Submitted by Jorge Silva (jorgelmsilva@ufrrj.br) on 2017-08-31T19:17:42Z No. of bitstreams: 1 2016 - Francine Fran?a Monken.pdf: 2589456 bytes, checksum: 06c9e0d64d97d48b268dfd24bee047a6 (MD5) / Made available in DSpace on 2017-08-31T19:17:42Z (GMT). No. of bitstreams: 1 2016 - Francine Fran?a Monken.pdf: 2589456 bytes, checksum: 06c9e0d64d97d48b268dfd24bee047a6 (MD5) Previous issue date: 2016-09-30 / CAPES / This study aimed determinate the chemical composition of raw secretions expelled by two species of Aparasphenodon genus from compounds isolation, purification and structural identification. For this, individuals of A. brunoi (n=5) e A. arapapa (n=3) were collected in Ilha da Marambaia, municipality of Mangaratiba (RJ), and in municipality of Ilh?us (BA), respectively. The secretions were obtained by smooth electric stimulus and were translucent and little viscous, with approximated yield of 4 mg of sample/individual. For each species, was realized chromatography of thin layer, the revelator reagent ninhydrin indicated presence of amine groups after violet color appearing. Samples than were submitted with the same retention time (0.88 and 1.44 min) in both analysis, indicating presence of similar compounds in both species. In same way, samples purification realized by semi preparative liquid chromatography of high efficiency presented the same fractions number for both species. The structural determination was made by LC-MS/MS only for A. brunoi and reveled high collagen incidence and other uncharacterized proteins. Biological assays were realized in concentrations of 1?g.mL-1 and 10?g.mL-1 for both species. The assay of cellular viability did not present survival reduction of yeast, such as dosing of lipid peroxidation that did not show reaction with malonaldehyde in all tested cases. In other hand, the assay of mitochondrial damage reveled toxicity in concentration of 10 ?g.mL-1, reducing for discreet form the cellular viability in both samples. We conclude that both species have proteins as the main compound and, in a cellular level, are not harmful in 1 ?g.mL-1, but can promote damage in 10 ?g.mL-1. Besides that, as reveled profiles to both extracts, both chemical and biological assays were very close, the existence of a pattern in chemical composition of cutaneous secretions in amphibians of the same genus can be reinforced, even that species be in distinct environmental conditions. / O presente estudo buscou determinar a composi??o qu?mica das secre??es brutas expelidas por duas esp?cies de Aparasphenodon, a partir do isolamento, purifica??o e identifica??o estrutural destes compostos. Para tal, indiv?duos de A.brunoi (n=5) e A.arapapa (n=3) foram coletados na Ilha da Marambaia, Mangaratiba (RJ) e no munic?pio de Ilh?us (BA), respectivamente. As secre??es foram obtidas por est?mulo el?trico suave e mostraram-se translucidas e pouco viscosas, com rendimento aproximado de 4 mg de amostra/indiv?duo. Para cada esp?cie, foi realizada cromatografia em camada delgada; o reagente revelador ninidrina indicou presen?a de grupos am?nicos ap?s aparecimento da cor violeta. As amostras foram ent?o submetidas ? cromatografia liquida de alta efici?ncia anal?tica, sendo detectados dois picos majorit?rios com mesmo tempo de reten??o (0,88 e 1,44 min) em ambas as an?lises, indicando assim a presen?a de compostos semelhantes nas duas esp?cies. Da mesma forma, a purifica??o das amostras realizada por cromatografia liquida de alta efici?ncia semi-preparativa apresentou o mesmo n?mero de fra??es para ambas as esp?cies. A determina??o estrutural foi determinada por LC-MS/MS apenas para A. brunoi e revelou alta incid?ncia de col?geno e outras prote?nas n?o caracterizadas. Os ensaios biol?gicos foram realizados nas concentra??es de 1 ?g.mL-1 e 10 ?g.mL-1 para ambas as esp?cies. O ensaio de viabilidade celular n?o apresentou redu??o da sobreviv?ncia das leveduras, assim como a dosagem de peroxida??o lip?dica n?o mostrou rea??o com malonalde?do, em todos os casos testados. Por outro lado, o ensaio de dano mitocondrial revelou toxicidade na concentra??o de 10 ?g.mL-1, reduzindo de forma discreta a viabilidade celular, em ambas as amostras. Conclu?mos ent?o que as duas esp?cies possuem prote?nas como seu principal componente e, a n?vel celular, n?o s?o nocivas em 1 ?g.mL-1, mas podem promover danos quando em 10 ?g.mL-1. Al?m disso, como os perfis revelados para ambos os extratos, tanto nos ensaios qu?micos como nos biol?gicos, foram muito pr?ximos, a exist?ncia de um padr?o na composi??o qu?mica das secre??es cut?neas em anf?bios de um mesmo g?nero pode ser refor?ada, ainda que as esp?cies se encontrem em condi??es ambientais distintas.

