No / Alangium lamarkii is traditionally used in India for the treatment of malaria. Partial activity guided-fractionation of the basic chloroform fraction of the methanolic extract of the bark led to the isolation of a novel tubulosine analogue, 10-demethyl-9ˊ-N-methyltubulosine (1), for which the trivial name tubulosatine is suggested. In addition, the known A. lamarkii constituents, tubulosine (2), cephaeline and emetine were isolated as potent antiplasmodial and cytotoxic constituents, but 1 was up to 1000-fold less potent than the former alkaloids against both malaria parasites and human cancer cell lines. The compounds were active against both chloroquine-sensitive and chloroquine-resistant malaria parasites, but no selective toxicity was observed towards malaria parasites compared with cancer cells with any of the alkaloids. Further work to explore the basis for the relatively weak biological activities of 1 would be worthwhile. Betulinic acid, stigmasterol and its 3-O-glucoside were isolated from the neutral chloroform fraction of the methanolic extract. / ACU, UK (Commonwealth Scholarship, Ref. No.: INCS-2004-144).

Os levantamentos etnodirigidos reportam o conhecimento das plantas medicinais utilizadas pelas populações locais de geração em geração. O objetivo da pesquisa foi esmiuçar o entendimento popular com relação ao uso e modo de preparo das plantas utilizadas na medicina popular nos municípios de Talismã e Gurupi situados na região sul do estado do Tocantins. Foram aplicados 50 questionários semiestruturado com indivíduos de faixa etária entre 20 a 89 pela metodologia bola de neve até o esgotamento amostral, tendo o gênero feminino com maior representatividade. Cento e seis (106) plantas foram identificadas no levantamento, totalizando 42 famílias destacando-se a família Lamiaceae. A planta mais citada simultaneamente nas duas cidades foi a Mentha piperita e a parte da planta mais usada foi a folha na cidade de Gurupi e a casca em Talismã. Os resultados contribuem para o conhecimento das plantas medicinais utilizadas na região estudada e para que novos levantamentos sejam realizados para maior perfilamento das plantas regionais e sua utilização. / Ethnodirigid surveys report the knowledge of medicinal plants used by local populations from generation to generation. The objective of the research was to sculpt the popular understanding regarding the use and method of preparation of the plants used in popular medicine in the counties of Talismã and Gurupi located in the southern region of the state of Tocantins. Fifty semistructured questionnaires were applied to individuals aged 20 to 89 by the snowball methodology until sample exhaustion, with the female gender being the most representative. One hundred and six (106) plants were identified in the survey, totaling 42 families, especially the Lamiaceae family. The most frequently cited plant in both cities was Mentha piperita and the most commonly used plant was the leaf in the town of Gurupi and the bark in Talisman. The results contribute to the knowledge of the medicinal plants used in the studied region and so that new surveys are carried out for a better profiling of the regional plants and their use.

