Orofacial antinociceptive effects of perillyl alcohol associated with codeine and its possible modes of action

Abstract This study evaluated the orofacial antinociceptive effect of (S)-(-)-perillyl alcohol (PA) associated with codeine (C) and investigated the possible molecular anchorage mechanisms of PA. Mice (n = 5 per group) were treated with PA alone and associated with codeine and assigned to the following groups: 75.0 mg/kg PA; 75.0 mg/kg PA + C 30 mg/kg; PA 37.5 mg/kg + C 15.0 mg/kg; C 30.0 mg/kg; and control. Nociception was induced by formalin, capsaicin, and glutamate, and was quantified based on the duration (in seconds) of face grooming. The possible mechanisms of action were evaluated by molecular docking study. In the formalin test, PA75/C30 presented an effect in the neurogenic (p < 0.0001) and inflammatory (p < 0.005) phases. Mice treated with PA75 (p < 0.0001) and PA75/C30 (p < 0.0005) showed a reduced nociceptive behavior in the capsaicin test. Glutamate-induced nociception also was blocked by PA75 (p < 0.0005) and C30 (p < 0.0005). The molecular anchorage analysis indicated high negative binding energy values for the evaluated receptors, especially glutamate receptors (AMPA -79.57 Kcal/mol, mGLUR6 -71.25, and NMDA -66.33 Kcal/mol). PA associated with codeine showed orofacial antinociceptive activity, with theoretical evidence of interaction with glutamate receptors.

Non-clinical study of the anxiolytic effect of Citrus aurantium L. essential oil in an inclusion complex with 2-hydroxypropyl-ß-cyclodextrin

Anxiety in the world population has increased significantly; the problem has encouraged studies regarding innovative alternatives for treatment. Research with Citrus aurantium L. essential oil (CEO) has revealed positive results with anxiolytic effects in both animals and humans. However, certain limitations affect its storage and preservation, its efficiency in therapy, and determination of adequate posologies. The potential use of cyclodextrins as drug carriers has been successfully explored. This study aims to assess the anxiolytic potential of a CEO/2-hydroxypropyl-ß-cyclodextrin (HP-ß-CD) inclusion complex. Preparation of the inclusion complex was performed using the Alpha 1-2 LDplus lyophilizer. To allow formation, and avoid loss of volatiles to the atmosphere, Limonene (LIM), the main compound in CEO, together with HP-ß-CD in a molar ratio of (1: 1M) was dispersed in ethanol for 36 hours using a laboratory shaker at room temperature (25°C). Non-clinical murine pharmacological tests were performed for anxiety assessment in experimental and control groups. To assess anxiety and motor impairment, the animals were evaluated using the elevated plus maze, open field, and rota-rod tests. Satisfactory results of the anxiolytic effect of the OEC complexed in HP-ß-CD were observed, with the indication of an potentiation of the effect with doses lower than 500 mg/kg and 250 mg/kg complexed, suggesting improvement in the anxiolytic properties of the OEC.

Orofacial antinociceptive activity and anchorage molecular mechanism in silico of geraniol

Abstract We aimed to evaluate the orofacial antinociceptive effect of geraniol in mice and its molecular anchorage mechanism. Seven mice per group (probabilistic sample) were treated with geraniol (12.5, 25 and 50 mg/kg, i.p.), morphine (6 mg/kg, i.p.) and vehicle (saline + Tween 80 at 0.2%, i.p.) 30 minutes prior to the beginning of the experiment. Injecting glutamate (25 μM), capsaicin (2.5 μg) and formalin (2%) into the right upper lip (perinasal) of the mouse induced nociception. Behavioral analysis of the animals considered the friction time (in seconds) of the mentioned region using hind or front paws by a researcher blinded to the treatment groups. The statistical analysis was performed blindly, considering α = 5%. The results showed that in the glutamate and capsaicin tests, concentrations of 25 mg/kg and 50 mg/kg presented antinociceptive activity (p < 0.005, power> 80%). In the formalin test, geraniol was able to reduce nociception at a concentration of 50 mg/kg (p < 0.005, power> 80%). In the molecular anchorage study, high values of binding between the evaluated substance and receptors of glutamate were observed (metabotropic glutamate receptor, -87.8501 Kcal/mol; N-methyl-D-aspartate, -86.4451 Kcal/mol; α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid, -85.6755 Kcal/mol). Geraniol presented orofacial antinociceptive activity, probably by interacting with glutamate-related receptors.