Submitted by Sandra Pereira (srpereira@ufrrj.br) on 2017-10-05T11:53:08Z No. of bitstreams: 1 2009 - Leticia Silotti Zampirolli.pdf: 25893124 bytes, checksum: bd44115917dd331e511dc65cd22738a1 (MD5) / Made available in DSpace on 2017-10-05T11:53:08Z (GMT). No. of bitstreams: 1 2009 - Leticia Silotti Zampirolli.pdf: 25893124 bytes, checksum: bd44115917dd331e511dc65cd22738a1 (MD5) Previous issue date: 2009-05-27 / Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior, CAPES, Brasil. / A series of new dialkylphosphorylhydrazones (phosphorohydrazidic acid, N?-[1,2-dihydro-2- oxo-(R1)-3H-indole-3-iliden]- dialkyl esters was synthesized and characterized by IR, 1H, 13C and 31P NMR and mass spectroscopy. These dialkylphosphorylhydrazones were synthesized in three steps. The first step involved the synthesis of different dialkylphosphites which are obtained by the reaction of PCl3 with three mols of the corresponding alcohols. The second step consisted of the reaction between the dialkylphosphites and hydrazine in a two phase system, leading to the formation of the dialkylphosphorylhydrazines. Finally, the last step was the condensation of these dialkylphosphorylhydrazines with different N-substituted isatins. The analysis of the 1H, 13C and 31P NMR spectra showed the existence of the two possible diastereoisomers E and Z for compounds 1, 2, 6, 10 and 12, while for the remaining compounds only the Z isomer is present. Ten of these compounds were preliminarily tested for their inhibition potential against two protozoa (Trypanosoma cruzi and Leishmania amazonensis). All compounds tested showed cell proliferation inhibition of 98% at 50 ?M for Leishmania amazonensis, whereas for T. cruzi, inhibition of epimastigote cell proliferation was found to be higher than 75% for all compounds tested except 6, which showed a 59% inhibition. These ten compounds were also evaluated against Plasmodium falciparum, affording inhibitions higher than 90% for a 1mM concentration. These compounds were also investigated for their fungicidal activity against phytopatogenic Rhizoctonia solani and Fusarium oxysporum. Compounds 9 and 11 showed a miscelial growth inhibition of 58% for Rhizoctonia solani while compound 12 afforde a 72% inhibition. Compounds 1, 2, 11 and 12 gave Fusarium oxysporum inhibition higher than 52%. Finally, the compounds synthesized were also evaluated for their inhibitory potential against lettuce seed germination and it was observed that the same compounds which showed fungicidal activity were not able to inhibit seed germination. / Uma s?rie de 16 dialquilfosforilidrazonas (?cido fosforoidraz?dico, N? -[1,2-diidro-2-oxo-(R1)- 3H- indol-3-ilideno] -, ?ster de dialquila), sendo todas in?ditas, foram sintetizadas e caracterizadas pelas t?cnicas de espectrometria de IV, RMN de 1H, RMN de 13C, RMN de 31P e massas. As novas dialquilfosforilidrazonas foram sintetizadas em tr?s etapas de rea??o. A primeira etapa consistiu na s?ntese de diferentes fosfitos de dialquila que foram obtidos atrav?s da rea??o do tricloreto de f?sforo (PCl3) com tr?s mols do ?lcool correspondente. Na segunda etapa, a rea??o dos fosfitos de dialquila com a hidrazina, em um sistema bif?sico, levou ? forma??o das dialquilfosforilidrazinas. A ?ltima etapa foi a condensa??o destas dialquilfosforilidrazinas com diferentes isatinas substitu?das. A an?lise dos espectros de RMN de 1H, RMN de 13C, RMN de 31P das dialquilfosforilidrazonas mostraram a coexist?ncia dos dois poss?veis diastereois?meros E e Z, para os compostos 1, 2, 6, 10 e 12, enquanto que para os compostos restantes observou-se apenas o diastereois?mero Z. Dos compostos sintetizados, dez foram avaliados preliminarmente quanto ao potencial inibit?rio de prolifera??o de dois protozo?rios (Trypanosoma cruzi e Leishmania amazonensis). Para Leishmania amazonensis todos os compostos testados apresentaram inibi??o da prolifera??o celular de 98 % a 50 ?M. Enquanto que para T.cruzi verificou-se inibi??o da prolifera??o celular de epimastigotas superior a 75% para todos compostos testados, a exce??o do composto (6) cuja inibi??o foi de 59 %. Esses dez compostos tamb?m foram avaliados frente ao protozo?rio Plasmodium falciparum apresentando inibi??o superior a 90 % para todos os compostos testados, a uma concentra??o de 1mM. Essas dialquilfosforilidrazonas tamb?m tiveram a a??o fungicida avaliada frente aos fungos fitopatog?nicos (Rhizoctonia solani e Fusarium oxysporum). Em Rhizoctonia solani os compostos (9) e (11) apresentaram inibi??o do crescimento miscelial de 58 %, j? o composto (12) apresentou inibi??o de 72%. Para o Fusarium oxysporum destacaram-se os compostos (1, 2, 11 e 12) com inibi??o superior a 52 %. Esses compostos tamb?m foram avaliados quanto ao potencial inibit?rio de germina??o em sementes de alface e verificouse que os mesmos compostos que apresentaram efeitos fungist?ticos, n?o inibiram a germina??o de sementes de alface.