Submitted by Jean Medeiros (jeanletras@uepb.edu.br) on 2016-03-17T14:18:06Z No. of bitstreams: 1 PDF - Katharina Rodrigues de Lima Porto Ramos.pdf: 2185372 bytes, checksum: d2b102a4f6ef6b42be28bada2852f309 (MD5) / Approved for entry into archive by Secta BC (secta.csu.bc@uepb.edu.br) on 2016-07-22T13:36:00Z (GMT) No. of bitstreams: 1 PDF - Katharina Rodrigues de Lima Porto Ramos.pdf: 2185372 bytes, checksum: d2b102a4f6ef6b42be28bada2852f309 (MD5) / Approved for entry into archive by Secta BC (secta.csu.bc@uepb.edu.br) on 2016-07-22T13:36:13Z (GMT) No. of bitstreams: 1 PDF - Katharina Rodrigues de Lima Porto Ramos.pdf: 2185372 bytes, checksum: d2b102a4f6ef6b42be28bada2852f309 (MD5) / Made available in DSpace on 2016-07-22T13:36:13Z (GMT). No. of bitstreams: 1 PDF - Katharina Rodrigues de Lima Porto Ramos.pdf: 2185372 bytes, checksum: d2b102a4f6ef6b42be28bada2852f309 (MD5) Previous issue date: 2013-09-04 / Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPES / Diarrhea is often associated with excessive defecation caused by increased motility and secretion. Spondias purpurea L. belongs to the genus Spondias, used by the population as gastroprotecti ve, antidiarrheal and antimicrobial. The objecti ve of this work was to evaluate the antidiarrheal acti vity of crude ethanol extract and dichloromethane phase of S. purpurea L., in animal models. Were obtained from the ethanol extract (Sp-EtOHE) and phase dichloromethane (Sp-DCPM) of the leaves of S. purpurea. In determi ning phytochemical noted that Sp-EtOHE was approximately 6.70% of total flavonoids, polyphenols and 3.17%. Toxicological evaluation by the method of Artemia salina Leach, the samples showed values of 50% lethal concentration (LC50) of 2300.67 ± 196.66 mg / mL for Sp-EtOHE and 1106.17 ± 102.24 mg / mL for Sp-DCPM, indicating not present toxicity. In Test Toxicology Preclinical acute was administered 2000 mg / kg Sp-EtOHE was observed only irritability reversed in females after the 2nd hour, this being a given insufficient for inferri ng toxicity, also did not cause variations i n the height or i n the macroscopic structure bodies, water consumption, diet and biochemical and hematological parameters. Unable to determine the LD50, as there were no deaths at the end of the 14 days of observation. With respect to antimicrobial acti vity by microdilution, there was no activity Sp-EtOHE and Sp-DCPM concentrations tested against the tested microorganisms. In determini ng the gastrointestinal motility through the model of induced diarrhea i n rats castor oil, the inhibition was 33, 54 and 63% Sp-EtOHE and 63, 68 and 85% for Sp-DCPM, both at doses of 125 , 250 and 500 mg/kg (po). It was observed a decrease i n the number of liquid stools at 41, 67 and 25% for Sp-EtOHE and 48, 68 and 65 for Sp-DCPM. In relation to the total number of feces both Sp- EtOHE and Sp-DCPM as presented similar behavior. The CRP-ultrasensitive was quantified and reduced levels of acute inflammation. There was an increase in the concentrations of ionograms. The study confirmed that Sp-DCPM minimized the histological damage in the ileum. The model to assess changes in gastric emptying and i ntesti nal motility values Sp-EtOHE and Sp-DCPM not statistically significant . These results show that S. purpurea may be possible antidiarrheal as indicated by the traditional medicine that does not cause constipation not reach the intesti nal bacterial flora and anti-inflammatory acti vity. / A diarreia está associada à frequência excessiva de defecação, provocada pelo aumento da motilidade e secreção. Spondias purpurea L. pertence ao gênero Spondias, utilizado pela população como gastroprotetora, antidiarreica e antimicrobiana. Assim, o objeti vo deste trabalho foi avaliar a atividade antidiarreica do extrato