Phytochemical analysis and investigation of analgesic, anti-inflammatory, and antispasmodic activities of hydroethanolic extracts of Alternanthera dentata, Ocimum carnosum, and Plectranthus barbatus, three species with vernacular names derived from analgesic drugs.

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.

Factors affecting the use of medicinal plants by migrants from rural areas of Brazilian Northeast after moving to a metropolitan region in Southeast of Brazil.

BACKGROUND: Ethnopharmacological studies about migrants reveal a dynamic process of knowledge and use of medicinal plants. In this study, we sought to elucidate quantitative and qualitatively the main factors influencing the use of medicinal plants by migrants from rural areas to an urban region in Brazil with traces of remnant natural vegetation. METHODS: Seven Northeastern individuals who migrated to the Southeastern Region of Brazil (Bororé Peninsula, in the city of São Paulo) were selected to participate in semi-structured interviews regarding the use of medicinal plants throughout their lives, and indicated an inhabitant in their hometown that would be able to accompany the field collections in each area. Socioeconomic, educational, family structure, and use of Western medicine data were provided during interviews with the individuals from their hometowns. Plant samples cited by the interviewees were collected both at the current place of residence and in their hometowns. RESULTS: The participants cited 131 plants and 315 recipes, being the main indications related to the gastrointestinal system, respiratory problems, and pain and inflammatory processes. We observed that most plant uses were maintained after migration. Higher percentages of maintenances and incorporations in plant uses occurred to exotic species, while replacements happen mainly to native plants. The introduction of new species into the migrants' therapeutics occurred mainly by observations of organoleptic similarities between the substituted plant and the incorporated species, conversations with neighbors, and contact with the television and print media. In addition, the public health system allowed the interviewees access to prophylactic drugs, leading to the discontinuation of certain recipes used in endemic diseases. CONCLUSION: Migrants were exposed to information about new plants and their uses, new diseases, and socioeconomic and cultural differences that impacted their use of medicinal plants. Although migration to a more developed city facilitated access to public health and education, on the other hand, it made access to fresh medicinal plants difficult, causing some medicinal plants to be replaced or ceased to be used.

Antioxidant, anticholinesterase and antifatigue effects of Trichilia catigua (catuaba).

BACKGROUND: Trichilia catigua A. Juss. (Meliaceae) is a species known as catuaba and used in folk medicine for the treatment of fatigue, stress, impotence and memory deficit. The main phytochemical compounds identified in the barks of T. catigua are flavalignans, flavan-3-ols and flavonoids which are associated with its antioxidant activity. Pre-clinical studies with T. catigua extracts have identified many pharmacological properties, such as anti-inflammatory, antidepressant, antinociceptive, pro-memory and neuroprotective against ischemia and oxidative stress. This study was designed in order to compare the chemical composition and in vitro antioxidant and anticholinesterase activity of four different polarity extracts and selected the one most active for in vivo studies in rodent models of stress, fatigue and memory. METHODS: Hexane, chloroform, hydroalcoholic and aqueous extracts from bark of Trichilia catigua were analyzed by RPHPLC-DAD-ESI-MS/MS. Antioxidant activity was assessed by 2,2-diphenyl-1-picryl hydrazyl (DPPH) assay and acetylcholinesterase inhibition by Ellman's modified method. In vivo studies (stress, fatigue and memory) were carried out with adult male mice and rats treated with hydroalcoholic extract in doses of 25-300 mg/kg (p.o.). RESULTS: We confirmed the presence of cinchonain IIa, Ia and Ib, as main constituents in the four extracts, while procyanidins were detected only in hydroalcoholic extract. Antioxidant and anticholinesterase activity were observed for all extracts, with most potent activity found on the hydroalcoholic extract (EC50 = 43 µg/mL and IC50 = 142 µg/mL for DPPH scavenger and acetylcholinesterase inhibition, respectively). The treatment of laboratory animals with hydroalcoholic extract did not protect rats from cold immobilization stress and did not prevent the scopolamine-induced amnesia in mice. However, the treatment of mice with the hydroalcoholic extract partially reduced the fatigue induced by treadmill, since the highest dose increased the spontaneous locomotor activity and reduced the deficit on grip strength after the forced exercise (p < 0.05), in some observation times. CONCLUSIONS: These data suggest the hydroalcoholic extract as the most suitable for plant extraction and partially support the folk use of T. catigua as antifatigue drug. . Trichilia catigua hydroalcoholic extract exhibits antioxidant and anticholinesterase activity in vitro and reduces the fatigue induced by forced exercise.

Pre-clinical interaction of ayahuasca, a brew used in spiritual movements, with morphine and propofol

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

Antinociceptive activity of the HPLC- and MS-standardized hydroethanolic extract of Pterodon emarginatus Vogel leaves.