Submitted by Ricardo Cedraz Duque Moliterno (ricardo.moliterno@uefs.br) on 2016-09-27T22:26:12Z No. of bitstreams: 1 DISSERTA??O Val?ria Silva G?es.pdf: 1629398 bytes, checksum: 6e130737f6d57007b90ea3ae8de5042b (MD5) / Made available in DSpace on 2016-09-27T22:26:12Z (GMT). No. of bitstreams: 1 DISSERTA??O Val?ria Silva G?es.pdf: 1629398 bytes, checksum: 6e130737f6d57007b90ea3ae8de5042b (MD5) Previous issue date: 2015-03-31 / The Lamiaceae family has a great importance in the Brazilian semiarid region due to their species of pharmacological properties. Martianthus leucocephalus (Mart. Ex Benth.) JFB Pastore belongs to the Lamiaceae family and has had the antimicrobial activity of essential oil proven. However, this species lacks pharmacological studies that evaluate its biological potential. Thus, the aim of this study was to evaluate the effect on the central nervous system, the acute toxicity, as well as investigate the antinociceptive and anti-inflammatory of Martianthus leucocephalus extract. The possible mechanism of action of species was also studied. The experiments were performed in the Chemistry Laboratory of Bioactive Natural Products and in the Laboratory of Pharmacology at the State University of Feira de Santana. The effect on the central nervous system was evaluated through Behavioral Pharmacological Screening by Rota Rod test. The acute toxicity was determined using the protocol Organization for Economic Cooperation and Development (OECD - 420/2001). The antinociceptive activity was investigated in the tests of acetic acid, formalin and hot plate. The mechanism of action was determined using the opioid antagonist naloxone in the hot plate model. The study of anti-inflammatory activity was performed using the paw edema induced by carrageenan tests and capillary permeability induced by acetic acid. The results were analyzed by analysis of variance (ANOVA). Martianthus leucocephalus showed no acute toxicity or muscle relaxant effects action on the motor system. The antinociceptive and anti-inflammatory properties were found significantly compared to the control group animals. / A fam?lia Lamiaceae tem uma grande import?ncia na regi?o do semi?rido brasileiro devido ?s suas esp?cies detentoras de propriedades farmacol?gicas. Martianthus leucocephalus (Mart. ex Benth.) J.F.B. Pastore pertence ? fam?lia Lamiaceae e j? teve a atividade antimicrobiana do seu ?leo essencial comprovada. No entanto, a referida esp?cie carece outros de estudos farmacol?gicos que avaliem seu potencial biol?gico. Diante disso, o objetivo desse trabalho foi avaliar o efeito sobre o sistema nervoso central, a toxidade aguda, bem como investigar as atividades antinociceptiva e anti-inflamat?ria de extratos de Martianthus leucocephalus proveniente de cultivo. O poss?vel mecanismo de a??o da esp?cie tamb?m foi estudado. Os experimentos foram realizados no Laborat?rio de Qu?mica de Produtos Naturais e Bioativos e no Laborat?rio de Farmacologia da Universidade Estadual de Feira de Santana. O efeito sobre o sistema nervoso central foi avaliado por meio da Triagem Farmacol?gica Comportamental e pelo teste do Rota Rod. A toxidade aguda foi averiguada utilizando o protocolo Organization for Economic Cooperation and Development (OECD ? 420/2001). A atividade antinociceptiva foi investigada nos testes do ?cido ac?tico, formalina e placa quente. O mecanismo de a??o foi apurado utilizando o antagonista opioide naloxona no modelo da placa quente. O estudo da atividade anti-inflamat?ria foi realizado utilizando os testes do edema de pata induzido por carragenina e da permeabilidade capilar induzida por ?cido ac?tico. Os resultados obtidos foram analisados atrav?s da an?lise de vari?ncia (ANOVA). Martianthus leucocephalus n?o mostrou toxidade aguda nem a??o miorrelaxante sobre o sistema motor. As propriedades antinociceptiva e anti-inflamat?ria foram evidenciadas de forma significativa em rela??o aos animais do grupo controle.