Antinociceptive activity of Sargassum polyceratium and the isolation of its chemical components

Abstract Marine algae have been the focus of important studies over the past fifty years, with a considerable number of components important to chemists and taxonomists having been isolated and characterized. The scientific data available on Sargassum polyceratium are extremely limited. The objective of the present study was to evaluate the antinociceptive activity of an ethanol extract of S. polyceratium and to isolate its components. Intraperitoneal treatment with ethanol extract of S. polyceratium reduced the number of acetic acid-induced writhes and the amount of time spent in paw-licking in the second phase of the formalin test. Ethanol extract of S. polyceratium also reduced the amount of time spent in paw-licking in the glutamate test; however, there was no difference in the reaction time in the hot plate test at any of the doses tested. The chemical components isolated from ethanol extract of S. polyceratium were identified using one- and two-dimensional spectroscopic methods such as infrared spectroscopy, mass spectrometry and 1H and 13C nuclear magnetic resonance spectroscopy. The analytical results were also compared with data obtained in the literature. The following porphyrin derivatives were isolated from S. polyceratium: 132-hydroxy-(132-R)-pheophytin-a, 132-hydroxy-(132-S)-pheophytin-a, pheophytin-a, and the steroid fucosterol. The present results indicate that the ethanol extract of S. polyceratium has antinociceptive activity. In addition, four new substances were isolated from the species evaluated.

Toxicidade Aguda em Ratos Wistar Tratados com o Extrato Etanólico de Dioclea grandiflora Mart. Ex Benth (Fabaceae) (EEDg) / Acute Toxicity of Dioclea grandiflora Mart. Ex Benth (Fabaceae) Ethanolic Extract in Wistar Rats

Introdução: A Dioclea grandiflora, conhecido como Mucunã de caroço,atua sobre o Sistema Nervoso Central, doenças da próstata e pedrasnos rins. Objetivo: Realizar estudo toxicológico não clínico agudo, emratos, com base na Instrução Normativa nº4, de 18 de junho de 2014da Agência Nacional de Vigilância Sanitária (ANVISA). Material eMétodos: Foram utilizados ratos Wistar, ambos os sexos, dose 2000mg/kg, via oral, do extrato etanólico bruto de Dioclea grandifloraadministrado a um grupo tratado e um grupo controle (veículo). Apósa administração, os parâmetros de comportamento foi observado por30, 60, 90, 120, 180 e 240 minutos, consumo de ração e água,parâmetros hematológicos e bioquímicos. O número de sobreviventescontabilizados para determinar a DL50. Resultados: Houve aumentoestatisticamente significativo no consumo de água (Controle:160,4±5,85; Tratado: 201,3±8,55) e ração das fêmeas (Controle:95,98±3,02; Tratado: 113,1±2,42) e aumento estatisticamentesignificativo no consumo de água (Controle: 236,7±6,43; Tratado:267,5±8,72) e ração dos machos (Controle: 152,4±2,51; Tratado:177,64,15). Aumento estatisticamente significativo na albumina dosmachos (Controle: 3,2±0,08; Tratado: 3,6±0,08), nas fêmeas reduziuestatisticamente significativo a fosfatase alcalina (Controle:198,5±18,81; Tratado: 99,97±16,02) , proteína total (Controle:7,85±0,09; Tratado: 6,85±0,24) e globulinas (Controle: 4,28±0,14;Tratado: 3,27±0,27). Diminuiu estatisticamente significativo o númerode hemácias nas fêmeas (Controle: 10,18±0,28; Tratado: 9,62±0,18).Conclusão: De acordo com os resultados a DL50 foi superior à dosetestada, porém são necessários estudos toxicológicos de longa duraçãopara atestar a segurança de seu uso...