etanólico bruto e da fase diclorometano de S. purpurea L., em modelos animais. Foram obtidos o extrato etanólico (EEtOH-Sp) e a fase diclorometano (FaDCM-Sp) das folhas de S. purpurea. Na determi nação fitoquímica foi observado que o EEtOH-Sp apresentou aproximadamente 6.70% de flavonóides totais, e 3,17% de polifenóis. Na avaliação toxicológica, pelo método da Artemia salina Leach, as amostras apresentaram valores de Concentração Letal 50% (CL ) de 2300,67±196,66 µg/mL para o EEtOH-Sp e 1106,17±102,24 µg/mL para a FaDCM- Sp, indicando não apresentarem toxicidade. No Ensaio Toxicológico Pré-clínico Agudo, foi administrada 2000 mg/kg do EEtOH-Sp e foi observada apenas irritabilidade revertida nas fêmeas após a 2ª hora, sendo este um dado insufi ciente para inferir toxicidade, também não provocou variações no peso nem na estrutura macroscópica dos órgãos, no consumo de água, ração e nos parâmetros bioquímicos e hematológicos. Não foi possível determinar a DL , visto que não houve mortes, ao fi nal dos 14 dias de observação. Com relação à ati vidade 50 antimicrobiana pela técnica de microdiluição, não foi observada atividade de EEtOHSp e FaDCM-Sp nas concentrações testadas frente aos microorganismos testados. Na determi nação da motilidade gastri ntesti nal, através do modelo de diarreia induzida por óleo de rícino em ratos, a inibição foi de 33, 54 e 63% para EEtOH-Sp e 63, 68 e 85% para FaDCM-Sp, ambos nas doses de 125, 250 e 500 mg/kg (v.o.). Foi observada uma diminuição do número de fezes líquidas em 41, 67 e 25% para EEtOH-Sp e 48, 68 e 65% para FaDCM-Sp. Em relação ao número total de fezes tanto o EEtOH-Sp quanto a FaDCM-Sp apresentaram comportamento semelhante. A PCR-ultrassensível foi quantificada e reduziu os níveis de inflamação aguda. Houve um aumento nas concentrações dos ionogramas. O estudo histopatológico confirmou que FaDCM-Sp minimizou o dano histológico no íleo. No modelo para avaliar alterações no esvaziamento gástrico e na motilidade intestinal, os valores do EEtOH-Sp e FaDCM-Sp não apresentaram significância estatística. Estes resultados mostram que S. purpurea pode ser um possível antidiarreico, como indicado pela medicina tradicional, que não causa constipação, não atinge a flora bacteriana intestinal e com atividade anti-inflamatória.

Submitted by Jean Medeiros (jeanletras@uepb.edu.br) on 2016-03-18T11:35:43Z No. of bitstreams: 1 PDF - Cynthia Layse Ferreira de Almeida.pdf: 3612014 bytes, checksum: ff23a88527b4e07c470c1b649ddb0716 (MD5) / Approved for entry into archive by Secta BC (secta.csu.bc@uepb.edu.br) on 2016-07-22T15:01:26Z (GMT) No. of bitstreams: 1 PDF - Cynthia Layse Ferreira de Almeida.pdf: 3612014 bytes, checksum: ff23a88527b4e07c470c1b649ddb0716 (MD5) / Approved for entry into archive by Secta BC (secta.csu.bc@uepb.edu.br) on 2016-07-22T15:01:35Z (GMT) No. of bitstreams: 1 PDF - Cynthia Layse Ferreira de Almeida.pdf: 3612014 bytes, checksum: ff23a88527b4e07c470c1b649ddb0716 (MD5) / Made available in DSpace on 2016-07-22T15:01:35Z (GMT). No. of bitstreams: 1 PDF - Cynthia Layse Ferreira de Almeida.pdf: 3612014 bytes, checksum: ff23a88527b4e07c470c1b649ddb0716 (MD5) Previous issue date: 2013-09-04 / Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPES / Spondias purpurea L. (Anacardiaceae), popularly known as “siriguela”, is used in folk medicine for the relief of fever and pain, as diarrhea medication, antispasmodic, diuretic, anti-anemic and analgesic. Pharmacognostic studies with the species indicate the strong presence of tannins, flavonoids and triterpenes in their leaves, and roots, which are generally related to the antiulcer activity. The aim of this study was to evaluate the gastroprotective activity of the extract phase of S. purpurea in animal models. For this, the ethanolic extract (Sp-EtOHE) and the dichloromethane fraction (Sp-DCMF) of leaves of S. purpurea were obtained. Regarding the gastroprotective activity, doses of 125, 250 and 500 mg/kg (p.o.) were tested against different models of acute induction of ulcer by acidified ethanol, ethanol, stress immobilization and cold, and nonsteroidal anti-inflammatory drug (NSAID). In the model of acidified ethanol, there was a reduction in the ulcerative lesion index (ULI) for 61, 71 and 65% Sp-EtOHE and 29, 77 and 68% to Sp-DCMF. In ulceration caused by ethanol, Sp-EtOHE and Sp-DCMF in the same doses protect the gastric mucosa and were not altered parameters of the stomach contents of rats. The evaluation by the stress model, Sp-EtOHE and Sp-DCMF decreased the ULI in 23, 59 and 70% and 24, 61 and 72%, respectively. Previous models were made for the determination of C-Reactive Protein (CRP) in blood samples and were observed significant reductions of this parameter. Similarly, in the model of NSAID-induced gastric ulcers, there was inhibition of injuries to Sp-EtOHE and Sp-DCMF. In order to investigate the mechanisms of action related to gastroprotection promoted by SpEtOHE (250 mg/kg) and Sp-DCMF (250 mg/kg) was evaluated the involvement of nitric oxide and sulfhydryl compounds. Thus, it was verified that the gastroprotective effect of S. purpurea not involve the participation of nitric oxide. However, this effect is related to the participation of sulfhydryl compounds. Thus, these data suggest that S. purpurea presents gastroprotective activity, possibly related to mechanisms cytoprotectives. / Spondias purpurea L. (Anacardiaceae), popularmente conhecida como “siriguela”, é utilizada na medicina popular para o alívio de febre e dores, como antidiarréico, antiespasmódico, diurético, analgésico e antianêmico. Estudos farmacognósticos realizados com a espécie indicam a presença marcante de taninos, flavonoides e triterpenos em suas folhas, e raízes, os quais geralmente estão relacionados com a atividade antiulcerogênica. Assim, o objetivo deste trabalho foi avaliar a atividade gastroprotetora do extrato e fase de S. purpurea em modelos animais. Para isso foram obtidos o extrato etanólico (EEtOH-Sp) e a fase diclorometano (FaDCM-Sp) das folhas de S. purpurea. Com relação à atividade gastroprotetora, as doses de 125, 250 e 500 mg/kg (v.o.) do EEtOH e FaDCM foram testados frente a modelos de indução aguda de úlcera por etanol acidificado, etanol, estresse por imobilização e frio e anti-inflamatório não-esteroidal (AINE). No modelo de etanol acidificado, houve a redução do índice de lesão ulcerativo (ILU) em 61, 71 e 65% para EEtOH e 29, 77 e 68% para FaDCM. Nas ulcerações causadas por etanol, EEtOH-Sp e FaDCM-Sp nas mesmas doses protegeram a mucosa gástrica, bem como não foram alterados parâmetros do conteúdo estomacal dos ratos. Na avaliação pelo modelo do estresse, EEtOH-Sp e FaDCM-Sp diminuíram o ILU em 23, 59, 70 e 24, 61, 72%, respectivamente. Foram realizados para os modelos anteriores a dosagem da Proteína C reativa ultrassensível (PCR) nas amostras de sangue e foram observadas reduções significativas deste parâmetro. Da mesma maneira, no modelo de úlceras gástricas induzidas por AINE, houve inibição das lesões para EEtOH-Sp e FaDCM-Sp. No intuito de investigar os mecanismos de ação relacionados à gastroproteção promovida pelo EEtOH-Sp (250 mg/kg) e FaDCM-Sp (250 mg/kg), foi avaliado o envolvimento do óxido nítrico e dos grupamentos sulfidrílicos. Assim, foi observado que o efeito gastroprotetor de S. purpurea não envolve a participação do óxido nítrico. Entretanto, este efeito está relacionado à participação dos grupamentos sulfidrílicos, sugerindo que S. purpurea apresenta atividade gastroprotetora, possivelmente relacionada a mecanismos citoprotetores.

