RESUMO
Samanea tubulosa Benth. it has been widely used in traditional medicine to treat inflammatory processes. The present study aimed to investigate the antinociceptive effect and mechanism of action of the fractions obtained from the Samanea tubulosa pods in mice. The antinociceptive activity was evaluated in formalin, capsaicin and glutamate tests and the. The possible mechanisms of action involved in the antinociceptive effect of the hexane and ethyl acetate fraction in the opioid system, also the the K + ATP channels and the L-arigine pathways of nitric oxide were evaluated. The chemical characterization analysis revealed in the hexane fraction the presence of triterpenes such as lupenone and lupeol. In the glutamate test, the hexane and ethyl acetate fractions showed antinociceptive activity at the dose of 12.5 and 25 mg kg-1. The antinociception produced by the hexane and ethyl acetate fractions was significantly reversed by naloxone, indicating that the fractions act through the opioid pathway. Antinociceptive response of the ethyl acetate fraction was blocked by glibenclamide, indicating that this fraction acts via the K + ATP channels activation. It is concluded that the fractions under study exert antinociceptive activity possibly related to the opioid route and through K+ ATP channels activation.
Assuntos
Dor Aguda , Fabaceae , Dor Aguda/tratamento farmacológico , Trifosfato de Adenosina , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Analgésicos Opioides , Animais , Fabaceae/metabolismo , Ácido Glutâmico , Hexanos , CamundongosRESUMO
Reserva Ecológica de Guapiaçu (REGUA) is a private, protected area inside a remnant of the Atlantic Forest with high biodiversity. Although the bats of the reserve have been sampled for more than two decades, few studies have been published about them. Based on a compilation of data from several surveys, we present an updated list of the bat species there and compare it with surveys from other locations in the Atlantic Forest. From August 1998 to September 2021, at least 194 sampling nights were carried out at REGUA by different research groups from various institutions, totaling 448,092 m2.h of sampling. A total of 4,069 individuals were captured, belonging to 47 species and six families. Additionally, our results indicate that it is possible that some species that occur at REGUA have not been recorded yet. REGUA has the greatest number of bat species known for the Atlantic Forest. This most likely results from the fact that the reserve includes large areas of mature, continuous forest connected with other protected areas in the State of Rio de Janeiro. Another factor contributing to the high diversity of bat species at REGUA is that the area has been intensely sampled for many years. Given that the bat assemblage there appears to be a good proxy to ascertain the ecological patterns of biodiversity in well-preserved forests, we consider REGUA to be an important area for long-term ecological research. The basic knowledge about the ecological interactions of bats with different food resources and zoonotic microorganisms offers a unique opportunity to carry out research in several areas of knowledge, making it possible to address questions about bat assemblage structure, bat-parasite ecology, competition, niche partitioning, and other related studies.
Assuntos
Animais , Quirópteros/classificação , Biodiversidade , Brasil , FlorestasRESUMO
We analyzed the bat assemblages found in protected areas in the state of Rio de Janeiro, Brazil, which is the best-sampled region of the Atlantic Forest. We selected 24 strict nature reserves and nine sustainable-use protected areas. We used data from inventories and complemented with data from the literature. We compared strict and sustainable-use protected areas, and tested whether the bat assemblages varied between habitat types. We tested the effect of geographic distance on the dissimilarity between bat assemblages, as well as the relationship between species composition and the size, mean altitude of the protected area, and capture effort. We compiled a total of 34,443 capture records, involving 67 species. Three species were captured only once, which raises cause for concern. Bat assemblages did not vary between protected area categories, but did vary among habitats with less than 1,000 captures. Assemblages were more similar to one another in geographically proximate areas. The size of the protected area and capture effort did not affect the composition of the bat assemblages, but altitude did influence this parameter. The Atlantic Forest is a priority biome for research and conservation, and reliable data on species distributions are essential for the development of conservation strategies.
