RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Plant vernacular names can provide clues about the popular use of a species in different regions and are valuable sources of information about the culture or vocabulary of a population. Several medicinal plants in Brazil have received names of medicines and brand-name products. AIM OF THE STUDY: The present work aimed to evaluate the chemical composition and pharmacological activity in the central nervous system of three species known popularly by brand names of analgesic, anti-inflammatory, antispasmodic, and digestive drugs. MATERIALS AND METHODS: Hydroethanolic extracts of Alternanthera dentata (AD), Ocimum carnosum (OC), and Plectranthus barbatus (PB) aerial parts were submitted to phytochemical analysis by HPLC-PAD-ESI-MS/MS and evaluated in animal models at doses of 500 and 1000 mg/kg. Mice were tested on hot plate, acetic acid-induced writing, formalin-induced licking, and intestinal transit tests. Aspirin and morphine were employed as standard drugs. RESULTS: The three extracts did not change the mice's response on the hot plate. Hydroethanolic extracts of AD and PB reduced the number of writhes and licking time, while OC was only effective on the licking test at dose of 1000 mg/kg. In addition, AD and OC reduced intestinal transit, while PB increased gut motility. CONCLUSIONS: Pharmacological tests supported some popular uses, suggesting peripheral antinociceptive and anti-inflammatory effects, while the phytochemical analysis showed the presence of several flavonoids in the three hydroethanolic extracts and steroids in PB, with some barbatusterol derivatives described for the first time in the species.
Assuntos
Amaranthaceae , Analgésicos , Anti-Inflamatórios , Parassimpatolíticos , Compostos Fitoquímicos , Componentes Aéreos da Planta , Extratos Vegetais , Plectranthus , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Analgésicos/farmacologia , Analgésicos/química , Camundongos , Parassimpatolíticos/farmacologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Masculino , Amaranthaceae/química , Plectranthus/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Dor/tratamento farmacológico , Ocimum/química , Espectrometria de Massas em Tandem , Brasil , Trânsito Gastrointestinal/efeitos dos fármacosRESUMO
BACKGROUND: There are over 500 species in the Passiflora genus, and while some of them are very well known in folk medicine for their anxiolytic effects, very little is known for the other genus representants, which could also present medicinal effects. OBJECTIVE: In this study, we performed an interspecific pharmacological comparison of five investigated Passiflora species, all native to Brazil, namely P. bahiensis, P. coccinea, P. quadrangularis, P. sidaefolia, and P. vitifolia. METHODS: Extracts were administered to mice before behavioral testing, including a general pharmacological screening and anxiolytic-like effect investigation. RESULTS: Three of the species (P. coccinea, P. quadrangularis, and P. sidaefolia) induced a decrease in locomotor activity of mice; P. coccinea also reduced the latency to sleep. Importantly, none of the species interfered with motor coordination. Oral administration evoked no severe signs of toxicity, even at higher doses. Regarding the anxiolytic-like profile, P. sidaefolia reduced the anxious-like behavior in the Holeboard test in a similar way to the positive control, Passiflora incarnata, while not affecting total motricity. CONCLUSION: These results indicated that P. coccinea, P. quadrangularis, and P. sidaefolia reduced the general activity of mice and conferred a calmative/sedative potential to these three species, which must be further elucidated by future investigations.
