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Diss. (sammanfattning) Stockholm : Karol inst., 2003. / Härtill 6 uppsatser.

Orientador: Antonio Olavo Cardoso Jorge / Banca: Luciane Dias de Oliveira / Banca: Cristiane Aparecida Pereira / Resumo: O número de espécies bacterianas resistentes aos antimicrobianos tem atingido níveis elevados. Com isso, torna-se necessária a realização de pesquisas que avaliem os efeitos de métodos terapêuticos alternativos. Os objetivos desse trabalho foram avaliar a citotoxicidade do extrato glicólico de Zingiber officinale em macrófagos de camundongos e queranócitos humanos, atividade antimicrobiana sobre biofilmes monotípicos (micro-organismos aeróbios: Candida albicans, Staphylococcus aureus, Streptococcus mutans, Pseudomonas aeruginosa, e anaeróbios: Porphyromonas gingivalis, Porphyromonas endodontalis, Prevotella intermedia) e biofilmes heterotípicos (associação: C. albicans e bactérias aeróbias). Para ação citotóxica, as células foram cultivadas em meio DMEM, semeadas (2 x 104 células/poço) na placa de 96 poços. Após aderência inicial, foi adicionado o extrato em diluição seriada (5 min e 24 h), e realizado o teste de MTT. Para avaliar a ação antimicrobiana, a Concentração Inibitória Mínina (CIM) e Concentração Microbicida Mínima (CMM) foram determinadas segundo as normas do CLSI. Para biofilmes, foram adicionados 100 µL meio de cultura e 100 µL suspensão microbiana (107 UFC/mL) em placas de 96 poços, nos heterotípicos foram utilizados 50 µL de cada micro-organismo. As placas foram incubadas (37ºC), por 48 h (aeróbios) ou por 7 dias (anaeróbios). Aplicou-se o extrato (5 min e 24 h), nas concentrações efetivas pré-determinadas (CMM) e duas superiores, depois os biofilmes foram desa... (Resumo completo, clicar acesso eletrônico abaixo) / Abstract: The number of bacterial species resistant to antimicrobials has reached high levels. Thus, it is necessary to perform research that evaluates the alternative therapeutic methods, such as ginger. The present study was to evaluate the cytotoxicity of the Zingiber officinale glycolic extract in human and mouse macrophages, antimicrobial activity on monotypic biofilms (aerobic microorganisms: Candida albicans, Staphylococcus aureus, Streptococcus mutans, Pseudomonas aeruginosa, and anaerobes: Porphyromonas gingivalis, Porphyromonas endodontalis, Prevotella intermedia) and heterotypic biofilms (association: C. albicans and aerobic bacteria). To cytotoxic action, the cells have been cultivated in DMEM medium, seeded (2x104 cells/well) in the 96-well plate. After initial adhesion, the extract has been added to serial dilution (5 min and 24 h), and the MTT tests were performed. In order to assess the antimicrobial action, Minimal Inhibitory Concentration (MIC) and Minimum Microbicidal Concentration (MMC) were determined in according to CLSI standards. In the biofilms case, 100 μL culture medium and 100 μL microbial suspension (107 CFU / mL) were added to 96-well plates, 50 μL of each microorganism was used in the heterotypics. The plates were incubated (37°C) for 48 h period (aerobic) or for 7 days (anaerobic). The extract (5 min and 24 h) was applied at the pre-determined effective concentrations (MMC) and two higher concentrations, after which the biofilms were disaggregated and se... (Complete abstract click electronic access below) / Mestre

A alveolite seca é uma das complicações pós-operatórias mais comuns e sintomáticas na exodontia, porém, até o momento não possui um protocolo de tratamento definido. A oxitetraciclina (OTC) é um antibiótico de amplo espectro utilizado no tratamento de múltiplas infecções. Entretanto, nos últimos anos as tetraciclinas de primeira geração, tais como a OTC, têm sido evitadas devido ao surgimento de microrganismos resistentes. Afortunadamente, nos últimos anos tem se observado uma tendência contrária graças às medidas de controle no uso de antibióticos. Sistemas de liberação controlada podem evitar o desenvolvimento de resistência bacteriana