Made available in DSpace on 2015-05-14T12:59:42Z (GMT). No. of bitstreams: 1 ArquivoTotal.pdf: 2781161 bytes, checksum: 6e4a880e963d8266a3616bed552926f8 (MD5) Previous issue date: 2012-12-07 / Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPES / Aerial parts of Hyptis suaveolens (Lamiaceae), known as alfazema-brava , tapera-velha , erva-canudo , cheirosa and alfavacão , is used in traditional medicine to treat stomach ailments, inflammations and infections. The aim of this study was to evaluate the gastroprotection, wound healing and toxicity of Hyptis suaveolens, with a view to validate its efficacy, safety as well as to corroborate existing data. To this end, behavioral evaluation and acute toxicity study of the ethanol extract (EEtOH-Hs) and hexane fraction (FaHex-Hs) at a single dose of 2.000 mg/kg (p.o) was performed in mice. Pharmacological effects, in particular, the gastroprotective activities of EEtOH-Hs and FaHex-Hs were evaluated. Initial pharmacological screening was conducted with EEtOH-H, Hs-FaHex, dichloromethanic fraction (FaDCM-Hs) and ethyl acetate fraction (FaAE-Hs) against acidified ethanol-induced gastric ulcers. Acute gastric ulcers induced by ethanol, NSAIDs, immobilization and cold stress, at the were carried out at doses of 62.5, 125, 250 and 500 mg / kg (po), and at 250 mg/kg (id) in gastric juice containment by pylorus ligature and ischemia-reperfusion. To evaluate ulcer healing property of EEtOH-Hs and FaHex-Hs, acetic acid-induced ulcers experiment was realized. In addition the toxicity of EEtOH-Hs and FaHex-Hs by repeated dosing for 14 days was also assessed using acetic acid ulcer model. The antimicrobial effect against Helicobacter pylori bacterium was investigated by agar diffusion method. Gastric juice parameters were evaluated in the pylorus ligature assay. Next, was investigated participation of mucus, sulfhydryl groups and nitric oxide (NO) in the gastroprotection and determine endogenous antioxidants parameters through the levels of lipid peroxidation (LPO) and superoxide dismutase (SOD) activity in gastric mucosa following ulcers induction by ischemia-reperfusion. Oral administration of EEtOH-Hs caused hyperactivity in the animals. However, it caused no death to none of the animals. Thus it was not possible to determine LD 50. In this assay, no sign of toxicity was evidenced in animals treated with FaHex-Hs. In pharmacological screening, EEtOH-Hs, as well as all fractions studied (FaHex-Hs, FaDCM-Hs, FaAE-Hs) caused significant inhibitions of the ulcerative lesion index (ULI) in the acidified ethanol ulcer model, being that FaHex-Hs was the most effective. EEtOH-Hs and FaHex-Hs, significantly reduced ULI in all models tested. EEtOH-Hs and FaHex-Hs exhibited healing properties in the acetic acid model of ulcers. EEtOH-Hs and FaHex-Hs had no effect on the gastric juice parameters and left unaltered the levels of mucus of the gastric mucosa. However changes were observed in the ulcerative lesion area (U.L.A) with the use of sulfhydryl groups blocker, inhibition of lipid peroxidation and increased SOD activity in the gastric mucosa. Therefore, the antiulcerogenic effect of EEtOH-Hs and FaHex-Hs may involve antioxidant and cytoprotective mechanisms. / Partes aéreas de Hyptis suaveolens (Lamiaceae), conhecida como alfazema-brava e tapera-velha , são utilizadas na medicina tradicional no tratamento de problemas gástricos, inflamações e infecções. Estudos farmacológicos realizados com esta espécie e evidenciaram as atividades antinociceptiva, cicatrizante, anti-inflamatória e antioxidante. O objetivo deste estudo foi realizar ensaios farmacológicos relacionados à gastroproteção, cicatrização e toxicidade de Hyptis suaveolens, na perspectiva de validar a sua eficácia e segurança e corroborar aos dados já existentes. Para isto, foi realizada uma triagem comportamental e ensaio da toxicidade aguda do extrato etanólico-EEtOH-Hs e fase hexânica-FaHex-Hs (2.000 mg/kg). Foi realizada uma triagem farmacológica utilizando o EEtOH-Hs, FaHex-Hs, fase diclorometânica-FaDCM-Hs e fase acetato de etila-FaAE-Hs pelo modelo de indução de úlceras gástricas por etanol acidificado. Foram realizados ensaios de indução de úlceras agudas pelo etanol, AINES, estresse por imobilização e frio (62,5, 125, 250 e 500 mg/kg), contensão do suco gástrico por ligadura do piloro e isquemia-reperfusão (250 mg/kg). Para avaliar a propriedade cicatrizante do EEtOH-Hs e FaHex-Hs, foi