This thesis investigates the phytochemistry and pharmacology of two neotropical plants used traditionally to treat anxiety and stress, Souroubea sympetala (Marcgraviaceae) and Piper amalago (Piperaceae). A method of phytochemical analysis was developed to characterize S. sympetala extracts, identifying and quantifying four triterpenes, which were present in higher amounts in bark as compared to leaf. Subsequently, a standardized supercritical CO2 extraction procedure for S. sympetala was developed and compared favourably with conventional extraction methods in terms of its anxiety-reducing effects in a behavioural assay of anxiety and content of the active principle, betulinic acid (BA). All of these materials demonstrated anxiolytic properties. The pharmacological mode of action of S. sympetala raw plant, extracts and isolated active principle were examined in rodent behavioural models of anxiety. The extracts were shown to have affinity for the γ-amino butyric acid (GABA)a benzodiazepine (GABAa- BZD) receptor of the central nervous system in vitro, in a competitive binding assay. Pre-treatment of animals with the GABAa-BZD antagonist flumazenil, followed by plant extract and pure compound extinguished the anxiety-reducing effect, demonstrating that S. sympetala and BA act at the GABAa- BZD receptor in vivo. The effect of S. sympetala in stressed animals, specifically its cortisol-lowering ability was investigated in vitro and in vivo in rainbow trout. Both leaf extract and BA significantly lowered cortisol in response to an adrenocorticotropic hormone (ACTH) challenge in vitro and a standardized net restraint assay in vivo. The anxiety-reducing effect of P. amalago was examined and the bioactive principle identified by bioassay-guided fractionation. P. amalago extract significantly reduced anxiety-like behaviour in rats and demonstrated affinity for the GABAa-BZD receptor in vitro. The bioactive molecule was determined to be a furofuran lignan. Together these results provide a pharmacological basis for the traditional use of S. sympetala and P. amalago to treat anxiety and elucidate their mode of action and active principles. S. sympetala is now thoroughly characterized and represents an excellent candidate plant for development as a natural health product.

Thesis (PhD)-- Macquarie University, Division of Environmental and Life Sciences, Dept. of Chemistry and Biomolecular Science. 2006. / Bibliography: p. 229-249.

Au Burkina Faso, W. indica L. syn. W. americana est utilisée en médecine traditionnelle dans la prise en charge aussi bien curative que préventive de l'asthme. Basée sur une approche ethnopharmacologique, cette étude visait à caractériser W. indica sur le plan chimique et pharmacologique en relation avec l'usage traditionnel contre l'asthme. Méthodologie : Après avoir confirmé les données bibliographiques sur l'usage antiasthmatique de la plante par un entretien avec des tradipraticiens de santé, une recherche bioguidée a été réalisée. Des investigations chimiques à type d'extraction, de purification et de détermination structurale ont été conduites en alternance avec les investigations biologiques de laboratoire. En outre, une caractérisation in situ des groupes chimiques a été réalisée dans différentes parties de la plante. Puis, une évaluation de la toxicité générale aigue de l'extrait hydro alcoolique des racines a été réalisée chez la souris. Résultats et discussion : Des alcaloïdes et des polyphénols ont été mis en évidence dans les différentes parties de la plante. Plusieurs composés ont été isolés à partir de l'extrait hydro alcoolique (HA) des racines. Un seul a été identifié comme étant (-)-épicatéchine. HA, ses fractions n-hexane (F1), dichlorométhane (F2), acétate d'éthyle (F3), la fraction résiduelle (F4) et l'épicatéchine isolée de F3 inhibaient in vitro l'activité de la 5-LOX, la LOX-IB de soja et la PLA2 de manière dose dépendante. L'inhibition de la PDE4A1α par les fractions n'était pas dose dépendant. Sur le plan tissulaire, HA, F3 et les fractions dérivées de F3 inhibaient les contractions induites par l'acétylcholine sur la trachée de rat ex vivo. Un effet dose dépendant était observé avec une CI50 de 1051 µg/mL pour HA, entre 181 et 477 µg/mL pour F3 et ses fractions. HA est modérément toxique chez la souris par voie intrapéritonéale (DL50 =210 mg/Kg). Cette étude est la première investigation pharmacologique de l'usage traditionnel de W. indica contre l'asthme. Nos résultats supportent cet usage traditionnel de la plante et