Made available in DSpace on 2014-12-17T14:03:27Z (GMT). No. of bitstreams: 1 CarlosEMG.pdf: 434119 bytes, checksum: cffd1dddf77ec049b23dadc1bfa89773 (MD5) Previous issue date: 2004-12-20 / Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior / A proteinaceous trypsin inhibitor was purified from Crotalaria pallida seeds by ammonium sulphate fractionation, affinity chromatography on immobilized Trypsin-Sepharose and TCA precipitation. The trypsin inhibitor, named ITC, had Mr of 32.5 kDa by SDS-PAGE and was composed by two subunits with 27.7 and 5.6 kDa linked by disulphide bridges, a typical characteristic of Kunitz-Inhibitor family. ITC was stable until 50?C, and at 100?C its residual activity was of about 60%. Also, ITC was stable at pHs 2 to 12. The inhibition of trypsin by ITC was non-competitive, with a Ki of 8,8 x 10-7M. ITC inhibits weakly other serine proteinases such as chymotrypsin and elastase. The inhibition of papain (44% of inhibition), a cysteine proteinase was an indicative of the bi-functionality of ITC. In vitro assays against digestive proteinases from several Lepdoptera, Diptera and Coleoptera pests were made. ITC inhibited in 100% digestive enzymes of Ceratitis capitata (fruit fly), Spodoptera frugiperda and Alabama argillacea, the last one being a cotton pest. It also inhibited in 74.4% Callosobruchus maculatus (bean weevil) digestive enzymes, a Coleoptera pest. ITC, when added in artificial diet models, affected weakly the development of C. capitata larvae and it had a WD50 of 2.65% to C. maculatus larvae / Um inibidor de proteinase foi isolado de sementes de Crotalaria pallida por fracionamento com sulfato de am?nio, cromatografia de afinidade em Sepharose com tripsina acoplada e precipita??o com ?cido tricloroac?tico (TCA). O inibidor de tripsina, denominado ITC, possui massa molecular de 32,5 kDa determinada por SDS-PAGE e ? composto por duas subunidades, uma de 25,7 e outra de 5,6 kDa, ligadas por pontes dissulfeto; uma caracter?stica t?pica da fam?lia de inibidores de Kunitz. ITC foi est?vel at? 50?C e a 100?C sua atividade residual foi cerca de 60%. ITC tamb?m foi est?vel em valores de pHs variando de 2 a 12. A inibi??o da tripsina por ITC ? do tipo n?o-competitivo, com um Ki de 8,8 x 10-7M. ITC inibe fracamente outras proteinases ser?nicas como quimotripsina e elastase. A inibi??o da papa?na (44%), uma proteinase ciste?nica, foi indicativa da bifuncionalidade de ITC. Ensaios in vitro contra proteinases digestivas de v?rios insetos praga das ordens Lepidoptera, Diptera e Coleoptera foram realizados. ITC inibiu em cerca de 100% enzimas digestivas de Ceratitis capitata (mosca-das-frutas), Spodoptera frugiperda (lagarta do cartucho do algod?o), e Alabama argillacea (curuquer? do algod?o). ITC tamb?m inibiu em 74,4% enzimas digestivas de Callosobruchus maculatus (broca do feij?o) uma praga da ordem Coleoptera. ITC, quando adicionado a dietas artificiais, afetou fracamente o desenvolvimento de larvas de C. capitata e teve um WD50 de 2,65% contra larvas de C. maculatus

Submitted by Ricardo Cedraz Duque Moliterno (ricardo.moliterno@uefs.br) on 2016-06-14T22:02:36Z No. of bitstreams: 1 63-lais-cardoso-dissertacao-completa-07-08-2014.pdf: 1594778 bytes, checksum: 095a7789d1a934007d9907b518ed7989 (MD5) / Made available in DSpace on 2016-06-14T22:02:36Z (GMT). No. of bitstreams: 1 63-lais-cardoso-dissertacao-completa-07-08-2014.pdf: 1594778 bytes, checksum: 095a7789d1a934007d9907b518ed7989 (MD5) Previous issue date: 2014-08-07 / Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior - CAPES / The species was selected to carry out the research because of the wide medicinal use for diarrhea treatment by the Brazilian northeast population. The objective of this work was to study the morphological and anatomical aspects of the leaves of Stachytarpheta jamaicensis, detect the presence of the major classes of secondary metabolites present in the crude extract of the leaves and still assessing the potential