ABSTRACT
Statins are inhibitors of the 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, thereby inhibiting cell synthesis of cholesterol and isoprenoids. Moreover, several studies have been evaluating pleiotropic effects of statins, mainly because they present neuroprotective effects in various pathological conditions. However, knowledge about behavioral effects of statins per se is relatively scarce. Considering these facts, we aimed to analyze behavioral responses of atorvastatin or simvastatin-treated mice in the open field test, elevated plus maze and object location test. Atorvastatin treatment for 7 consecutive days at 1 mg/kg or 10 mg/kg (v.o.) or simvastatin 10 mg/kg or 20 mg/kg enhanced cognitive performance in object location test when compared to control group (saline-treated mice). Simvastatin effects on mice performance in the object location test was abolished by post-training infusion of the beta-adrenoceptor antagonist propranolol. Atorvastatin and simvastatin did not change the behavioral response in open field and elevated plus-maze (EPM) tests in any of the used doses. These data demonstrate the positive effects of both statins in cognitive processes in mice, without any alteration in locomotor parameters in the open field test or anxiolytic-like behavior in EPM. In conclusion, we demonstrate that atorvastatin and simvastatin per se improve the cognitive performance in a rodent model of spatial memory and this effect is related to beta-adrenergic receptors modulation.
Subject(s)
Cognition/drug effects , Exploratory Behavior/drug effects , Hydroxymethylglutaryl-CoA Reductase Inhibitors/pharmacology , Receptors, Adrenergic, beta/metabolism , Adrenergic beta-Antagonists/pharmacology , Analysis of Variance , Animals , Dose-Response Relationship, Drug , Locomotion/drug effects , Male , Maze Learning/drug effects , Memory, Short-Term/drug effects , Mice , Propranolol/pharmacology , Random AllocationABSTRACT
Echinodorus macrophyllus leaf has been used in Brazilian folk medicine to treat inflammatory conditions and kidney dysfunctions. The present study evaluated the effects of leaf ethanolic extract from E. macrophyllus (EEEm) in acute and subchronic models of inflammation. The EEEm was found to cause significant and potent inhibition of carrageenan- and dextran-induced paw edema in rats and marked decreases in the exudate volume and leukocyte migration in rats with carrageenan-induced pleurisy, the vascular permeability increase induced by intraperitoneal acetic acid, and the croton oil-induced topical ear edema in mice. On the other hand, the EEEm was not active in the test model of cotton pellet-induced granuloma in rats. Phytochemical analysis with E. macrophyllus leaves revealed the presence of triterpenoids, steroids, flavones, flavonols, and xanthones. Two flavonoids were isolated from the ethyl acetate fraction and identified as isovitexin and vitexin. Our results support the traditional use of E. macrophyllus leaves in the treatment of acute inflammatory conditions.
Subject(s)
Alismataceae/chemistry , Anti-Inflammatory Agents/administration & dosage , Phytotherapy , Plant Extracts/administration & dosage , Plant Leaves/chemistry , Acetic Acid , Animals , Capillary Permeability/drug effects , Carrageenan , Croton Oil , Dermatitis, Contact/drug therapy , Dermatitis, Contact/etiology , Dextrans , Edema/chemically induced , Edema/drug therapy , Flavonoids/analysis , Male , Mice , Peritoneum/blood supply , Plant Extracts/chemistry , Pleurisy/chemically induced , Pleurisy/drug therapy , Rats , Rats, Wistar , Triterpenes/analysisABSTRACT
A planta Pectis jangadensis, popularmente conhecida como "roxinha", "erva do carregador" ou "coentro da chapada" é utilizada em chás pela população matogrossense, como calmante. Não há estudo na literatura sobre qualquer atividade farmacológica dessa planta. Nosso objetivo foi avaliar atividade analgésica de seu extrato hidro-alcoólico nas doses de 100, 500 e 1000 mg/kg pelos métodos de Contorções induzidas pelo ácido acético e teste da formalina. Os nossos resultados demonstram que não houve diferença significativa entre o grupo controle e os grupos tratados com diferentes doses do extrato tanto em relação ao número de contorções induzidas pelo ácido acético quanto ao tempo de lambedura da pata, na fase 1 e 2, induzida pela formalina. Portanto, pelo menos, por via oral, parece que o extrato hidro-alcoólico da Pectis jangadensis não apresenta atividade analgésica.