Several studies have demonstrated the analgesic and anti-inflammatory effects of fruit and seed extracts from Pterodon emarginatus Vogel (Fabaceae). The objective of this study was to evaluate the antinociceptive activity of the hydroethanolic extract of P. emarginatus leaves in mice and characterize its chemical composition using HPLC coupled to UV-vis diode array detection and mass spectrometry with electrospray ionization. Our results showed that the doses of 500 and 1000 mg/kg produced an antinociceptive effect, as observed in the hot plate test and writhing induced by acetic acid. The chromatographic profile and spectral mass data suggest the presence of di-C-glycosylflavones (e.g., vicenin-2 and schaftoside), C,O-glycosylflavones (e.g., chrysoeriol-8-C-glucosyl-2″-O-glucuronide-6-C-arabinoside) and luteolin-7-O-rutinoside as the main constituents. Lower levels of oleanane-type saponins, such as soyasaponin Bb and Be, and the saponin derivatives hederagenin and aglycone B, which are typical of Fabaceae family, were also found. From this study, it is suggested that the analgesic effect observed is not due to the terpenoids previously reported from fruit and seed extracts, but could be attributed to flavones and the hederagenin derivatives that were identified as main constituents of the hydroethanolic extract from the leaves.

Memory retrieval improvement by Heteropterys aphrodisiaca in aging rats

Few data exists about the pharmacological properties of Heteropterys aphrodisiaca O. Mach. (Malpighiaceae), which is native to the scrubland regions of Brazil. The present study investigated the effects of oral treatment with H. aphrodisiaca extract (BST0298) on the learning and memory of young (3-6 months) and aged (21-23 months) rats, and compared the in vitro antioxidant activity of three lots collected in different years. An improvement in the number of sessions to learn the task was observed in the left/right discrimination test in aged rats treated for 45 days with 25 mg/kg (7.0 ± 0.5; p=0.005) or 50 mg/kg (7.6 ± 0.6; p=0.012) compared with control old rats (11.0 ± 1.6). On the other hand, pre-treatment did not improve the performance of scopolamine-treated mice in the passive avoidance test. The in vitro malondialdehyde test showed that all three different extracts presented similar antioxidant activity. The flavonoids astilbin, isoastilbin and neoastilbin were isolated from the extract and may contribute to the biological activity. These results suggest that repeated treatment with H. aphrodisiaca improves learning and memory, probably by a non-muscarinic mechanism.

Existem poucos dados disponíveis sobre as propriedades farmacológicas da Heteropterys aphrodisiaca O. Mach. (Malpighiaceae), nativa da região do pantanal brasileiro. O presente estudo investigou o efeito do tratamento oral com um extrato de H. aphrodisiaca (BST0298) sobre a memória e aprendizagem de ratos jovens (3-6 meses) e idosos (21-23 meses) e comparou a atividade antioxidante in vitro de três lotes, coletados em diferentes anos. Melhora quanto ao número de sessões necessárias para aprender a tarefa foi observada no teste de discriminação direita/esquerda em ratos idosos tratados por 45 dias com doses de 25 mg/kg (7,0 ± 0,5; p=0,005) e 50 mg/kg (7,6 ± 0,6; p=0,012) comparados com ratos idosos controle (11,0 ± 1,6). Por outro lado, o pré-tratamento com o extrato não melhorou o desempenho de camundongos tratados com escopolamina no teste da esquiva passiva. Em relação à avaliação da atividade antioxidante in vitro pelo teste do malonodialdeído, os três lotes analisados apresentaram atividade antioxidante semelhante. Os flavonóides astilbina, isoastilbina e neoastilbina foram isolados do extrato e podem contribuir para a atividade biológica. Estes resultados sugerem que a administração repetida de H. aphrodisiaca melhora a memória e aprendizagem provavelmente por um mecanismo não muscarínico.

Possible anxiolytic effect of two extracts of Passiflora quadrangularis L. in experimental models.

Several species of the genus Passiflora, known in Brazil as 'maracujá', have widespread use in folk medicine as sedatives and anxiolytics. The anxiolytic activities of aqueous and hydroalcohol extracts of Passiflora quadrangularis leaves were evaluated using the elevated plus-maze, open field and holeboard tests. The hydroalcohol extract presented results suggestive of anxiolytic activity in dosages around 100, 250 and 500 mg/kg, as expressed by elevation of the time spent on the open arms in the plus-maze; a decrease of freezing and an increase of deambulation and rearing in the open field test. The hydroalcohol extract showed results similar to diazepam on the holeboard. No positive results were found for the aqueous extract.

Evaluation of Baccharis trimera and Davilla rugosa in tests for adaptogen activity.