Introduction: Dioclea grandiflora, known as Mucunã de caroço, acts onthe central nervous system, and against prostate disease and kidneystones. Objective: To perform a nonclinical acute toxicology study inrats following the Normative Instruction #4 as of June 18th 2014 of theNational Health Surveillance Agency (ANVISA). Material and Methods:Wistar rats of both sexes were used in the study. A dose of 2000 mg/kg of Dioclea grandiflora ethanolic extract was administered orally tothe test group. A control group using only the vehicle was also included.Then behavioral parameters were monitored for 30, 60, 90, 120, 180,and 240 minutes after feed and water intake, along with hematologicaland biochemical parameters. The number of survivors was recordedto determine the LD50. Results: There was a statistically significantincrease in water (Control: 160.4 ± 5.85; Treated: 201.3 ± 8.55), andfeed intake (Control: 95.98 ± 3.02; Treated: 113.1 ± 2.42) for femalerats; and a statistically significant increase in water (Control: 236.7 ±6.43; Treated: 267.5 ± 8.72) and feed intake (Control: 152.4 ± 2.51;Treated: 177.6 ± 4.15) for males. A statistically significant increase inalbumin levels was observed for males (Control: 3.2 ± 0.08; Treated:3.6 ± 0.08), and a decrease in alkaline phosphatase (Control: 198.5 ±18.81; Treated: 99.97 ± 16.02), total protein (Control: 7.85 ± 0.09;Treated: 6.85 ± 0.24) and globulin (Control: 4.28 ± 0.14; Treated: 3.27± 0.27) was found for females. Also, in females the number of redblood cells was found to be significantly reduced (Control: 10.18 ±0.28; Treated: 9.62 ± 0.18). Conclusion: According to the results, theLD50 value found was higher than that of the tested dose. Howeverlong-term toxicology studies are needed to further prove the safetyof the extract...

Central nervous system effects of Dioclea grandiflora pods on mice / Efectos en el sistema nervioso central de la vaina de Dioclea grandiflora en camundongos

Many plant substances are known for their interference with the central nervous system (CNS). Dioclea grandiflora Mart. Ex. Benth (Fabaceae) is a plant used in folk medicine to treat prostate disorders and kidney stones whose extracts from its seeds and root barks were reported to have a significant activity on the CNS and analgesic effect in rodents. In this study, the psychopharmacological activities of D. grandiflora were investigated, using the pods of this plant. Swiss mice were submitted to acute treatments with ethanol extract from the pods of D. grandiflora (EDgP) at doses of 75, 150 and 300 mg/kg by intraperitoneal administration followed by the evaluation of anxiety, depressant and anticonvulsant-related responses. The treatment with EDgP produced a depressant activity on the CNS and a sedative effect in mice. These findings suggest that EDgP has a central activity in mice, indicating an anxiogenic effect.

Varias sustancias de plantas son conocidas por su acción en el sistema nervioso central (SNC). La Dioclea grandiflora Mart. Ex. Benth (Fabaceae) es una planta utilizada en la medicina popular para tratar enfermedades en la próstata y piedras en los riñones, cuyos extractos de sus semillas y de las cáscaras de sus raíces presentan una actividad significativa sobre el SNC y efecto analgésico en roedores. En este estudio, las actividades psicofarmacológicas de D. grandiflora fueron investigadas, utilizando la vaina de la planta. Camudongos Swiss fueron sometidos a tratamientos agudos por la administración intraperitoneal del extracto etanólico de la vaina de D. grandiflora (EDgP) en dosis de 75, 150 y 300 mg/kg administrados intraperitonealmente seguida por la evaluación de respuestas relacionadas con la ansiedad, depresión y anticonvulsivo. El tratamiento con EDgP produjo una actividad depresora sobre el sistema nervioso central y un efecto sedante en camundongos. Estos resultados sugieren que EDgP tiene una actividad central en camundongos, indicando un efecto ansiogénico.

Avaliação da toxicidade aguda e das alterações histopatológicas em camundongos tratados com fitol / Assessment of acute toxicity and histopathological changes in mice treated with phytol