realizado o ensaio de indução de úlceras por ácido acético e avaliação da toxicidade do EEtOH-Hs e FaHex-Hs por doses repetidas durante 14 dias nesse modelo. Realizou-se a investigação do efeito contra a bactéria Helicobacter pylori pelo método de difusão em ágar. Os parâmetros do suco gástrico foram avaliados no ensaio de ligadura do piloro. Foram investigadas as participações do muco, grupamentos sulfidrilas e NO na gastroproteção do EEtOH-Hs e FaHex-Hs. Foram determinados os parâmetros antioxidantes pela determinação dos níveis de lipoperoxidação (LPO) e atividade da enzima superóxido dismutase (SOD) na mucosa gástrica, utilizando o modelo de isquemia-reperfusão. A administração do EEtOH-Hs, provocou hiperatividade nos animais, entretanto, não causou morte nos animais, não tendo sido possível determinar a DL 50. Nenhum sinal de toxicidade foi evidenciado nos animais tratados com a FaHex-Hs. O EEtOH-Hs, bem como todas as fases testadas promoveram inibição significativa do índice de lesão ulcerativa-ILU no modelo de indução por etanol acidificado, sendo que a FaHex-Hs foi a mais eficaz. O EEtOH-Hs e a FaHex-Hs, reduziram significativamente o ILU nos modelos de úlceras gástricas induzidas por todos os agentes lesivos. O EEtOH-Hs e a FaHex-Hs não alteraram os parâmetros do suco gástrico e os níveis de muco gástrico, entretanto, foram observadas alterações na área de lesão ulcerativa-ALU mediante a utilização do bloqueador de grupamentos sulfidrilas, indicando sua participação na atividade gastroprotetora. Foi observada inibição da peroxidação lipídica e aumento da atividade da enzima SOD da mucosa gástrica. Portanto, o efeito gatroprotetor do EEtOH-Hs e da FaHex-Hs pode envolver mecanismos antioxidantes e citoprotetores.

Submitted by Rafael Santana (rafael.silvasantana@ufpe.br) on 2017-06-09T18:33:27Z No. of bitstreams: 2 license_rdf: 811 bytes, checksum: e39d27027a6cc9cb039ad269a5db8e34 (MD5) Tese Bárbara Laine Ribeiro da Silva.pdf: 2635614 bytes, checksum: 8384212e8db84a27bc2b1fd6a579e7ad (MD5) / Made available in DSpace on 2017-06-09T18:33:27Z (GMT). No. of bitstreams: 2 license_rdf: 811 bytes, checksum: e39d27027a6cc9cb039ad269a5db8e34 (MD5) Tese Bárbara Laine Ribeiro da Silva.pdf: 2635614 bytes, checksum: 8384212e8db84a27bc2b1fd6a579e7ad (MD5) Previous issue date: 2016-04-01 / CAPES / Em ambientes com clima semiárido, a sobrevivência das plantas depende da adaptação de características morfológicas, anatômicas e fisiológicas. O hábito das espécies e a estrutura do ambiente no qual a planta está inserida também determina sua sobrevivência em ambientes com condições ambientais limitantes, como a caatinga. No caso das espécies herbáceas, é necessário descobrir qual a principal limitação ambiental para o seu desenvolvimento, já que a maioria delas possui ciclo de vida restrito ao período de chuvas na região, bem como quais são as características desenvolvidas que permitem sua sobrevivência no ambiente. O trabalho avaliou características fisiológicas, anatômicas e morfológicas de três espécies herbáceas (Hyptis suaveolens L., Stachytarpheta sanguinea Mart. ex Schauer e Jacquemontia evolvuloides (Moric.) Meisn., em áreas de caatinga com 22, 44 e mais de 60 anos de regeneração, na Paraíba. Foram analisadas: área foliar; área foliar específica; espessura das epidermes, das cutículas, dos parênquimas e do mesofilo; densidade estomática e de tricomas; concentrações de clorofila a, clorofila b e carotenoides; potencial hídrico foliar, trocas gasosas, concentrações de compostos fenólicos totais, nitrogênio, potássio e fósforo. As três espécies apresentaram características anatômicas de folhas de sol, com estômatos e tricomas em ambas as faces foliares e maior concentração na face abaxial. J. evolvuloides apresentou mais características de locais ensolarados, com a menor área foliar específica na área em regeneração mais recente, maior espessura de epiderme e parênquima isobilateral. Algumas variações morfoanatômicas entre as áreas foram comuns entre as três espécies, como as maiores espessuras dos mesofilos e dos parênquimas na caatinga mais antiga que nas áreas com 22 e 44 anos em regeneração. No geral, H. suavoelens e S. sanguinea foram espécies mais plásticas que J. evolvuloides, com as maiores diferenças morfofisiológicas entre as áreas. J. evolvuloides demonstrou ser mais adaptada à baixa disponibilidade hídrica e à alta incidência luminosa. / In environments with semi-arid climate, the