Assuntos
Ansiolíticos , Passiflora , Ansiolíticos/farmacologia , Ansiolíticos/uso terapêutico , Ansiedade/tratamento farmacológico , Hipnóticos e Sedativos/farmacologia , Hipnóticos e Sedativos/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêuticoRESUMO
ABSTRACT Ayahuasca is a beverage with psychoactive properties used in religious and ceremonial rituals by some religious groups. The main active components of ayahuasca are dimethyltryptamine and the harmala alkaloids with ß-carboline structure acting as monoamine oxidase A inhibitors. This combination produces a pronounced activation of serotonergic pathways and presents potential interaction with other psychotropics. The objective of this study was to investigate the possible interactions between ayahuasca and agents employed in general anesthesia. The pharmacological interactions between ayahuasca and morphine or propofol were evaluated in mice using doses of 12, 120 and 1200 mg/kg (0.1 to 10 times the average dose consumed by humans in religious rituals). Ayahuasca alone showed an antinociceptive effect in the writhing and formalin tests, and intensified the analgesic effect of morphine in the hot plate test. Concerning the pharmacological interactions between ayahuasca and propofol, the results were opposite; ayahuasca intensified the depressant effect of propofol in the rotarod test, but decreased the sleeping time induced by propofol. These set of results showed the occurrence of some interactions between ayahuasca and the drugs morphine and propofol, possibly by both pharmacokinetics and pharmacodynamics mechanisms
Assuntos
Animais , Masculino , Camundongos , Interações Medicamentosas , Avaliação Pré-Clínica de Medicamentos , Morfina/análise , Bebidas/efeitos adversos , Propofol/análise , Banisteriopsis/efeitos adversos , Psychotria/efeitos adversos , Analgésicos/efeitos adversosRESUMO
OBJECTIVE: To evaluate the phytochemical composition of hydroethanolic extracts from powdered aerial parts of Turnera diffusa Willd (Turneraceae; T. diffusa), as well as its toxicity in astrocytes. METHODS: Chemical analyses of hydroethanolic extract from powdered aerial parts ofT. diffusa were carried out using HPLC-DAD-ESI-MS/MS.In vitro assays using astrocytes culture were performed to evaluate cell death. RESULTS: Flavone-C, O-diglycosides, such as, luteolin-8-C-[6-deoxy-2-O-rhamnosyl]-xylo-hexos-3-uloside, apigenin-8-C-[6-deoxy-2-O-rhamnosyl]-xylo-hexos-3-uloside and apigenin-7-O-6"-p-coumaroylglucoside were the main compounds found in this hydroethanolic extract. Concentration time-effect demonstrated the toxicity of this extract at a concentration of 1,000µg/mL in astrocyte culture, after 6 and 24 hours of incubation. CONCLUSION: In phytochemical analyses, important antioxidants (mainly flavonoids) were observed. T. diffusa extracts presented cytotoxic effect in high concentrations, leading to increased cell death in astrocyte culture.
Assuntos
Antioxidantes/química , Astrócitos/efeitos dos fármacos , Extratos Vegetais/química , Turnera/química , Animais , Astrócitos/química , Morte Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão/métodos , Flavonas/análise , Flavonas/toxicidade , Extratos Vegetais/toxicidade , Ratos , Espectrometria de Massas por Ionização por Electrospray/métodosRESUMO
ABSTRACT Objective To evaluate the phytochemical composition of hydroethanolic extracts from powdered aerial parts of Turnera diffusa Willd (Turneraceae; T. diffusa), as well as its toxicity in astrocytes. Methods Chemical analyses of hydroethanolic extract from powdered aerial parts ofT. diffusa were carried out using HPLC-DAD-ESI-MS/MS.In vitro assays using astrocytes culture were performed to evaluate cell death. Results Flavone-C, O-diglycosides, such as, luteolin-8-C-[6-deoxy-2-O-rhamnosyl]-xylo-hexos-3-uloside, apigenin-8-C-[6-deoxy-2-O-rhamnosyl]-xylo-hexos-3-uloside and apigenin-7-O-6”-p-coumaroylglucoside were the main compounds found in this hydroethanolic extract. Concentration time-effect demonstrated the toxicity of this extract at a concentration of 1,000µg/mL in astrocyte culture, after 6 and 24 hours of incubation. Conclusion In phytochemical analyses, important antioxidants (mainly flavonoids) were observed. T. diffusa extracts presented cytotoxic effect in high concentrations, leading to increased cell death in astrocyte culture.