O fitol, (3,7,11,15-tetrametilhexadec-2-en-1-ol), é um diterpeno pertencente ao grupo dos álcoois acíclicos insaturados de cadeia longa e ramificada. É um componente da molécula da clorofila, presente em folhas verdes de várias plantas medicinais. Entretanto, pouco é descrito na literatura sobre os possíveis efeitos toxicológicos produzidos pelo fitol. O objetivo do nosso estudo foi avaliar a toxicidade aguda do fitol, após administração intraperitoneal para determinação da dose letal 50% (DL50) e os efeitos sobre os parâmetros bioquímicos, hematológicos e histopatológicos no hipocampo e corpo estriado de camundongos adultos tratados com fitol nas doses de 25, 50 e 75 mg/kg. Os testes para determinação do grau de toxicidade aguda, bem como a investigação da DL50, revelou que o valor é aproximadamente 1153.39 mg/kg. Os camundongos tratados com as doses selecionadas do fitol a partir da DL50 apresentaram todos os parâmetros hematológicos dentro da faixa de referência, observando-se alterações nos valores dos linfócitos. Por sua vez, a maioria dos valores dos parâmetros bioquímicos diminuiu em todas as doses testadas (p<0,05). Em nosso estudo, apenas os animais tratados com fitol na dose de 75 mg/kg demonstraram uma discreta vacuolização no corpo estriado e um discreto comprometimento caracterizado por vacuolização no hipocampo em apenas um dos animais. Nossos resultados indicam que o tratamento com fitol não produz alterações hematológicas, bioquímicas e histopatológicas cerebrais em camundongos. O estudo toxicológico pré-clínico com fitol demonstrou que o produto avaliado possui discreta toxicidade aguda por via intraperitoneal, sendo estes dados uma contribuição para pesquisas com compostos obtidos de plantas medicinais com potencial farmacológico. Porém, ressalta-se a necessidade de futuras pesquisas que possibilitem comparar os resultados em outras vias, bem como para realizar análises anatomopatológicas dos animais tratados com fitol, para assegurar o uso seguro deste diterpeno.

Phytol (3,7,11,15-tetramethylhexadec-2-en-1-ol) is a diterpene belonging to the group of acyclic unsaturated long-chain branched alcohols. It is a component of the chlorophyll molecule, present in green leaves of various medicinal plants. However, there is little in the literature about the possible toxic effects produced by phytol. The aim of our study was to assess the acute toxicity of phytol after intraperitoneal (ip) administration, by determining its 50% lethal dose (LD50) and effects on biochemical parameters, hematology and the histopathology of the hippocampus and corpus striatum of adult mice treated with doses of 25, 50 and 75 mg/kg phytol. The acute toxicity tests and investigation of the LD50 revealed its value to be approximately 1153.39 mg/kg. Mice treated with sublethal doses of phytol based on the LD50 showed all hematological parameters within their reference ranges, with small changes in the lymphocyte count. In turn, most of the biochemical parameters decreased at all doses tested (p<0.05). In our study, only those animals treated with phytol at a dose of 75 mg/kg showed slight vacuolation in the corpus striatum and a slight impairment characterized by vacuolation in the hippocampus in one animal. Our results indicate that treatment with phytol produces no hematological, biochemical or brain histopathological changes in the mice. The preclinical toxicological study with phytol showed that it has slight acute toxicity when injected ip. These data contribute to research on natural compounds obtained from medicinal plants with pharmacological potential. However, we emphasize the need for future research to enable results obtained by other routes to be compared, as well as to conduct pathological analysis in animals treated with phytol, to ensure the safe use of this diterpene.

Parâmetros bioquímicos e hematológicos de ratos wistar e camundongos swiss do biotério professor Thomas George / Biochemical and hematological parameters of wistar rats and swiss mice in the professor Thomas George animal laboratory

Objetivo: Este trabalho teve como objetivo estabelecer valores de referência de parâmetros bioquímicos e hematológicos de roedores provenientes do Biotério Professor Thomas George do Laboratório de Tecnologia Farmacêutica (LTF) da Universidade Federal da Paraíba(UFPB). Metodologia: Avaliaram-se o perfil hematológico,hemograma, contagem de plaquetas, e a determinação bioquímica de vários constituintes plasmáticos: glicose, uréia,creatinina, colesterol total, triglicerídeos, ácido úrico,proteínas totais e frações, fosfatase alcalina, transaminases,sódio, potássio, cálcio e magnésio. Foram utilizados ratos Wistar albinos e camundongos Swiss, adultos, pesando 150a 350g e 15 a 35g, respectivamente, totalizando 40 para cada espécie animal (20 machos e 20 fêmeas). Resultados:Algumas variações foram detectadas entre os valores obtidos nos animais investigados e os parâmetros da literatura. Nos ratos, observaram-se valores inferiores para leucócitos e eosinófilos, e para camundongos obtiveram-se valores elevados para plaquetas, AST, ALT, fosfatase alcalina, globulina, íons cálcio e magnésio, em comparação com dados na literatura. Conclusão: Portanto, é importante oconhecimento e a divulgação dos valores de parâmetros fisiológicos dos animais de experimentação, considerando que podem exibir variações influenciadas por vários fatores que devem ser levados em consideração nas pesquisas experimentais, como sexo, linhagem e genótipo.