survival of plants depends on the adaptation of morphological, anatomical and physiological characteristics. The habit of the species and environmental structure in which the plant is inserted, also determines their survival in environments with limiting environmental conditions, such as the caatinga. In the case of herbaceous species, it is necessary to find out what is the main environmental limitations for its development, since most they have a life cycle restricted to the rainy season in the region, and what are the features developed to survival in the environment. This work determined the physiological, anatomical and morphological characteristics of three herbaceous species (Hyptis suaveolens L. Stachytarpheta sanguinea Mart. Ex Schauer and Jacquemontia evolvuloides (Moric.) Meisn., in areas of caatinga with 22, 44 and over 60 years of regeneration, in Paraiba state. Were analyzed the leaf area, specific leaf area, thickness of the epidermis, cuticle, parenchyma and mesophyll, the stomata and trichomes densities; concentrations of chlorophyll a, chlorophyll b and carotenoids, the leaf water potential, gas exchange, concentrations of total phenolic compounds, nitrogen, potassium and phosphorus. The three species have anatomical features of sun leaves with stomata and trichomes in both leaf surfaces and a greater concentration on the abaxial surface. J. evolvuloides showed more characteristics of sunny locations, with lowest specific leaf area in the most recent regeneration area, thickest epidermis and isobilateral parenchyma. Some morphoanatomical variations between the areas were common among the three species, such as the greater thicknesses of mesophyll and parenchyma in the oldest caatinga than in the areas with 22 and 44 years in regeneration. Overall, H. suavoelens and S. sanguinea were more plastic species than J. evolvuloides, with the largest morphophysiological differences between areas. J. evolvuloides proved to be more acclimatized to low water availability and high light incidence.

Petroleum ether, dichloromethane, and 80% ethanol extracts of 15 plant species collected in Nigeria were screened for in vitro antibacterial, anti-inflammatory and antimalarial activities. Antibacterial activity was tested using the agar diffusion method, while the minimum inhibitory concentrations (MIC) of the active extracts were determined using the microtitre serial dilution method. Most antibacterial activity detected was against Gram-positive bacteria with Staphylococcus aureus being the most susceptible. The highest activity was found in petroleum ether and dichloromethane leaf extracts of Mallotus oppositifolius; petroleum ether, dichloromethane and ethanolic root extracts of Newbouldia laevis; and ethanolic root extracts of Morinda lucida and Canthium subcordatum. Against the Gram-negative bacterium Escherichia coli, the highest activity was found in dichloromethane leaf extracts of Newbouldia laevis, ethanolic root extracts of Phyllanthus amarus, Mallotus oppositifolius, and Canthium subcordatum. A total of 60 plant extracts were screened for antiplasmodial activity. A chloroquine sensitive strain of Plasmodium falciparum (D10) was used. In the assay, the parasite lactate dehydrogenase (pLDH) activity was used to measure parasite viability. About 11 extracts showed promising activity with an IC₅₀ ranging from 2.5 to 13.4 µg/ml. The petroleum ether leaf extract of Hyptis suaveolens had the highest activity (IC₅₀ = 2.5 µg/ml). The cyclooxygenase (COX-1 and COX-2) assays were used to test for anti-inflammatory activity. All the plant species, with the exception of Hedranthera barteri and Picralima nitida showed anti-inflammatory activity. Apart for a few ethanolic extracts, all the activities were recorded with petroleum ether and dichloromethane extracts. Employing bioassay-guided activity fractionation, an antibacterial anthraquinone identified as emodin was isolated from ethanolic root extract of Senna occidentalis. Although this compound had been isolated from other sources, this was the first report of isolation from Senna occidentalis. Using a similar approach a novel antimalarial diterpenoid was isolated from the petroleum ether leaves extract of Hyptis suaveolens. It had IC₅₀ of 0.1 µg/ml. This new compound is worthy of further investigation and may act as an important lead compound for future antimalarial drugs. / Thesis (Ph.D.)-University of KwaZulu-Natal, 2005.