RESUMO Objetivo Avaliar a composição fitoquímica do extrato hidroetanólico das partes aéreas de Turnera diffusa Willd (Turneraceae; T. diffusa) e sua toxicidade em astrócitos. Métodos Análises químicas do extrato hidroetanólico de partes aéreas de T. diffusa foram feitas por HPLC-DAD-ESI-MS/MS. Os ensaiosin vitro utilizaram culturas de astrócitos para avaliar morte celular. Resultados Flavonas-C, O-diglicosídeos, como, luteolina-8-C-[6-deoxi-2-O-raminosil]-xilo-hexos-3-ulosideo, apigenina-8-C-[6-deoxi-2-O-raminosil]-xilo-hexos-3-ulosideo e apigenina-7-O-6”-p-cumaroilglucosídeo foram os principais constituintes encontrados neste extrato hidroetanólico. Uma curva tempo-concentração demonstrou toxicidade desse extrato na concentração de 1.000µg/mL, na cultura de astrócitos após 6 e 24 horas de incubação. Conclusão Nas análises fitoquímicas, importantes antioxidantes, sobretudo flavonoides, foram observados. Extratos de T. diffusa apresentaram efeitos citotóxicos em altas concentrações, ocasionando aumento de morte celular em cultura de astrócitos.
Assuntos
Animais , Ratos , Extratos Vegetais/química , Astrócitos/efeitos dos fármacos , Turnera/química , Antioxidantes/química , Extratos Vegetais/toxicidade , Astrócitos/química , Cromatografia Líquida de Alta Pressão/métodos , Morte Celular/efeitos dos fármacos , Espectrometria de Massas por Ionização por Electrospray/métodos , Flavonas/análise , Flavonas/toxicidadeRESUMO
Multiple sclerosis is an inflammatory disease of the central nervous system. Chronic pain is one of the main symptoms, affecting many patients. Studies show that the lignans or the apolar extracts of Phyllanthus amarus have antinociceptive effects in different animal models. To evaluate the antihypernociceptive effect of a hexanic extract of P. amarus in experimental autoimmune encephalomyelitis in mice, the chemical composition of the hexanic extract was analyzed by gas chromatography mass spectrometry. After EAE induction, animals were treated with the hexanic extract of P. amarus for 26 consecutive days. Motor coordination and mechanical hypernociception were evaluated on alternate days. The principal lignans found were phyllanthin, niranthin, and 5-demethoxyniranthin. The hexanic extract of P. amarus at a dose of 100, 200, or 400 mg/kg did not affect the development of the disease. The motor coordination and pain threshold of the treated animals were not altered in this experiment. In conclusion, in this test, the hexanic extract of P. amarus did not show evidence of antihypernociceptive activity in experimental autoimmune encephalomyelitis.
Assuntos
Anisóis/farmacologia , Dioxóis/farmacologia , Encefalomielite Autoimune Experimental , Hiperalgesia , Lignanas/farmacologia , Esclerose Múltipla/complicações , Phyllanthus/química , Extratos Vegetais/farmacologia , Animais , Anisóis/análise , Anisóis/uso terapêutico , Dioxóis/análise , Dioxóis/uso terapêutico , Encefalomielite Autoimune Experimental/tratamento farmacológico , Feminino , Hiperalgesia/tratamento farmacológico , Hiperalgesia/etiologia , Lignanas/análise , Lignanas/uso terapêutico , Camundongos , Camundongos Endogâmicos C57BL , Esclerose Múltipla/tratamento farmacológico , Extratos Vegetais/química , Extratos Vegetais/uso terapêuticoRESUMO
OBJECTIVE: To verify if the medicinal plants Panax ginseng C.A. Mey, Turnera diffusa Willd. ex Schult., and Heteropterys tomentosa O. Mach., which are amply used by the population as tonics and cognition enhancers, could have a protective effect on cell death by apoptosis, since this could be one of the mechanisms of action of these substances. METHODS: Aged male Wistar rats (n = 24) were divided into four groups. Over 30 days, three groups received treatments with hydroalcoholic extracts of the plants, and one group received saline solution. A fifth group with young adult male Wistar rats (n = 4) received saline solution during the same period. Using the TUNEL technique, the percentage of apoptosis in the hippocampus of these animals was evaluated. RESULTS: No differences were observed between the percentage of apoptotic cells in the hippocampus of aged animals and of young control animals. The percentage of apoptosis in the hippocampus of aged animals treated chronically with the extracts from the three plants also did not differ from the percentage of apoptosis in the hippocampus of the control group of aged animals. CONCLUSION: Treatment with the hydroalcoholic extracts of Panax ginseng, Turnera diffusa, and Heteropterys tomentosa did not influence the apoptosis of the hippocampal cells of aged rats.