Objective: The objective of the present study was to establish reference values for the biochemical and hematological parameters of rodents from the Professor Thomas George animal laboratory of the Pharmaceutical Technology Laboratory, Federal University of Paraíba. Methodology: The parameters evaluated consisted of hematological profile withfull blood and platelet counts, as well as serum components including glucose, urea, creatinine, total cholesterol, triglycerides, uric acid, total protein and protein fractions, alkaline phosphatase, transaminases, sodium, potassium, calcium and magnesium. Adult albino Wistar rats and Swissmice (20 males and 20 females of each species), weighing150-350 grams and 15-35 grams, respectively, were used inthe study. Results: Variations were detected between values obtained in the animals and parameters established in theliterature. In rats, leukocyte and eosinophile counts werelower, while in mice, platelet counts, AST, ALT, alkalinephosphatase, globulin, calcium and magnesium levels werehigher compared to data published in the literature. Conclusion: In conclusion, the physiological parameters of experimental animals should be well established and made available in view of the variations that may exist as a result of various factors such as sex, lineage and geno type of the rodents that must be taken into consideration in experimental studies.

Analgesic effect of hydroalcoholic extract of Cissampelos sympodialis Eichl leaves / Efecto analgésico del extracto hidroalcoholico de las hojas de Cissampelos sympodialis Eichl

Cissampelos sympodialis Eichl is a species of the family Meniespermaceae known as “Milona”, which extracts showed low toxicity and several pharmacological activities as anti-inflammatory, anti-allergic or anti-depressive. In the present study two classic analgesia models in mice were used to evaluate the hydroalcoholic extract of C. sympodialis leaves (HAECs) at doses of 50, 100 and 200 mg/kg, i.p. In the test of writhing by acetic acid HAECs- treatment induced a significant reduction in the number of abdominal contortions in a dose-dependent manner (p <0,05). In the formalin test, HAECs-200 mg/kg induced a significant inhibition of the second phase (15-30 minutes) (p <0,05). Results suggest that the HAECs presented outlying antinociceptive peripheral activity probably related with the alleged anti-inflammatory proprieties of extracts of this plant.

Existen varios estudios que evidencian que la Cissampelos sympodialis posee atividad anti-inflamatoria, antialérgica, antidepresiva y de baja toxicidad. Este estudio evaluó los efectos de la administración intraperitoneal, del extracto hidroalcohólico de hojas de cissampelos sympodialis (EHACS), en las dosis de 50, 100 y 200 mg/Kg, en modelos de analgesia en camumdongos. En el modelo de las contracciones inducidas por el ácido acético (0,85 por ciento) fue encontrada una reducción en el número de contracciones proporcional a las dosis usadas (p<0,05). En el test de la reacción al formaldeído las dosis utilizadas no presentaron efecto significante en la primera fase del test (0-5 minutos). Sin embargo, la dosis de 200mg/Kg presentó una significante inhibición en la segunda fase (15 – 30 minutos) del test (p<0,05). Los resultados mostraron que el EHACS presentó una actividad antinociceptiva periférica probablemente relacionada con la alegada actividad anti-inflamatoria.

Uso da terapia não farmacológica, medicina alternativa e complementar na fibromialgia / Non-pharmacological therapy and complementary and alternative medicine in fibromyalgia

A fibromialgia é uma síndrome dolorosa crônica que afeta até 5 por cento da população mundial. Pode associar-se com distúrbios do sono, do humor e fadiga, e cursar com incapacidade funcional. Sua patogênese envolve distúrbio de modulação central da dor, comprometimento do sistema inibitório descendente e hiperatividade da substância P. Em função da vasta sintomatologia apresentada pelos pacientes e da natureza multifatorial da sua patogênese, seu tratamento ideal requer uma abordagem multidisciplinar incluindo a associação de terapia farmacológica e não farmacológica. A terapia farmacológica atualmente preconizada nessa síndrome inclui, entre outros compostos, antidepressivos, moduladores dos canais de cálcio, relaxantes musculares e analgésicos. O tratamento não farmacológico é realizado, na maioria dos casos, por meio de educação do paciente, atividade física aeróbica supervisionada e terapia cognitivo-comportamental. No entanto, muitos pacientes não apresentam respostas satisfatórias ou apresentam efeitos colaterais associados ao uso dos fármacos a longo prazo, além de referirem dificuldades em permanecer em uma terapia baseada em exercícios e medicina física. Há, portanto, um crescente interesse por parte dos médicos e pacientes por uma terapia alternativa e complementar na fibromialgia. Nesta revisão, os autores discorrem sobre as diversas modalidades terapêuticas empregadas nessa doença, enfatizando as evidências da terapia não farmacológica e do uso de medicina alternativa e complementar nesses pacientes.