démontrent la participation de l'épicatéchine aux propriétés antiasthmatiques. Conclusion : La validation pharmacologique de l'usage traditionnel de W. indica contre l'asthme doit être complétée par les futures investigations précliniques avec l'isolement et les tests biologiques d'autres composés de la plante qui participeraient à l'activité de W. indica. / In Burkina Faso, W. indica L. syn. W. americana is used by traditional healers for curative and preventive management of asthma. Based on an ethnopharmacological approach, this study aimed to characterize W. indica on the chemical and pharmacological level according to the traditional use against asthma. Methodology: First, interviews of traditional healers confirmed the literature data concerning traditional use of the plant against asthma. Second, chemical investigations were conducted alternatively with biological investigation. Moreover, an in situ characterization of mains chemical groups was performed in different parts of the plant; then, a general acute toxicity of hydro alcoholic extract was evaluated in mice. Results and discussion: Alkaloids and polyphenols are presents in different parts of W. indica. Several compounds have been isolated from hydro alcoholic roots extract (HA). One compound have been identified as (-)-epicatechin. In vitro, HA, its fractions n-hexane (F1), dichloromethane (F2), ethyl acetate (F3), residual fraction (F4) and (-)-epicatechin isolated from F3 dose-dependently inhibited the activity of 5-LOX, LOX-IB de soja and PLA2. Inhibition of PDE4A1α by fractions was not dose-dependent. On tissue level, HA, F3 and fractions from F3 inhibited contraction induced by acetylcholine on rat trachea ex vivo. This effect was dose-dependent with IC50 of 1051 µg/mL for HA, between 181 and 477µg/mL for F3 and its fractions. HA is moderately toxic in mice (LD50 =210 mg/Kg, intraperitoneal route). This study is the first pharmacological investigation of traditional use of W. indica against asthma. Our results validate the use of W. indica in traditional for management of asthma. These effects should be, at least in part, attributed to the presence of (-)-epicatechin in roots of W. indica. Conclusion: The pharmacological validation of traditional use of W. indica against asthma must be completed in the future research by isolation and biological assays of other compounds which could participate to activity of W. indica.

Submitted by Mario BC (mario@bc.ufrpe.br) on 2016-07-28T12:45:58Z No. of bitstreams: 1 Vanessa de Carvalho Nilo Bitu.pdf: 8806452 bytes, checksum: ac94c591ad656bdd84aaf9a0faaa5f5a (MD5) / Made available in DSpace on 2016-07-28T12:45:58Z (GMT). No. of bitstreams: 1 Vanessa de Carvalho Nilo Bitu.pdf: 8806452 bytes, checksum: ac94c591ad656bdd84aaf9a0faaa5f5a (MD5) Previous issue date: 2015-08-03 / This bioprospective study with an ethno-directed approach took into consideration the knowledge of vendors of medicinal plants in a region of Northeast Brazil known as Triângulo Crajubar. Our aim was to survey the plants sold for therapeutic purposes in public markets in the area studied, to select the plant species based on ethnopharmacological use and to analyze them for phytochemical composition and antibacterial and antiparasitic activities. Medicinal plant vendors were asked to fill out a questionnaire to determine the relative importance of the species and informant consensus factor. Ninety-one species were indicated as being therapeutically useful; they were distributed in 49 families and 89 genera. Thirteen species showed great versatility in their use. There were 291 indications of use in 13 disease categories. On the basis of these results, the plant species Operculina hamiltonii, Cephaelis ipecacuanha and Lippia gracilis were selected and evaluated as follows, according to their ethnopharmacological use. The infusion of O. hamiltonii (IOh) and decoction of C. ipecacuanha (DCi) were analyzed by HPLC-DAD, while the chemical composition of the essential oil of L. gracilis (OELG) was determined by gas chromatography coupled to mass spectrometry. IOh was tested in vitro for epimastigote and promastigote susceptibility and cytotoxicity. IOh, DCi and OELG were subjected to broth microdilution assays to determine the minimal inhibitory concentration against bacteria; solutions of the natural products were also tested at subinhibitory concentrations to evaluate them for antibiotic resistance-modifying activity. O. hamiltonii showed high leishmanicidal and trypanosomicidal activities, but also