 1.4% methanol and 3158Kcal/kg of metabolizable energy. At 21, 33 and 42 days of age the remains of feed and the birds were weighed to determine the feed intake, body weight, body weight gain and feed conversion. Were collected 1 to 3ml of venous blood of the birds during the last days of each phase (19 to 21, 31 to 33 and 40 to 42 days of age) for determination of hematocrit, hemoglobin concentration, reticulocyte total plasma proteins and fibrinogen. To evaluate the serum biochemistry were collected venous blood of birds without anticoagulant, only in the final phase (40 to 42 days). Performance data, hematological and biochemical obtained were submitted to analysis of variance. We used the Tukey test with α = 0.05 probability, to compare the means. There were no statistical difference between the treatments on the performance parameters and biochemical and blood parameters, except plasma proteins for between 19 and 21, which increased with the inclusion of glycerin, and reticulocytes that reduced with the inclusion of glycerin. The inclusion of up to 12% glycerin with 1.4% residual methanol in broiler diets (8 to 42 days of age) can be performed without loss in performance and health.(AU)
Asunto(s)
Animales , Pollos/crecimiento & desarrollo , Dieta/veterinaria , Metanol/uso terapéutico , Glicerol/análisis , Alimentación Animal/análisis , Sodio en la Dieta/análisisRESUMEN
Em função da grande variabilidade na composição da glicerina oriunda do biodiesel, torna-se imprescindível a busca por informações que contribuam estabelecê-la com uma alternativa na alimentação de aves. O objetivo deste estudo foi avaliar o efeito da inclusão de glicerina com alto de teor de metanol em dietas para frangos de corte sobre o desempenho e parâmetros sanguíneos. Foram utilizados 90 pintos de corte machos da linhagem Cobb, com 8 dias de idade, distribuídos em um delineamento inteiramente casualizado com três tratamentos (níveis de inclusão de 0, 6 e 12% de glicerina) e seis repetições de cinco aves cada, totalizando 18 unidades experimentais. As dietas foram formuladas a base de milho e farelo de soja para atender as exigências nutricionais e a glicerina utilizada continha 1,4% de metanol e 3158Kcal/kg de energia metabolizável. Aos 21, 33 e 42 dias de idade as sobras de ração e as aves foram pesadas para determinação do consumo de ração, peso médio, ganho de peso e conversão alimentar. Foram colhidos de 1 a 3mL de sangue venoso das aves, nos últimos dias de cada fase de criação (19-21, 31-33 e 40-42 dias de idade), para determinação do hematócrito, concentração de hemoglobina, reticulócitos, proteínas plasmáticas totais e fibrinogênio. Para avaliação da bioquímica sérica foram colhidos sangue venoso das aves sem anticoagulante, apenas na fase final da criação (40-42 dias). Os dados de desempenho, parâmetros hematológicos e bioquímicos obtidos foram submetidos à análise de variância. Utilizou-se o teste de Tukey com α=0,05 de probabilidade, para comparação das médias. Não foram observadas diferença estatística dos tratamentos sobre as variáveis de desempenho, parâmetros sanguíneos e bioquímicos, exceto para as proteínas plasmáticas entre 19 e 21, que aumentaram com a inclusão de glicerina, e para os reticulócitos que reduziram com a inclusão de glicerina. A inclusão de até 12% de glicerina com 1,4% de metanol residual em dietas de frangos de corte de 8 a 42 pode ser realizada sem prejuízos no desempenho e saúde dos mesmos.(AU)
Due to the great variability in the composition of glycerin derived from the biodiesel, it is essential to search for information which helps establish it with an alternative in poultry feed. The aim of this study was to evaluate the effect of inclusion of glycerin with high methanol content in diets for broilers on performance and blood parameters. They used 90 Cobb male broiler chicks with 8 days old, distributed in a completely randomized design with three treatments (0, 6 and 12% glycerin inclusion levels) and six replications of five birds each, a total of 18 experimental units. Diets were formulated based on corn and soybean meal to meet the nutritional requirements and glycerin used contained 1.4% methanol and 3158Kcal/kg of metabolizable energy. At 21, 33 and 42 days of age the remains of feed and the birds were weighed to determine the feed intake, body weight, body weight gain and feed conversion. Were collected 1 to 3ml of venous blood of the birds during the last days of each phase (19 to 21, 31 to 33 and 40 to 42 days of age) for determination of hematocrit, hemoglobin concentration, reticulocyte total plasma proteins and fibrinogen. To evaluate the serum biochemistry were collected venous blood of birds without anticoagulant, only in the final phase (40 to 42 days). Performance data, hematological and biochemical obtained were submitted to analysis of variance. We used the Tukey test with α = 0.05 probability, to compare the means. There were no statistical difference between the treatments on the performance parameters and biochemical and blood parameters, except plasma proteins for between 19 and 21, which increased with the inclusion of glycerin, and reticulocytes that reduced with the inclusion of glycerin. The inclusion of up to 12% glycerin with 1.4% residual methanol in broiler diets (8 to 42 days of age) can be performed without loss in performance and health.(AU)