Assuntos
Apoptose/efeitos dos fármacos , Hipocampo/efeitos dos fármacos , Malpighiaceae/química , Panax/química , Extratos Vegetais/farmacologia , Turnera/química , Animais , Hipocampo/citologia , Masculino , Ratos , Ratos WistarRESUMO
OBJECTIVE: To verify if the medicinal plants Panax ginseng C.A. Mey, Turnera diffusa Willd. ex Schult., and Heteropterys tomentosa O. Mach., which are amply used by the population as tonics and cognition enhancers, could have a protective effect on cell death by apoptosis, since this could be one of the mechanisms of action of these substances. METHODS: Aged male Wistar rats (n=24) were divided into four groups. Over 30 days, three groups received treatments with hydroalcoholic extracts of the plants, and one group received saline solution. A fifth group with young adult male Wistar rats (n=4) received saline solution during the same period. Using the TUNEL technique, the percentage of apoptosis in the hippocampus of these animals was evaluated. RESULTS: No differences were observed between the percentage of apoptotic cells in the hippocampus of aged animals and of young control animals. The percentage of apoptosis in the hippocampus of aged animals treated chronically with the extracts from the three plants also did not differ from the percentage of apoptosis in the hippocampus of the control group of aged animals. CONCLUSION: Treatment with the hydroalcoholic extracts of Panax ginseng, Turnera diffusa, and Heteropterys tomentosa did not influence the apoptosis of the hippocampal cells of aged rats.
OBJETIVO: Plantas medicinais, como Panax ginseng C.A. Mey, Turnera diffusa Willd. Ex Schult. e Heteropterys tomentosa O. Mach. são amplamente utilizadas pela população como tônicas e para melhora da cognição. O presente estudo verificou se essas plantas poderiam ter algum efeito protetor na morte celular por apoptose, podendo este ser um dos mecanismos de ação dessas substâncias. MÉTODOS: Ratos machos Wistar idosos (n=24) foram divididos em quatro grupos. Durante 30 dias, três grupos receberam tratamento com extratos hidroalcoólicos das plantas e um grupo recebeu solução salina. Um quinto grupo com ratos machos Wistar adultos jovens (n=4) recebeu solução salina durante o mesmo período. Utilizando-se a técnica de TUNEL, avaliou-se a porcentagem de apoptose no hipocampo desses animais. RESULTADOS: Não foram observadas diferenças entre a porcentagem de células apoptóticas no hipocampo de animais idosos e de animais jovens controles. A porcentagem de apoptose no hipocampo dos animais idosos tratados cronicamente com os extratos das três plantas também não diferiu da porcentagem de apoptose do hipocampo dos animais idosos do grupo controle. CONCLUSÃO: O tratamento com os extratos hidroalcoólicos de Panax ginseng, Turnera diffusa e Heteropterys tomentosa não influenciou a apoptose das células hipocampais de ratos idosos.
Assuntos
Humanos , Idoso , Envelhecimento , Apoptose , Hipocampo , Plantas MedicinaisRESUMO
The present study aimed to assess the preclinical toxicity of two plants commonly used to treat "stomach ailments" in Brazil: Schinus terebinthifolius Raddi (S) and Myracrodruon urundeuva Allemão (M). In male rats, chronic treatment (83 days) with both pepper trees (17.6 and 13.8 mg/kg, S and M, respectively) has been shown to decrease hematocrit. However, a reduction in the number of red blood cells and hemoglobin was only seen following administration of S. terebinthifolius. None of the plants caused anatomopathological alterations following chronic treatment, and mating ability and fertility were not affected. Both pepper trees showed moderate toxicity following acute and chronic treatment by gavage, particularly S. terebinthifolius. Moreover, bone malformations were induced in fetuses, and a slight delay in recovery time of the postural reflex was observed in pups from female animals treated (18 days) with S. terebinthifolius. Given these results, a better assessment of the risks and benefits of the internal use of these plants is necessary, especially when used by women of childbearing age.