Baccharis trimera (Asteraceae) and Davilla rugosa (Dilleniaceae) are used popularly as tonics, aphrodisiacs and for stomach ailments, among other uses. Hydroalcohol extracts of the aerial parts of both plants were investigated with regard to their chemical constitution and their pharmacological activity in tests that evaluate adaptogen activity. Alkaloids, flavonoids, saponins, polyphenols/tannins and coumarins were identified in both extracts, while lignans were found only in the extract of Davilla rugosa. This extract presented also a marked antioxidant activity and exerted a moderate antiulcer effect in rats submitted to cold immobilization stress. It did not, however, inhibit the increase in the levels of ACTH and corticosterone induced by stress. Moreover, the Davilla rugosa did not improve the physical performance of mice submitted to forced exercise and the learning time of old rats in the T-maze, neither did it reduce the blood viscosity of the old animals. Conversely, the Baccharis trimera extract only presented a moderate antioxidant activity, without any positive effect on the other tests. These results point to the absence of an adaptogen activity of Baccharis trimera, with some effects that could be related to such an activity as regards the Davilla rugosa.

Brazilian plants as possible adaptogens: an ethnopharmacological survey of books edited in Brazil.

In a survey, from Brazilian books, we searched plants that are in popular use for purposes resembling those of an adaptogen. This study focused on 24 books by authors from diverse regions in the country, resulting in a total of 1317 citations of uses related to a possible adaptogen effect from approximately 766 plants. Only species native to Brazil, cited in at least four books, were selected, resulting a total of 33 species, belonging to 24 families. Of these, four species have been studied previously in relation to effects that are considered as part of an adaptogen effect (anti-stress, memory enhancement, increased physical and/or sexual performance): Heteropterys aphrodisiaca (Malpighiaceae), Paullinia cupana (Sapindaceae), Ptychopetalum olacoides (Olacaceae), and Turnera diffusa (Turneraceae). Three others--Pfaffia glomerata, Pfaffia paniculata (Amaranthaceae), and Trichilia catigua (Meliaceae)--have also been the object of pharmacological studies that support their use as a possible adaptogen, but they are listed in less than four books. The overall results obtained in the present review of Brazilian folk literature reveals that Brazil is rich in plants with potential adaptogen-like effect, but lacks pharmacological studies (mostly clinical ones) to confirm these therapeutic properties.

Avaliação farmacológica da carqueja(Baccharis trimera) e do cipó-caboclo(Davilla rugosa), duas plantas brasileiras utilizadas popularmente como tônicas, em teste para ação adaptógena / Pharmacological evaluation of carqueja(Baccharis trimera and cipó-caboclo(davilla rugosa), two brazilian plants popularly used as tonics, in tests for adaptogen activity

O termo adaptógeno foi criado por Lazarev para classificar substâncias capazes de induzir um aumento não específico da resistência do organismo frente a fatores estressantes de diferentes naturezas. Além disto, prega-se que um adaptógeno poderia aumentar as condições de saúde, melhorando a qualidade de vida, as funções cognitivas e aumentando o desempenho físico e sexual. Apesar de algumas dúvidas, se os adaptógenos poderiam agir em indivíduos saudáveis, a literatura aponta estudos em humanos tanto com resultados positivos como negativos. Os mecanismos de ação pelos quais os adaptógenos agem não estão claros, mas parece que seus efeitos ocorrem por meio de um conjunto de ações, incluindo modulação do eixo HPA e do sistema imunológico, aumento da síntese protéica, da atividade da hexoquinase e ação antioxidante. Entre as principais plantas utilizadas como adaptógenas, devem ser citadas o Panax ginseng, a Ginkgo biloba e o Eleutherococcus senticosus. No Brasil, o termo adaptógeno é pouco conhecido, porém a população faz uso de diversas expressões que lembram as características englobadas por um adaptógeno, como tônico, antiestresse, afrodisíaco, bom para a memória, entre tantos outros. Um levantamento realizado na literatura popular apontou um grande número de plantas com as indicações acima. Para este estudo foram selecionadas duas espécies bastante citadas e que não possuem estudos científicos relacionados com o efeito-alvo desta pesquisa: Baccharis trimera (BT) e Davilla rugosa (DR) - respectivamente chamadas pela população de carqueja e cipó-caboclo. Inicialmente, preparou-se o extrato hidroalcoólico (EHA) das partes aéreas das duas plantas e foi realizada a prospecção fitoquímica com eles, indicando a presença de flavonóides, cumarinas, saponinas, polifenóis / taninos para ambos os extratos. Lignanas foram identificadas apenas no extrato de BT. Outras classes fitoquímicas não foram detectadas ou pesquisadas. Os EHA foram administrados agudamente em camundongos para realização de um "screenig" e verificação da toxicidade. As duas plantas apresentaram baixa toxicidade por via oral, no entanto os extratos de DR e BT mostraram moderada toxicidade para a via ip...