Asunto(s)
Animales , Pollos/crecimiento & desarrollo , Dieta/veterinaria , Metanol/uso terapéutico , Glicerol/análisis , Alimentación Animal/análisis , Sodio en la Dieta/análisisRESUMEN
O presente trabalho foi planejado para testar os diferentes estágios de desenvolvimento encontrados no quarto dia após injeçäo de HCG em camundongos superovulados, afetam as taxas de desenvolvimento dos embriöes, criopreservados em uma soluçäo 3M de metanol.Foram criopreservados embriöes nos estágios de: 1) mórula, 2) blastocisto jovem (aqueles em que a cavidade ocupasse menos do que 50% do volume do embriäo), e 3) blastocisto (aqueles em que a cavidade ocupasse mais do que 50% do volume do embriäo). Os embriöes foram colocados diretamente numa soluçäo 3M de metanol em PBSS, a temperatura ambiente, durante 10 minutos, acondicionados em "paillets" de 0,25 ml, e colocados no aparelho de criopreservaçäo, diretamente, a 10§C. Após 5 minutos a essa temperatura, foi induzida a formaçäo de gelo. Uma vez transcorridos 6 minutos de equilíbrio, após a nucleaçäo a 10§C, os embriöes foram submetidos a queda de temperatura de 0,5§C, por minutos, até atingir a temperatura de 30§C, quando foram mergulhados diretamente em nitrogênio líquido a 196§. Näo houve diferença estatisticamente significativa, na percentagem de desenvolvimento, em cultura, entre os embriöes criopreservados nos estágios de mórula e blastocisto jovem (p> 0,05) mas houve uma diferença significativa (p<0,05) dos embriöes criopreservados, no estágio de blastocisto, quando comparado com o estágio de mórula e blastocisto jovem.
Asunto(s)
Crioprotectores/uso terapéutico , Congelación , Metanol/uso terapéutico , Ratones/crecimiento & desarrollo , Estructuras EmbrionariasRESUMEN
Of 433 schistosomiasis mansoni patients in St. Lucia who were treated with hycanthone (3 mg/kg of body weight), 190 were seen 2 years after treatment and 143 of these had attended all follow-up examinations at 6 weeks, 6 months, 1 year and 2 years. Viable eggs were not detected in 86% at 1 year nor in 76% at 2 years. The reinfection rate, as judged by a significant increase in egg excretion, was 15% and was related to the geographic area to which the patient returned. Extremely high total reduction in egg excretion (98%) was achieved through 1 year, and even with reinfections this fell only to 87% at 2 years. Liver and spleen enlargement was related to intensity of infection and responded to treatment in 92% and 83% of instances, respectively. Among patients with hepatosplenomegaly, those 15 years or older showed less clinical response than younger patients but were too few for statistical comparison.
Asunto(s)
Schistosoma mansoni , Esquistosomiasis/tratamiento farmacológico , Esquistosomicidas/uso terapéutico , Tioxantenos/uso terapéutico , Adolescente , Adulto , Niño , Etilenodiaminas/administración & dosificación , Etilenodiaminas/efectos adversos , Etilenodiaminas/uso terapéutico , Heces/parasitología , Estudios de Seguimiento , Hepatomegalia/inducido químicamente , Humanos , Metanol/administración & dosificación , Metanol/efectos adversos , Metanol/uso terapéutico , Recuento de Huevos de Parásitos , Esquistosomiasis/parasitología , Esquistosomicidas/administración & dosificación , Esquistosomicidas/efectos adversos , Esplenomegalia/inducido químicamente , Tioxantenos/administración & dosificación , Tioxantenos/efectos adversos , Indias OccidentalesRESUMEN
Of 433 schistosomiasis mansoni patients in St. Lucia who were treated with hycanthone ( 3mg/kg of body weight), 190 were seen 2 years after treatment and 143 of these had attended all follow-up examinations at 6 weeks, 6 months, 1 year, and 2 years. Viable eggs were not detected in 86 percent at 1 year nor in 76 percent at 2 years. The reinfection rate, as judged by a significant increase in egg excretion, was 15 percent and was related to the geographic area to which the patient returned. Extremely high total reduction in egg excreation (98 percent) was achieved through 1 year, and even with reinfections this fell only to 87 percent at 2 years. Liver and spleen enlargement was related to intensity of infection and responded to treatment in 92 percent and 83 percent of instances, respectively. Among patients with hepatosplenomegaly, those 15 years or older showed less clinical response than younger patients but were too few for statistical comparison. (AU)