substantial cytotoxicity. O. hamiltonii and C. ipecacuanha did not exhibit satisfactory antibacterial activity, but assays for modulatory potential demonstrated interesting results with synergism observed using various combinations of antibiotics and natural products. OELG was able to modulate bacterial resistance and could be used as a coadjuvant therapy against multidrug-resistant microrganisms. / Esse trabalho bioprospectivo com abordagem etnodirigida levou em consideração o conhecimento dos vendedores de plantas medicinais em uma região do Nordeste brasileiro conhecida como Triângulo Crajubar e objetivou realizar um levantamento das plantas comercializadas para fins terapêuticos nos mercados públicos da área estudada, selecionar espécies vegetais a partir do seu uso etnofarmacológico e realizar análises químicas, microbiológicas e parasitológicas. Foram aplicados aos vendedores de plantas nos mercados públicos, formulários que permitiram o cálculo da importância relativa das espécies e do fator de consenso dos informantes. Foram indicadas por estes, 91 espécies úteis terapeuticamente, distribuídas em 49 famílias botânicas e 89 gêneros. Treze espécies apresentaram grande versatilidade quanto ao seu uso. Foram obtidas 291 indicações de uso em 13 categorias de doenças. Com base nesses resultados, foram selecionadas as espécies botânicas Operculina hamiltonii, Cephaelis ipecacuanha e Lippia gracilis, que foram avaliadas nas etapas subsequentes, segundo o seu uso etnofarmacológico. A infusão de Operculina hamiltonii (IOh) e o decocto de Cephaelis ipecacuanha (DCi) tiveram seus compostos fenólicos e flavonóides quantificados por HPLC-DAD enquanto o óleo essencial de Lippia gracilis (OELG) teve a sua composição química analisada por cromatografia gasosa acoplada a espectrofotometria de massas. A IOh foi submetida a ensaios de susceptibilidade epimastigota e promastigota in vitro e ensaios citotóxicos. Para a IOh, o DCi e o OELG foram determinadas as concentrações inibitórias mínimas em ensaio de microdilução em caldo; as soluções dos produtos naturais foram testadas em concentrações subinibitórias para avaliação da atividade moduladora da resistência aos antibióticos. Operculina hamiltonii apresentou uma elevada atividade leishmanicida e tripanossomicida, no entanto com citotoxicidade significativa. Operculina hamiltonii e a Cephaelis ipecacuanha não apresentaram atividade antibacteriana clinicamente satisfatória pelo método estudado, no entanto os testes de avaliação do potencial modulador demonstraram resultados relevantes com sinergismo observado em várias combinações dos antibióticos com os produtos naturais. O óleo essencial de Lippia gracilis teve a capacidade de modular a resistência bacteriana e pode ser utilizado como uma terapia coadjuvante contra microrganismos multirresistentes.

Orientador: Alba Regina Monteiro Souza Brito / Tese (doutorado) - Universidade Estadual de Campinas, Instituto de Biologia / Made available in DSpace on 2018-08-11T01:42:07Z (GMT). No. of bitstreams: 1 Fernandes_PriscilaCorreia_D.pdf: 3896629 bytes, checksum: 2adb4a717d2889c7460fc1fd86d20a4e (MD5) Previous issue date: 2005 / Resumo: A etnofarmacologia é uma ciência multidisciplinar que estuda a diversidade cultural e biológica. Especificamente lida com os usos que comunidades tradicionais fazem das espécies vegetais para fins terapêuticos. A disciplina utiliza recursos das ciências humanas e biológicas para traduzir e representar o saber tradicional em conhecimento científico. O grupo do Laboratório de Produtos Naturais tem se dedicado à pesquisa de compostos de origem vegetal com potencial atividade medicinal. A principal base para escolha dos compostos a serem pesquisados são dados etnofarmacológicos. O projeto "Etnofarmacologia e Educação Ambiental" surgiu do interesse do grupo de pesquisa pela devolução do conhecimento científico para as comunidades. Dessa forma a presente pesquisa estuda o uso da etnofarmacologia como ferramenta principal no estabelecimento de projetos de educação ambiental. A pesquisa foi desenvolyida em quatro comunidades, sendo duas rurais e duas urbanas nos municípios de Atibaia e Sumaré, nos anos de 2002 a 2004, onde foram realizados levantamento etnofarmacológicos. A pesquisa etnofarmacológica deu base para projetos de educação ambiental em unidades escolares de ensino fundamental. Foi possível verificar que a escola pode atuar como via de acesso do pesquisador na comunidade estudada, proporcionando o reconhecimento da realidade local e do conhecimento