"Preliminary evaluation of Pectis jangadensis (S. Moore) analgesic activity's". The plant Pectis jangadensis, popularly known as "roxinha", "erva do carregador" or "coentro da chapada" is used in teas by the matogrossense's people, as a calmative. There isn't any study in the literature about its pharmacologic activity. Our object was to evaluate its extract hidroalcoolic analgesic activity in doses of 100, 500 and 1000 mg/kg by the methods of abdominal writhing induced by acetic acid and the Formalin test. The results show that there wasn't significant difference between the control groups and the groups treated with different doses of the extract in both testes. Therefore, at least by oral, seems that the Pectis jangadensis' hidroalcoolic extract doesn't have analgesic activity.
ABSTRACT
Foram sintetizados derivados para-substituidos do (R,S)-3-fenil-3-(O,O-dietilfosfono)-propanoato de etila, compreendendo 14 substancias incluindo o proprio. Todas as substancias foram caracterizadas por analise elementar, espectroscopia no infravermelho e ultravioleta, espectrometria de RMN-'H POT. 1' e RMN-'C POT. 13'. Foram determinados experimentalmente alguns parametros fisico-quimicos, com indices de refracao, densidades, cromatograficos em camada delgada, Log P. Outros parametros fisico-quimicos e estruturais foram estimados atraves de calculos teoricos utilizando tecnicas computacionais. Com excecao do (R,S)-3-fenil-3-(O,O-dietilfosfono)-propanoato de etila, todas as substancias sintetizadas nao foram ainda descritas em literatura
Subject(s)
Phosphonoacetic Acid/pharmacology , Phosphonoacetic Acid/chemical synthesis , Esters/chemical synthesis , Trypanosoma cruzi/drug effects , Phosphonoacetic Acid/therapeutic use , Antiprotozoal Agents/therapeutic use , Chemistry, Pharmaceutical , Chagas Disease/drug therapy , Magnetic Resonance Spectroscopy/methods , Spectrophotometry, Infrared , Spectrophotometry, Ultraviolet , Structure-Activity RelationshipABSTRACT
Foram sintetizadas tres series de derivados do acido 3-fosfonopropionico, compreendendo 22 substancias, das quais 16 ainda nao descritas na literatura. Todas as substancias foram caracterizadas por analise elementar, espectroscopia no infravermelho e espetrometria de ressonacia magnetica protonica. Os compostos obtidos foram encaminhados para ensaios experimentais na doenca de Chagas
Subject(s)
Propionates/chemical synthesis , Chagas Disease/etiology , Phosphorus Acids/chemical synthesis , Spectrum Analysis , Propionates/analysis , Phosphorus Acids/analysisABSTRACT
Diversos derivados do acido 3-fosfonopropionico foram submetidos a ensaios in vivo e in vitro, contra formas tripomastigotas da cepa Y de Trypanosoma Cruzi. Nos ensaios in vivo, realizados em camundongos previamente infectados,os derivados ensaiados se mostraram inativos, sendo que os acidos (R,S)-3-fenil-3-fosfonopropionico e (R,S)-3-fenil-3-(0,0-dietilfosfono)-propionico foram letais para alguns dos animais. Nos ensaios in vitro efetuados em cultura de tecido os compostos ensaiados foram inativos, com excecao do (R,S)-3-fenil-3-(0,0-dietilfosfono)-propionato de etila, que apresentou alguma atividade.