Analisamos as assembleias de morcegos encontradas em Unidades de Conservação (UCs) no estado do Rio de Janeiro, Brasil, que é a região melhor amostrada da Mata Atlântica. Selecionamos 24 UCs de Proteção Integral e nove de Uso Sustentável. Utilizamos dados de inventários e complementamos com dados da literatura. Comparamos as UCs de Proteção Integral e de Uso Sustentável e testamos se as assembleias de morcegos variavam entre os tipos de habitat. Testamos o efeito da distância geográfica na dissimilaridade entre as assembleias de morcegos, bem como a relação entre a composição das espécies e o tamanho, a altitude média das UCs e o esforço de captura. Compilamos um total de 34.443 registros de captura, de 67 espécies. Três espécies foram capturadas apenas uma vez, o que mostra motivos de preocupação. As assembleias de morcegos não variaram entre categorias das UCs, mas variaram entre habitats com menos de 1.000 capturas. As assembleias foram mais parecidas entre si em áreas geograficamente próximas. O tamanho da UC e o esforço de captura não afetaram a composição das assembleias de morcegos, mas a altitude influenciou esse parâmetro. A Mata Atlântica é um bioma prioritário para pesquisa e conservação, e dados confiáveis sobre a distribuição de espécies são essenciais para o desenvolvimento de estratégias de conservação.
Assuntos
Animais , Conservação dos Recursos Naturais , Ecossistema , Quirópteros/crescimento & desenvolvimentoRESUMO
ABSTRACT We analyzed the bat assemblages found in protected areas in the state of Rio de Janeiro, Brazil, which is the best-sampled region of the Atlantic Forest. We selected 24 strict nature reserves and nine sustainable-use protected areas. We used data from inventories and complemented with data from the literature. We compared strict and sustainable-use protected areas, and tested whether the bat assemblages varied between habitat types. We tested the effect of geographic distance on the dissimilarity between bat assemblages, as well as the relationship between species composition and the size, mean altitude of the protected area, and capture effort. We compiled a total of 34,443 capture records, involving 67 species. Three species were captured only once, which raises cause for concern. Bat assemblages did not vary between protected area categories, but did vary among habitats with less than 1,000 captures. Assemblages were more similar to one another in geographically proximate areas. The size of the protected area and capture effort did not affect the composition of the bat assemblages, but altitude did influence this parameter. The Atlantic Forest is a priority biome for research and conservation, and reliable data on species distributions are essential for the development of conservation strategies.
RESUMO Analisamos as assembleias de morcegos encontradas em Unidades de Conservação (UCs) no estado do Rio de Janeiro, Brasil, que é a região melhor amostrada da Mata Atlântica. Selecionamos 24 UCs de Proteção Integral e nove de Uso Sustentável. Utilizamos dados de inventários e complementamos com dados da literatura. Comparamos as UCs de Proteção Integral e de Uso Sustentável e testamos se as assembleias de morcegos variavam entre os tipos de habitat. Testamos o efeito da distância geográfica na dissimilaridade entre as assembleias de morcegos, bem como a relação entre a composição das espécies e o tamanho, a altitude média das UCs e o esforço de captura. Compilamos um total de 34.443 registros de captura, de 67 espécies. Três espécies foram capturadas apenas uma vez, o que mostra motivos de preocupação. As assembleias de morcegos não variaram entre categorias das UCs, mas variaram entre habitats com menos de 1.000 capturas. As assembleias foram mais parecidas entre si em áreas geograficamente próximas. O tamanho da UC e o esforço de captura não afetaram a composição das assembleias de morcegos, mas a altitude influenciou esse parâmetro. A Mata Atlântica é um bioma prioritário para pesquisa e conservação, e dados confiáveis sobre a distribuição de espécies são essenciais para o desenvolvimento de estratégias de conservação.