Asunto(s)
Humanos , Niño , Adulto , Schistosoma mansoni , Esquistosomiasis/tratamiento farmacológico , Esquistosomicidas/uso terapéutico , Tioxantenos/uso terapéutico , Metanol/administración & dosificación , Metanol/efectos adversos , Metanol/uso terapéutico , Etilenodiaminas/administración & dosificación , Etilenodiaminas/efectos adversos , Etilenodiaminas/uso terapéutico , Heces/parasitología , Hepatomegalia/inducido químicamente , Recuento de Huevos de Parásitos , Esquistosomiasis/parasitología , Esquistosomicidas/administración & dosificación , Esquistosomicidas/efectos adversos , Esplenomegalia/inducido químicamente , Tioxantenos/administración & dosificación , Tioxantenos/efectos adversos , Indias OccidentalesAsunto(s)
Antihelmínticos/uso terapéutico , Etilenodiaminas/uso terapéutico , Infecciones por Salmonella/complicaciones , Esquistosomiasis/complicaciones , Tioxantenos/uso terapéutico , Adolescente , Adulto , Anciano , Peso Corporal , Niño , Evaluación de Medicamentos , Etilenodiaminas/efectos adversos , Femenino , Humanos , Inyecciones Intramusculares , Masculino , Metanol/efectos adversos , Metanol/uso terapéutico , Persona de Mediana Edad , Esquistosomiasis/tratamiento farmacológico , Esquistosomicidas/efectos adversos , Esquistosomicidas/uso terapéutico , Tioxantenos/efectos adversosAsunto(s)
Antihelmínticos/efectos adversos , Enfermedad Hepática Inducida por Sustancias y Drogas , Etilenodiaminas/efectos adversos , Parasitosis Hepáticas/tratamiento farmacológico , Hígado/efectos de los fármacos , Esquistosomiasis/tratamiento farmacológico , Tioxantenos/efectos adversos , Adulto , Evaluación de Medicamentos , Etilenodiaminas/uso terapéutico , Femenino , Humanos , Inyecciones Intramusculares , Metanol/efectos adversos , Metanol/uso terapéutico , Schistosoma mansoni , Esquistosomicidas/efectos adversos , Esquistosomicidas/uso terapéutico , Tioxantenos/uso terapéuticoAsunto(s)
Antihelmínticos/efectos adversos , Enfermedad Hepática Inducida por Sustancias y Drogas/complicaciones , Etilenodiaminas/efectos adversos , Hígado/efectos de los fármacos , Esquistosomiasis/tratamiento farmacológico , Tioxantenos/efectos adversos , Adulto , Antihelmínticos/uso terapéutico , Etilenodiaminas/uso terapéutico , Humanos , Masculino , Metanol/efectos adversos , Metanol/uso terapéutico , Esquistosomicidas/efectos adversos , Esquistosomicidas/uso terapéutico , Tioxantenos/uso terapéuticoAsunto(s)
Antihelmínticos/farmacología , Antimonio/farmacología , Etilenodiaminas/farmacología , Niridazol/farmacología , Schistosoma mansoni/efectos de los fármacos , Serotonina/farmacología , Tioxantenos/farmacología , Animales , Antihelmínticos/toxicidad , Biomphalaria , Computadores , Relación Dosis-Respuesta a Droga , Tecnología de Fibra Óptica , Metanol/uso terapéutico , Movimiento/efectos de los fármacos , Parasitología/instrumentación , Puerto Rico , Schistosoma mansoni/fisiología , Esquistosomicidas/uso terapéutico , Serotonina/fisiologíaRESUMEN
WR 33063, a phenanthrene methanol, was studied in human volunteers for tolerance and toxicity. In normal volunteers, it was possible to give 4.6 g in four divided doses without adverse effect for 10 days. At this dose level, there was neither evidence of photosensitivity nor adverse renal or cardiac effect. At a dose level of 1.6 g in four divided doses for 6 days, WR 33063 cured 18 of 23 nonimmune volunteers infected with the Smith strain of Plasmodium falciparum from Vietnam. In addition, infections due to the Marks and Braithwaite Vietnam strains were also treated because these strains represent a major therapeutic challenge to chloroquine; six of six and two of three volunteers, respectively, were cured. With the Malayan Camp strain, 1.6 g in four divided doses for 6 days cured all of five volunteers. The African Uganda I strain of chloroquine-responsive malaria was even more responsive to WR 33063; all of six men who received 1.6 g in four divided doses for 6 days were cured, and all of three men who received this same dosage for 3 days were cured. One subject infected with a Haitian strain of P. falciparum was treated and cured. Blood-induced infections with the Chesson strain of P. vivax also responded well to WR 33063 with four of five men cured. In all, 52 men received WR 33063 in tolerance trials, and 59 men with experimental malaria and one man with clinical malaria were treated with WR 33063.