Fibromyalgia is a chronic painful syndrome that affects up to 5 percent of the world population. It is associated with sleep and mood disorders, fatigue, and functional disability. Its pathogenesis involves a disorder of the central modulation of pain, impairment of the descending inhibitory system, and hyperactivity of substance P. Because of the extensive symptomatology of patients with fibromyalgia and its multifactorial pathogenesis, its ideal treatment requires a multidisciplinary approach including the association of pharmacological and non-pharmacological therapies. The pharmacological therapy currently recommended for the syndrome includes antidepressants, calcium-channel modulators, muscle relaxants, and analgesics. In most cases, the non-pharmacological treatment consists of patient education, supervised aerobic physical activity, and cognitive-behavioral therapy. However, many patients do not respond satisfactorily, or have side effects associated with the long-term use of drugs, in addition to reporting difficulties in adhering to a therapy based on exercises and physical medicine. Thus, physicians and patients are increasingly interested in an alternative and complementary therapy for fibromyalgia. This review approaches the different therapeutic modalities used in fibromyalgia, emphasizing the evidence of non-pharmacological therapy and use of alternative and complementary medicine for these patients.

Avanços no estudo da atividade ansiolítica do panax ginseng C. A. Meyer: [revisão] / Advances in the study of anxiolytic activity of panax ginseng C. A. Meyer: [review]

To focus on the current evidence on the anxiolytic activity of Panax ginseng C.A Meyer. Recent studies showed the anxiolytic effects of the constituents of the roots of this species. Triterpenoid saponins of ginseng known as ginsenosides, are the active chemical components of the roots of this plant likely related to its anxiolytic activity. The interaction of these components with ligands of GABA receptor, increasing its affinity for the receptor, decreased production of mRNA catabolic enzyme (Abat) and this inhibitory neurotransmitter GABA transporter (GAT1) are related events so far to the anxiolytic effect of ginseng.Both the white ginseng and red ginseng have anxiolytic properties.

Estudo enfoca as atuais evidências sobre a atividade ansiolítica do Panax ginseng C.A Meyer. Recentes pesquisas evidenciaram os efeitos ansiolíticos dos constituintes das raízes desta espécie. Saponinas triterpenóides de ginseng, conhecidos como ginsenosídeos, são os componentes químicos ativos das raízes desta planta relacionados à sua provável atividade ansiolítica. A interação destes constituintes com ligantes do receptor GABA, aumentando a sua afinidade pelo receptor, a diminuição da produção de RNAm da enzima catabólica (Abat) deste neurotransmissor inibitório e do transportador GABA (GAT1) são eventos relacionados até o momento ao efeito ansiolítico do ginseng. Tanto o ginseng branco como o ginseng vermelho apresentam propriedades ansiolíticas.

Evidência de uma ação central exercida pela fração total de alcalóides de Chondrodendron Platyphyllum em camundongos / Evidence of a central activity exerted by total alkaloid fraction of Chondrodendron Platyphyllum in mice

Avaliar a atividade de Chondrodendronplatyphyllum sobre o sistema nervoso central. Material eMétodos: Realizou-se testes gerais para avaliar o efeito dafração total de alcalóides sobre o SNC. A FTA nas doses de100, 200 e 400 mg/kg foi administrada em camundongos porvia i.p e foi realizado uma triagem farmacológica experimental,na qual foi avaliada a mudança comportamental dosanimais. No teste da potencialização do tempo de sonobarbitúrico, o pentobarbital sódico (PTB) 40 mg/kg, via i.p.,foi administrado trinta minutos após da solução de FTA 200mg/kg e os parâmetros observados neste teste foram: latênciae tempo de sono. Também foi avaliada a coordenação motorados animais tratados com FTA 200 mg/kg, no teste do rotarod,foram considerados aptos os animais que permaneceramna barra giratório por 180s. Resultados: Os resultadosobtidos por meio da triagem farmacológica demonstram queesta fração possui uma atividade no sistema nervoso centrale que possivelmente esta atividade é depressora. Otratamento com a FTA não interferiu na latência e nem notempo de sono induzido pelo PTB. A FTA não tem nenhumefeito miorrelaxante e não interfere na coordenação motorados animais submetidos ao rota-rod. Conclusão: AChondrodendron platyphyllum exerce um efeito no SNC...