RESUMO
We analyzed the bat assemblages found in protected areas in the state of Rio de Janeiro, Brazil, which is the best-sampled region of the Atlantic Forest. We selected 24 strict nature reserves and nine sustainable-use protected areas. We used data from inventories and complemented with data from the literature. We compared strict and sustainable-use protected areas, and tested whether the bat assemblages varied between habitat types. We tested the effect of geographic distance on the dissimilarity between bat assemblages, as well as the relationship between species composition and the size, mean altitude of the protected area, and capture effort. We compiled a total of 34,443 capture records, involving 67 species. Three species were captured only once, which raises cause for concern. Bat assemblages did not vary between protected area categories, but did vary among habitats with less than 1,000 captures. Assemblages were more similar to one another in geographically proximate areas. The size of the protected area and capture effort did not affect the composition of the bat assemblages, but altitude did influence this parameter. The Atlantic Forest is a priority biome for research and conservation, and reliable data on species distributions are essential for the development of conservation strategies.(AU)
Analisamos as assembleias de morcegos encontradas em Unidades de Conservação (UCs) no estado do Rio de Janeiro, Brasil, que é a região melhor amostrada da Mata Atlântica. Selecionamos 24 UCs de Proteção Integral e nove de Uso Sustentável. Utilizamos dados de inventários e complementamos com dados da literatura. Comparamos as UCs de Proteção Integral e de Uso Sustentável e testamos se as assembleias de morcegos variavam entre os tipos de habitat. Testamos o efeito da distância geográfica na dissimilaridade entre as assembleias de morcegos, bem como a relação entre a composição das espécies e o tamanho, a altitude média das UCs e o esforço de captura. Compilamos um total de 34.443 registros de captura, de 67 espécies. Três espécies foram capturadas apenas uma vez, o que mostra motivos de preocupação. As assembleias de morcegos não variaram entre categorias das UCs, mas variaram entre habitats com menos de 1.000 capturas. As assembleias foram mais parecidas entre si em áreas geograficamente próximas. O tamanho da UC e o esforço de captura não afetaram a composição das assembleias de morcegos, mas a altitude influenciou esse parâmetro. A Mata Atlântica é um bioma prioritário para pesquisa e conservação, e dados confiáveis sobre a distribuição de espécies são essenciais para o desenvolvimento de estratégias de conservação.(AU)
Assuntos
Animais , Quirópteros/crescimento & desenvolvimento , Ecossistema , Conservação dos Recursos NaturaisRESUMO
The aim of this study was to reevaluate the ecology of an area in the Atlantic Forest, southeast Brazil, where Chagas disease (CD) has been found to occur. In a previous study, immediately after the occurrence of a CD case, we did not observe any sylvatic small mammals or dogs with Trypanosoma cruzi cruzi infections, but Triatoma vitticeps presented high T. c. cruzi infection rates. In this study, we investigated bats together with non-volant mammals, dogs, and triatomines to explore other possible T. c. cruzi reservoirs/hosts in the area. Seventy-three non-volant mammals and 186 bats were captured at three sites within the Guarapari municipality, Espírito Santo state. Rio da Prata and Amarelos sites exhibited greater richness in terms of non-volant mammals and bats species, respectively. The marsupial Metachirus nudicaudatus, the rodent Trinomys paratus, and the bats Artibeus lituratus and Carollia perspicillata were the most frequently captured species. As determined by positive hemocultures, only two non-volant mammals were found to be infected by Trypanosoma species: Monodelphis americana, which was infected by T. cascavelli, T. dionisii and Trypanosoma sp., and Callithrix geoffroyi, which was infected by T. minasense. Bats presented T. c. cruzi TcI and TcIII/V, T. c. marinkellei, T. dionisii, T. rangeli B and D, and Trypanosoma sp. infections. Seven dogs were infected with T. cruzi based only on serological exams. The triatomines T. vitticeps and Panstrongylus geniculatus were found to be infected by trypanosomes via microscopy. According to molecular characterization, T. vitticeps specimens were infected with T. c. cruzi TcI, TcII, TcIII/V, and TcIV, T. c. marinkellei and T. dionisii. We observed high trypanosome diversity in a small and fragmented region of the Atlantic Forest. This diversity was primarily maintained by bats and T. vitticeps. Our findings show that the host specificity of the Trypanosoma genus should be thoroughly reviewed. In addition, our data show that CD cases can occur without an enzootic cycle near residential areas.