Assuntos
Anacardiaceae/toxicidade , Extratos Vegetais/toxicidade , Animais , Brasil , Eritrócitos/efeitos dos fármacos , Feminino , Fertilidade/efeitos dos fármacos , Feto/efeitos dos fármacos , Hematócrito , Hemoglobinas/análise , Masculino , Exposição Materna , Camundongos , Osteogênese/efeitos dos fármacos , Gravidez , Ratos , Testes de Toxicidade Subcrônica , Árvores/toxicidade , Aumento de PesoRESUMO
A study was conducted on 22,158 special B prescriptions (notificações B) containing amphetamine-type anorectic drugs or benzodiazepines, obtained from compounding pharmacies or drugstores located in the city of Natal, RN, Brazil. The data obtained were compared with those from other Brazilian cities. Results showed that compounding pharmacies dispensed 85.4 percent of the prescriptions, indicating that these pharmacies filled out nearly 10 times more of these prescriptions than did the drugstores. The majority (83.5 percent) of B prescriptions issued for the compounding pharmacies were for women, where the female/male patient ratio ranged from 7.1/1.0 for mazindol to 10.3/1.0 for amfepramone. Similar results were obtained for the benzodiazepines with ratios of 1.9/1.0 for clonazepam to 15.6/1.0 for oxazepam. Omissions and mistakes were present in the B prescriptions, including missing information about the patient (in 49.6 percent of the documents) or about the pharmacies or drugstores (50.4 percent). There were cases where the name and/or CRM of the physician was lacking. It was noted that one medical doctor made out 1855 B prescriptions within one year. The same patient's name appeared on 138 prescriptions, and the same RG (identification card number) was present in 125 others. Comparison of Natal's data with those of several other Brazilian cities disclosed a striking similarity throughout Brazil, from Pelotas - Rio Grande do Sul State to Belem-Para State, revealing a practically identical medical/pharmaceutical behavior. This pattern of prescription/dispensation of amphetamine-type substances mostly to women for weight loss is therefore for cosmetic reasons. Consequently, there is an urgent need for an ethical review of this behavior.
Foram examinadas 22.158 notificações B contendo substâncias anoréticas tipo-anfetamina ou de benzodiazepínicos, obtidas de drogarias e de farmácias de manipulação. Os dados foram comparados com os de outras cidades do Brasil, obtendo-se uma visão nacional sobre o assunto. Os achados mostraram que as farmácias de manipulação, dispensaram 85,4 por cento das notificações, ou seja, as farmácias de manipulação atenderam cerca de 10 vezes mais do que as drogarias. A maioria (83,5 por cento) das notificações B nas farmácias de manipulação eram destinadas às mulheres sendo a relação entre pacientes femininos/masculinos de 7,1/1,0 no caso do mazindol e de 10,3/1,0 para a anfepramona. Dados semelhantes foram obtidos para os benzodiazepínicos: relação de 1,9/1,0 para o clonazepam até 15,6/1,0 para o oxazepam. Falhas e erros gritantes foram também observados no preenchimento das notificações B: ausência de dados de pacientes (em 49,6 por cento dos documentos), do fornecedor (50,4 por cento) etc. Houve casos de notificações sem o nome ou CRM do médico e um único médico prescreveu 1.855 notificações B; o nome de uma mesma compradora apareceu em 138 notificações e um mesmo RG em 125 outras. A comparação destes achados com os de outras cidades mostrou uma surpreendente semelhança, ao longo do país, desde Pelotas-RS até Belém-PA; evidenciando um padrão de comportamento médico/farmacêutico praticamente idêntico. Este padrão de prescrição para mulheres destina-se mais para uma finalidade cosmética (perda de peso) do que para uma real necessidade terapêutica. É necessária uma revisão ética sobre este problema, que também tem sido observado e igualmente criticado em vários países.