To evaluate the activity of Chondrodendronplatyphyllum on CNS. Material and Methods: Were performedgeneral tests to assess the effect of the TAF on the CNS.The TAF in doses of 100, 200 and 400 mg / kg wasadministered to mice by intraperitoneal route and apharmacological screening trial was carried out, whichevaluated the behavioral change of the animals. In the test ofpotentiation of barbiturate sleeping time, sodium pentobarbital(PTB) 40 mg / kg, ip, was administered thirty minutes afterthe TAF solution of 200 mg / kg. The parameters observed inthis trial were: latency and sleep time. Were also evaluatedthe motor coordination of the animals treated with TAF 200mg / kg in the rota-rod test. The animals considered fit werethose which remained in the revolving bar for 180s. Results:The results obtained by pharmacological screening showedthat this fraction has an activity in the central nervous systemand possibly that this activity is depressing. The treatmentdid not interfere either with the TAF in latency or with the timeof sleep induced by PTB. The TAF has no myorelaxing effectand doesn’t interfere with motor coordination of the animalssubjected to rota-rod. Conclusion: Chondrodendronplatyphyllum exerts a depressant effect on CNS...

Ansiedade Patológica: Bases Neurais e Avanços na Abordagem Psicofarmacológica / Pathological Anxiety: Neural Bases and Advances in Psychopharmacological Approach

Apresentar uma visão atualizada e ampla da ansiedade emsua manifestação patológica, suas bases neurais e o avanço na suaabordagem terapêutica psicofarmacológica. Material e Métodos: Foirealizada uma revisão de literatura usando como fonte de pesquisaartigos indexados pela base de dados Pubmed, Medline e pesquisasem livros específicos que investigaram a ansiedade em seu aspectopatológico. Resultados: A literatura revelou que na gênese dostranstornos da ansiedade vários neurotransmissores são implicados,uma vez que eles participam, em maior ou menor grau, da modulaçãoe regulação dos comportamentos defensivos. As evidências obtidasaté então permitem constatar o progresso alcançado no tratamentodos transtornos da ansiedade com a utilização dos benzodiazepínicose, mais recentemente, com o uso de antidepressivos. Novasalternativas para o tratamento dos transtornos da ansiedade envolvempesquisas relacionadas à descoberta de novos antidepressivos, aouso de peptídeos neuroativos, como a colecistocinina (CCK), fatorde liberação de corticotropina (CRH), neuropetídeo Y, e antagonistasdo receptor glutamatérgico NMDA. Conclusão: Observa-se o progressoalcançado no tratamento farmacológico dos transtornos da ansiedadecom a utilização principalmente dos antidepressivos. Entretanto, umlongo caminho ainda haverá que ser trilhado em busca de novasopções terapêuticas para abordagem destes transtornos...

To present an updated and broad perspective of anxietyconcerning its pathological manifestation, neural bases and theprogress in its psychopharmacological therapeutic approach. Method:It was conduced a literature review whose source of research waspapers indexed by the database Pubmed, Medline and researchesfrom specific books that investigated the anxiety in its pathologicalaspect. Results: As regards the genesis of anxiety disorders, severalneurotransmitters are involved since they participate, in a greater orlesser degree, in the modulation and regulation of defensive behaviors.The evidence obtained so far allows noting the progress achieved inthe treatment of anxiety disorders with the use of benzodiazepinesand, more recently, antidepressants. New alternatives for the treatmentof the anxiety-related disorders involve researches related to thediscovery of new antidepressants, to the use of neuroactive peptidessuch as cholecystokinin (CCK), corticotropin releasing factor (CRH),neuropeptide Y, and antagonists of glutamatergic NMDA receptor.Conclusion: Advances can be observed in the pharmacologicaltreatment of anxiety disorders mainly by using antidepressants.However, there is still a long way to be followed in order to find newtherapeutic options for these disorders...