Assuntos
Biodiversidade , Quirópteros/parasitologia , Triatoma/parasitologia , Trypanosoma/fisiologia , Animais , Sequência de Bases , Brasil/epidemiologia , Cães , Geografia , Sequenciamento de Nucleotídeos em Larga Escala , Intestinos/parasitologia , Filogenia , RNA Ribossômico/genética , Floresta Úmida , Especificidade da Espécie , Tripanossomíase/epidemiologiaRESUMO
Introduction: Endoscopic submucosal dissection (ESD) is an already established procedure in the treatment of gastric and esophageal cancer in its early stages. Colorectal lesions, initially approached by endoscopic mucosal resection en bloc or in fragments, are the current focus for submucosal approach, especially for superficial lateral spreading tumor of 20 mm-diameter. The experience of Japanese centers, which are reference in therapeutic endoscopy, demonstrates reduction in the rate of disease recurrence with this approach and, according to specific histopathological criteria, may avoid colectomy in some cases of malignant neoplasia. Case report: The patient was 50-year-old female. She underwent endoscopic submucosal dissection of a rectal lateral spreading tumor measuring 50 mm, located 8 cm from the anal margin. The procedure was performed without major complications, with just two points for muscle layer detachment, without gross perforation and closed with metal clips. However, the patient developed air leakage to the peritoneum, retroperitoneum, mediastinum and subcutaneous tissue, being only treated with clinical procedures and without additional intervention. Conclusion: It is vital to know and be able to apply the technique of ESD, in addition to addressing its complications, since despite the numerous benefits compared to surgery, ESD can result in serious outcomes. (AU)
Introdução: A dissecção endoscópica da submucosa (ESD) já é procedimento consagrado no tratamento do câncer gástrico e esofagiano em suas fases precoces. As lesões colorre-tais, inicialmente abordadas por mucossectomia, em bloco ou em fragmentos, são o foco atual para a abordagem submucosa, principalmente para os tumores de crescimento lateral superficial a partir de 20 mm de diâmetro. A experiência de centros japoneses, referências em endoscopia terapêutica, demonstram redução no índice de recidiva da doença com esta abordagem e, segundo critérios histopatológicos específicos, podem evitar uma colectomia em alguns casos de neoplasia maligna. Relato de caso: Trata-se de paciente de 50 anos, submetida à dissecção endoscópica da submucosa de lesão de crescimento lateral, com 50 mm, localizada no reto, a 8 cm da margem anal. O procedimento foi realizado sem maiores intercorrências, com apenas dois pontos de afastamento da muscular, sem perfuração grosseira, fechados com clipe. Entretanto, a paciente evoluiu com escape aéreo para peritônio, retroperitônio, mediastino e subcútis, sendo tratada sem intervenção adicional, apenas com manejo clínico. Conclusão: É de fundamental importância conhecer e saber aplicar a técnica da ESD, além de abordar suas complicações, uma vez que, mesmo repleta de benefícios em relação à cirurgia, ela pode apresentar desfechos graves. (AU)
Assuntos
Humanos , Feminino , Pessoa de Meia-Idade , Retropneumoperitônio/diagnóstico , Enfisema Subcutâneo/diagnóstico , Ressecção Endoscópica de Mucosa/efeitos adversos , Enfisema Mediastínico/diagnóstico , ColonoscopiaRESUMO
This study aimed to study the in vitro antioxidant activity and cytotoxicity on tumor cells lines of six synthetic substances derived from riparins. All the substances showed antioxidant activity and riparins C, D, E, F presented cell growth inhibition rates greater than 70%, suggesting that these molecules have antitumor properties. These substances also caused greater than 80% releases of cytoplasmic lactate dehydrogenase enzyme (LDH). Although the antioxidant and antitumor properties presented herein require further assessment, the outcomes indicate that these novel riparins are promising biologically active compounds.
Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Benzamidas/farmacologia , Malondialdeído/antagonistas & inibidores , Óxido Nítrico/antagonistas & inibidores , Animais , Antioxidantes/síntese química , Benzamidas/síntese química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Óxido Nítrico/biossínteseRESUMO
Some bat species are able to adapt to urban areas, where they find food and roosts. Despite the high number of parks in Brazilian cities, they did not yet raise the interest of most zoologists, except for some surveys of birds and butterflies. The objectives of the present study were: (i) to inventory the bat species of Quinta da Boa Vista (QBV), a large (25 ha) urban park centrally located in densely populated Rio de Janeiro, which is Brazil's second largest metropolis; (ii) to compare the species richness observed in roosts with the richness recorded through mist netting in flight routes and near fruiting fig trees; and (iii) to analyze recaptures of bats marked in this park and recaptured in other sites and vice-versa. Sampling totaled 104 sampling nights resulting in 3,256 captures (including 133 recaptures) between April 1989 and December 2004. We also sampled roosts and received some specimens from park visitors and city workers. We documented 21 bat species, predominantly large frugivores. The number of expected species for this park was 24.0 ± 4.6, and the total sampled represented 87.5% of the expected. The recapture of bats marked in surrounding forest fragments and in QBV shows the importance of urban parks for the maintenance of bat diversity. Inspection of roosts produced two species that had not been captured with other methods. Sampling near fruiting fig trees did not differ in terms of richness from sampling carried out far from these trees or during their non-fruiting periods.