popular acumulado. O método mostrou-se útil no estabelecimento de comunicação entre fls comunidades escolares e o grupo de pesquisa, numa perspectiva de diálogo entre os saberes, a fim de valorizar o conhecimento tradicional e popular da flora e promover a divulgação científica. A educação ambiental foi trazida para uma realidade local, representada pela diversidade cultural e biológica também locais. O projeto mostrou-se interessante para a valorização da cultura popular, para a conservação e recuperação dos espaços locais e para a divulgação científica / Abstract: Ethnopharmacology is a multidisciplinary science that studies the cultural and biological diversity. Especifically deals with the traditional communities uses of vegetal species for terapeutic purposes. It uses resources from human and biological sciences to translate and represent the traditional wisdom in scientific language. The Natural ProductsLaboratory conéentrates efforts on the research of vegetal compounds with pharmacological activities. The main ground to the search for medicinal plant species is the ethnopharmacological research. The project called "Ethnopharmcology and Environmental Education" bom from the group interest in the devolution of benefits from the researches to the traditional communities. Thus, the present work studies the use of ethnopharmacological data as a tool in the establishment of environmental educational programms. The research was held in four communities, rural and urban in the cities of Atibaia and Sumaré, from 2002 to 2004. The ethnopharmcological research gave the base to Environmental Education projects in basic schools. It was possible to verify that the school can provide an efficient access of scientists to local realities and popular knowledge about medicinal species. The method is utile to establish communication between communities and university, to add value to the traditional knowledge about local flora and to promote scientific divulgation. The Envieronmental Education was brought to a .local reality, represented by local cultural and biological diversity. The project also showed value to the tservation of culture and biodiversity / Doutorado / Fisiologia / Doutor em Biologia Funcional e Molecular

This thesis investigates the phytochemistry and pharmacology of two neotropical plants used traditionally to treat anxiety and stress, Souroubea sympetala (Marcgraviaceae) and Piper amalago (Piperaceae). A method of phytochemical analysis was developed to characterize S. sympetala extracts, identifying and quantifying four triterpenes, which were present in higher amounts in bark as compared to leaf. Subsequently, a standardized supercritical CO2 extraction procedure for S. sympetala was developed and compared favourably with conventional extraction methods in terms of its anxiety-reducing effects in a behavioural assay of anxiety and content of the active principle, betulinic acid (BA). All of these materials demonstrated anxiolytic properties. The pharmacological mode of action of S. sympetala raw plant, extracts and isolated active principle were examined in rodent behavioural models of anxiety. The extracts were shown to have affinity for the γ-amino butyric acid (GABA)a benzodiazepine (GABAa- BZD) receptor of the central nervous system in vitro, in a competitive binding assay. Pre-treatment of animals with the GABAa-BZD antagonist flumazenil, followed by plant extract and pure compound extinguished the anxiety-reducing effect, demonstrating that S. sympetala and BA act at the GABAa- BZD receptor in vivo. The effect of S. sympetala in stressed animals, specifically its cortisol-lowering ability was investigated in vitro and in vivo in rainbow trout. Both leaf extract and BA significantly lowered cortisol in response to an adrenocorticotropic hormone (ACTH) challenge in vitro and a standardized net restraint assay in vivo. The anxiety-reducing effect of P. amalago was examined and the bioactive principle identified by bioassay-guided fractionation. P. amalago extract significantly reduced anxiety-like behaviour in rats and demonstrated affinity for the GABAa-BZD receptor in vitro. The bioactive molecule was determined to be a furofuran lignan. Together these results provide a pharmacological basis for the traditional use of S. sympetala and P. amalago to treat anxiety and elucidate their mode of action and active principles. S. sympetala is now thoroughly characterized and represents an excellent candidate plant for development as a natural health product.