Absence of mutagenic effect of Mikania glomerata hydroalcoholic extract on adult wistar rats in vivo

This work makes an assessment of the dominant lethality of Mikania glomerata in male Wistar rats. Adult male received 1 mL of M. glomerata hydroalcoholic extract at a dose level of 3.3 g/kg body weight for 52 days and were mated with untreated females for seven weeks (group 1) or one week prior to the beginning of treatment and on the week following the end of treatment (group 2). The parameters analyzed were: number of implanted embryos, resorptions and corpora lutea; mating, gestation, preimplantation loss, implantation and resorption indexes (group 1); number of offspring and weaning animals (group 2). The administration of M. glomerata did not show any impairment of fertility and no significant difference in the parameters analyzed, suggesting an absence of mutagenic effect on Wistar rats.

Mikania glomerata é uma planta utilizada na medicina popular, cujas folhas possuem flavonóides e cumarina. Essas substâncias, segundo a literatura, interferem na fertilidade de cães e ratas, respectivamente. O presente trabalho faz um estudo do teste do letal dominante com M. glomerata em ratos Wistar. Animals adultos foram tratados com 1 mL de extrato hidroalcoólico de M. glomerata na dose de 3.3 g/kg de peso corporal durante 52 dias. Os animais foram acasalados com fêmeas não tratadas por sete semanas (grupo 1) ou uma semana antes do início do tratamento e na semana seguinte ao término do mesmo (grupo 2). As variáveis analisadas foram: números de embriões implantados, reabsorções e corpos lúteos, índices de acasalamento, gestação, perda pré-implantação, implantação e reabsorção (grupo 1); número de filhotes nascidos e de animais desmamados (grupo 2). A administração de M. glomerata não interferiu com a fertilidade dos animais e não foram observadas alterações significativas das variáveis analisadas, o que sugere a ausência de efeito mutagênico em ratos Wistar por parte dessa planta.

Avaliação do efeito de mikania glomerata sobre o sistema reprodutor e órgaõs de ratos wistar submetidos a tratamento subagudo / Short-term exposure to mikania glomerata on male wistar rats' organs and reproductive system

Mikania glomerata (guaco) is a plant well known in Brazil for its therapeutic properties, especially in the treatament of respiratory diseases. Coumarin and flavonoids are active compounds of M. glomerata leaves and have been reported to cause adverse effects on the organism, including antifertility activity in famale rat and male dog respectively. This work analyzes the effect of short-term administration of M.glomerata hydroalcoholic extract on vital organs, of the reproductive system and sperm concentration of mature male wistar rats. Treated animals received 1 ml of the extract at a dose of 1.1 g/kg of body weight for live days. Body and organs weights, sperm production and food consumption were evaluated. No body weigth reduction and no toxic effect on the organs, gamete production or food intake were detected in any of the groups analyzed, given the experimental protocol used.

Atividade depressora do sistema nervoso central da iangambina / Depressant activity of central nervous system of iangambina

Neste estudo, os autores relatam os dados da avaliaçao dos efeitos a nível do sistema nervoso central da iangambina, uma lignana furofurânica isolada da Ocotea duckei Vattimo. Os principais efeitos observados em camundongos, foram: potencializaçao do tempo de sono induzido por pentobarbital e bloqueio das convulsoes induzidas por pentilenotetrazol.

Levantamento bibliográfico da flora medicinal de uso no tratamento da diabetes e alguns resultados experimentais / Literature search of medicinal plants of use in diabetes treatment and some experimental results

O uso de plantas no tratamento da diabete tem sido intenso em anos recentes, por esta razäo existem várias plantas que säo encontradas em muitos países que säo mencionados como portadoras de açäo hipoglicemiante. Um vasto levantamento foi feito inclusive uma busca na literatura e no campo. Um total de 68 espécies vegetais foram listadas como sendo usadas no tratamento da diabetes. Algumas dessas plantas já foram submetidas a investigaçöes farmacológicas. Em um estágio subseqüente a coleta e a identificaçäo de quatro dessas plantas foi feita: Bauhinia forficata Link, Bumelia sartorum Mart., Caesalpinea ferrea Mart., e Licania rigida Benth, elas foram submetidas ao screening farmacológico para testar seus efeitos hipoglicemiantes aclamados pela medicina tradicional