Algumas espécies de morcegos são capazes de se adaptar às áreas urbanas, onde encontram alimento e abrigo. Apesar do elevado número de parques nas cidades brasileiras estas ainda não despertaram o interesse dos zoólogos, exceção feita a inventários de aves e borboletas. Os objetivos do presente estudo foram: (i) inventariar as espécies de morcegos da Quinta da Boa Vista (QBV), um grande (25 ha) parque urbano centralmente localizado na povoada cidade do Rio de Janeiro, a segunda maior metrópole do Brasil; (ii) comparar a riqueza de espécies observadas em refúgios com a riqueza registrada através de redes de neblina abertas em rotas de voo e perto de figueiras em frutificação; e (iii) analisar as recapturas de morcegos marcados neste parque e recapturados em outras localidades, e vice-versa. A amostragem totalizou 104 noites, resultando em 3.256 capturas (incluindo 133 recapturas) entre abril de 1989 e dezembro de 2004. Nós também amostramos abrigos e recebemos alguns exemplares de visitantes do parque e dos cidadãos. No total, nós documentamos 21 espécies de morcegos, com a predominância de grandes frugívoros. O número de espécies esperadas para este parque foi de 24,0 ± 4,6, e o total amostrado representado foi de 87,5% do esperado. As recapturas de morcegos marcados em torno dos fragmentos florestais e em QBV mostram a importância de parques urbanos para a manutenção da diversidade de morcegos. As buscas e amostragens em abrigos resultaram em duas espécies que não tinham sido capturadas com outros métodos. As amostragens perto de figueiras em frutificação não diferiram em termos de riqueza em relação às amostragens realizadas longe destas árvores, ou durante os seus períodos de não frutificação.
Assuntos
Animais , Biodiversidade , Parques Recreativos , Quirópteros , Área Urbana , Estudos de Amostragem , BrasilRESUMO
Some bat species are able to adapt to urban areas, where they find food and roosts. Despite the high number of parks in Brazilian cities, they did not yet raise the interest of most zoologists, except for some surveys of birds and butterflies. The objectives of the present study were: (i) to inventory the bat species of Quinta da Boa Vista (QBV), a large (25 ha) urban park centrally located in densely populated Rio de Janeiro, which is Brazil's second largest metropolis; (ii) to compare the species richness observed in roosts with the richness recorded through mist netting in flight routes and near fruiting fig trees; and (iii) to analyze recaptures of bats marked in this park and recaptured in other sites and vice-versa. Sampling totaled 104 sampling nights resulting in 3,256 captures (including 133 recaptures) between April 1989 and December 2004. We also sampled roosts and received some specimens from park visitors and city workers. We documented 21 bat species, predominantly large frugivores. The number of expected species for this park was 24.0 ± 4.6, and the total sampled represented 87.5% of the expected. The recapture of bats marked in surrounding forest fragments and in QBV shows the importance of urban parks for the maintenance of bat diversity. Inspection of roosts produced two species that had not been captured with other methods. Sampling near fruiting fig trees did not differ in terms of richness from sampling carried out far from these trees or during their non-fruiting periods.(AU)
Algumas espécies de morcegos são capazes de se adaptar às áreas urbanas, onde encontram alimento e abrigo. Apesar do elevado número de parques nas cidades brasileiras estas ainda não despertaram o interesse dos zoólogos, exceção feita a inventários de aves e borboletas. Os objetivos do presente estudo foram: (i) inventariar as espécies de morcegos da Quinta da Boa Vista (QBV), um grande (25 ha) parque urbano centralmente localizado na povoada cidade do Rio de Janeiro, a segunda maior metrópole do Brasil; (ii) comparar a riqueza de espécies observadas em refúgios com a riqueza registrada através de redes de neblina abertas em rotas de voo e perto de figueiras em frutificação; e (iii) analisar as recapturas de morcegos marcados neste parque e recapturados em outras localidades, e vice-versa. A amostragem totalizou 104 noites, resultando em 3.256 capturas (incluindo 133 recapturas) entre abril de 1989 e dezembro de 2004. Nós também amostramos abrigos e recebemos alguns exemplares de visitantes do parque e dos cidadãos. No total, nós documentamos 21 espécies de morcegos, com a predominância de grandes frugívoros. O número de espécies esperadas para este parque foi de 24,0 ± 4,6, e o total amostrado representado foi de 87,5% do esperado. As recapturas de morcegos marcados em torno dos fragmentos florestais e em QBV mostram a importância de parques urbanos para a manutenção da diversidade de morcegos. As buscas e amostragens em abrigos resultaram em duas espécies que não tinham sido capturadas com outros métodos. As amostragens perto de figueiras em frutificação não diferiram em termos de riqueza em relação às amostragens realizadas longe destas árvores, ou durante os seus períodos de não frutificação.(AU)