antioxidant, cytotoxic and antibacterial said extract and its fractions. To achieve the objectives, paradermic sections and cross were made to study the epidermis and its annexes. Was also analyzed characters of leaf morphology and petiole through histological sections. Phytochemical screening of crude extracts was performed by colorimetric tests and tests precipitation. From the raw methanol extract was held partitions with increasing polarity solvents (hexane, chloroform and ethyl acetate). The fractionation and purification of the partitioned extracts was performed by column chromatography (CC) and monitored by thin layer chromatography (TLC). The crude extract (EB), and fractions were subjected to test the free radical sequestration 1,1 - diphenyl-2-picrylhydrazyl (DPPH) test and the mortality of Artemia salina, to assess antioxidant activities and cytotoxic activities, respectively. To evaluate the antibacterial activity were performed the disk diffusion techniques in well and MIC (minimum inhibitory concentration) compared to the strains of Salmonella and E.coli. The blade is amphistomatic with stomata of diac?tic type, the epidermis is uniseriate, with the presence of trichomes. The results detected the presence of tannins, flavonoids, alkaloids and saponins. In the evaluation of antioxidant activity, IC 50 values (mg / ml) were found 6.62 to 446.20 for the tested extracts. For cytotoxicity, all extracts showed LC50 values (mg / ml) 211.16 to 446.20, and the hexane extract the most active (LC50 211.16). For antibacterial analysis, has not been demonstrated activity of extracts front bacteria tested. The toxicity of the leaf of this species refers caution about their safety for use by the population. / A esp?cie foi selecionada para realiza??o da pesquisa devido ? ampla utiliza??o medicinal para tratamento de diarreia pela popula??o do nordeste brasileiro. O objetivo desse trabalho foi estudar os aspectos morfoan?tomicos das folhas de Stachytarpheta jamaicensis, detectar presen?a das principais classes de metab?litos secund?rios presentes no extrato bruto de suas folhas e ainda avalia??o do potencial antioxidante, citot?xico e antibacteriano do referido extrato e suas fra??es. Para alcan?ar os objetivos, sec??es parad?rmicas e transversais foram efetuadas para estudo da epiderme e seus anexos. Analisou-se tamb?m caracteres da morfologia foliar e do pec?olo atrav?s de cortes histol?gicos. Foi realizada triagem fitoqu?mica do extrato bruto atrav?s de testes colorim?tricos e ensaios de precipita??o. A partir do extrato bruto metan?lico, realizou-se parti??es com solventes de polaridade crescente (hexano, clorof?rmio e acetato de etila). O fracionamento e purifica??o dos extratos particionados foi realizado por cromatografia em coluna (CC) e monitorado por cromatografia em camada delgada (CCD). O Extrato Bruto (EB) e as frac?es foram submetidos ao teste do sequestro do radical livre 1,1 ? difenil-2-picrilhidrazil (DPPH) e ao ensaio de letalidade da Artemia salina, para avalia??o das atividades antioxidante e citot?xica, respectivamente. Para avalia??o da atividade antibacteriana foram executadas as t?cnicas de difus?o em disco, em po?o e MIC (concentra??o inibit?ria m?nima) frente ?s cepas de Samonella e E.coli. A l?mina foliar ? anfiestom?tica, com est?matos do tipo diac?tico, a epiderme ? uniestratificada, com presen?a de tricomas tectores. Os resultados detectaram presen?a de taninos, flavonoides, alcaloides e saponinas. Na avalia??o da atividade antioxidante, os valores de IC50 (mg/ml) encontrados foram de 6,62 a 446,20 para os extratos testados. Quanto ? citotoxicidade, todos os extratos apresentaram valores de LC50 (mg/ml) de 211,16 a 446,20, sendo o extrato hex?nico o mais ativo (LC50 211,16) . Quanto ? an?lise antibacteriana, n?o foi demonstrada atividade dos extratos frente as bact?rias testadas. A toxicidade apresentada pela folha dessa esp?cie remete cautela quanto ? sua seguran?a para uso pela popula??o.