Assuntos
Animais , Quirópteros , Parques Recreativos , Biodiversidade , Área Urbana , Brasil , Estudos de AmostragemRESUMO
OBJECTIVE: Evaluate the type and incidence of postoperative complications after surgery for deep infiltrative endometriosis at Biocor Hospital. METHODS: Our observational study involved a multidisciplinary surgical team that performed laparoscopy on 154 patients suffering from pelvic pain. Surgical complications occurring up to the 30th postoperative day were recorded. RESULTS: Mean age patient age was 34.1 years. Infertility was present in 69 (45%) although 31% had not attempted to get pregnant. Dysmenorrhea was the most frequent symptom (79.3%) followed by chronic pelvic pain (59.7%) and deep dyspareunia (48,7%). Most cases required extensive surgery as the majority (n=117; 76.9%) were classified as severe endometriosis (ASRM grade IV). The most frequent surgical procedures were: 136 adhesiolysis, 100 intestinal surgeries (85 retosigmoidectomies), 92 peritonal lesion excision, 39 vaginal resections, 19 myomectomies, 21 hysterectomies and 5 partial bladder resections. Postoperative complications were recorded in 14 (9.59%) patients: 8 (5.48%) major complications and 6 (4.11%) minor. Major complications included blood transfusion (n=2) retosigmoid anastomosis dehiscence (1), rectovaginal fistula (n=1), urinary fistula (n=1), deep vein thrombosis (n=1), lower limb compartment syndrome with motor deficit (n=1) and one intestinal obstruction (n=1). Minor complications were abdominal wall infection (n=3), peripheral neuropathy (n=3), bladder atony (n=1) and bladder perforation (n=1). No deaths were observed. All major complication cases underwent retosigmoidectomy associated with vaginal resection (n=6), uterosacral ligament excision (n=5) or hysterectomy (n=3). CONCLUSION: The surgical treatment of DIE is complex and subject to complications. The surgical expertise of a multidisciplinary team plays a vital role in this setting.
RESUMO
This study describes the isolation and identification of apigenin-7-O-ghicopyranoside, a flavonoid isolated from the flowers of Bellis perennis L., Asteraceae, an species with a broad spectrum of biological activities. The in vitro antioxidant activity and the inhibition of the enzyme acetylcholinesterase were evaluated. The flavonoid showed strong in vitro antioxidant potential, because of the capacity of removal of hydroxyl radicals and nitric oxide, and also prevented the formation of thiobarbituric acid-reactive substances. These parameters were inhibited at the highest concentration of ApG at rates of 77.7%, 72% and 73.4%, respectively, in addition to inhibiting acetylcholinesterase, suggesting potential use in the treatment of neurodegenerative diseases.
Assuntos
Antioxidantes/farmacologia , Asteraceae/química , Inibidores da Colinesterase/farmacologia , Flores/química , Extratos Vegetais/farmacologia , Acetilcolinesterase/efeitos dos fármacos , Asteraceae/classificação , Peroxidação de Lipídeos/efeitos dos fármacos , Extratos Vegetais/isolamento & purificaçãoRESUMO
The present study was conducted to evaluate the toxicity of the ethanolic extract of leaves of Parkia platycephala Benth., Fabaceae, on systemic and reproductive parameters. In toxicity on the estrous cycle, four groups of not-pregnant Wistar rats received distilled water and the doses 250, 500 and 1000 mg.kg-1 of plant extract for thirty days, at the end of which they were examined as to the frequency of their phases. The systemic toxicity was assessed through the consumption of water and food and by measuring body mass. After the extract was administered, serum AST, ALT, ALP, bilirubin (total, direct and indirect), urea and creatinine were dosed. The evaluation of the organs (brain, heart, hypophysis, adrenal glands, liver, spleen, uterus and ovaries) in their macroscopic aspects, relative and absolute masses and histological structure showed that the plant extract induced a decrease of water and food consumption and of body mass. It caused an increase in the luteal phase and a decrease in the follicular phase of the estrous cycle and rose serum alkaline phosphatase levels.The data exhibit systemic and reproductive toxicity induced by plant extract in female Wistar rats.
RESUMO
This study describes the isolation and identification of apigenin-7-O-ghicopyranoside, a flavonoid isolated from the flowers of Bellis perennis L., Asteraceae, an species with a broad spectrum of biological activities. The in vitro antioxidant activity and the inhibition of the enzyme acetylcholinesterase were evaluated. The flavonoid showed strong in vitro antioxidant potential, because of the capacity of removal of hydroxyl radicals and nitric oxide, and also prevented the formation of thiobarbituric acid-reactive substances. These parameters were inhibited at the highest concentration of ApG at rates of 77.7%, 72% and 73.4%, respectively, in addition to inhibiting acetylcholinesterase, suggesting potential use in the treatment of neurodegenerative diseases.
Assuntos
Antioxidantes/farmacologia , Asteraceae/química , Inibidores da Colinesterase/farmacologia , Flores/química , Extratos Vegetais/farmacologia , Acetilcolinesterase/efeitos dos fármacos , Asteraceae/classificação , Peroxidação de Lipídeos/efeitos dos fármacos , Extratos Vegetais/isolamento & purificaçãoRESUMO
We describe herein the discovery of (E)-N-methyl-N'-((5-nitrofuran-2-yl)methylene)benzo[d]( 1 , 3 ) dioxole-5-carbohydrazide (9e), named LASSBio-1215, as a novel antiplatelet agent belonging to the N-methyl-N-acylhydrazone class, which exert their antiaggregating actions on human and rabbit platelets induced by different agonists, through cyclooxygenase-1 (COX-1) or thromboxane synthase inhibition. This compound was elected after screening of a series of functionalized furyl N-acylhydrazone derivatives, synthesized from natural safrole 10. In vitro assays showed that compound 9e presents platelet-aggregating activity in rabbit platelet-rich plasma (PRP) induced by arachidonic acid (IC(50) = 0.7 µM) and collagen (IC(50) = 4.5 µM). Moreover, LASSBio-1215 also inhibited almost completely the second wave of adenosine diphosphate-induced platelet aggregation in human PRP, and this effect was correlated with their ability to block the production of pro-aggregating autacoid thromboxane A(2).
Assuntos
Benzodioxóis/farmacologia , Produtos Biológicos/farmacologia , Hidrazinas/farmacologia , Inibidores da Agregação Plaquetária/farmacologia , Safrol/química , Animais , Benzodioxóis/síntese química , Benzodioxóis/química , Produtos Biológicos/síntese química , Produtos Biológicos/química , Plaquetas/efeitos dos fármacos , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Humanos , Hidrazinas/síntese química , Hidrazinas/química , Estrutura Molecular , Agregação Plaquetária/efeitos dos fármacos , Inibidores da Agregação Plaquetária/síntese química , Inibidores da Agregação Plaquetária/química , Coelhos , Valores de ReferênciaRESUMO
In this work, we reported the synthesis and evaluation of the analgesic, antiinflammatory, and antiplatelet properties of new phenothiazine-attached acylhydrazone derivatives (6), designed exploring the molecular hybridization approach between antipsychotic chlorpromazine (4) and other heterocyclic derivatives (3) and (5) developed at LASSBio. Target compounds were synthesized in very good yields exploiting diphenylamine (7) as starting material, through regioselective functionalization of the C-1 position of 10H-phenothiazine ring. The evaluation of platelet antiaggregating profile lead us to identify a new potent prototype of antiplatelet derivative, that is (6a) (IC(50)=2.3 microM), which acts in arachidonic acid pathway probably by inhibition of platelet COX-1 enzyme. Additionally, the change of para-substituent group of acylhydrazone framework permitted us to identify hydrophilic carboxylate derivative (6g) and hydrophobic bromo derivative (6b) as two new leads of analgesics more active than dipyrone used as standard and with selective peripheral or central mechanism of action.