e diminuir o risco de efeitos adversos. Este estudo teve como objetivo preparar uma nanofibra polimérica de policaprolactona e oxitetraciclina (PCL/OTC), e ainda avaliar suas propriedades físicas e biológicas in vitro e in vivo, visando seu futuro uso no tratamento da alveolite seca. As nanofibras poliméricas carregadas com OTC foram preparadas pelo sistema de eletrofiação, caracterizadas através da microscopia eletrônica de varredura (MEV) e avaliadas sobre seu perfil de liberação do fármaco. A atividade antibacteriana da nanofibra sobre um biofilme misto de Porphyromonas gingivalis, Prevotella intermédia, Fusobacterium nucleatum, Eikenella corrodens, Streptococcus sanguis e Aggregatibacter actinomycetemcomitans foi analisada mediante a contagem das unidades formadoras de colônias viáveis após os tempos de contato de 1, 4, 24, 30 e 48 h. O processo de reparo alveolar induzido pela nanofibra PCL/OTC foi avaliado de forma histomorfológica e histomorfométrica após o tratamento da alveolite seca em molares de ratos, e comparado ao tratamento com nanofibras de PCL pura e Alvogyl®, 7, 14 e 21 dias após a exodontia. Finalmente, foi realizada a identificação e contagem de osteoclastos através da marcação da fosfatase ácida resistente ao tartarato (TRAP), nos mesmos tempos de avaliação. As nanofibras PCL/OTC apresentaram orientação randômica em camadas e morfologia multiforme. O perfil de liberação do sistema apresentou um efeito de explosão nas primeiras 8 horas, seguido por um período de liberação lenta e prolongada da OTC. A nanofibra PCL/OTC (132 ?g de OTC/mL) reduziu mais de 50% das colônias do biofilme nas primeiras horas de liberação, seguido por um período de manutenção em que a porcentagem de colônias bacterianas permaneceu baixa. O grupo tratado com PCL/OTC apresentou a maior porcentagem de tecido conjuntivo no 7º dia (p<0,05) e maior porcentagem de osso neoformado no 14º e 21º dias após a exodontia (p<0,05), em comparação aos outros grupos. O tratamento de alveolite seca com a fibra PCL/OTC permitiu a regeneração tecidual do alvéolo quase em sua totalidade até o 21º dia, sendo que a cronologia de regeneração tecidual com este material foi mais rápida do que com a fibra de PCL pura, e esta última mais rápida que do que o controle positivo Alvogyl®. O grupo PCL/OTC apresentou uma quantidade menor (p<0,05) de osteoclastos por área em relação aos outros grupos nos três tempos experimentais. O perfil de liberação prolongando de OTC e as propriedades biológicas relevantes apresentadas pela nanofibra PCL/OTC, sugerem que esta poderia ser considerada uma alternativa para o tratamento da alveolite seca. / Dry socket is one of the most common and symptomatic postoperative complications in tooth extraction, however, to date, it does not have an established treatment protocol. Oxytetracycline (OTC) is a broad-spectrum antibiotic, employed in the treatment of multiple infections. Nevertheless, in the last few years, first-generation tetracyclines such as OTC, have been avoided due to the development of resistant microorganisms. Fortunately, in recent years there has been a contrary trend thanks to control measures in the use of antibiotics. Controlled release systems can prevent the development of bacterial resistance and decrease the risk of adverse effects. This study aimed to prepare a polymeric nanofiber of polycaprolactone and oxytetracycline (PCL/OTC), and to evaluate its physical and biological properties in vitro and in vivo, aiming its use in the treatment of dry socket at the future. The OTC-charged polymeric nanofibers were prepared by electrospinning, and characterized by scanning electron microscopy (SEM) and drug release profile evaluation. The antibacterial activity of the nanofiber over a mixed biofilm containing Porphyromonas gingivalis, Prevotella intermedia, Fusobacterium nucleatum, Eikenella corrodens, Streptococcus sanguis, and Aggregatibacter actinomycetemcomitans was analyzed by counting the viable colony-forming units after 1, 4, 24, 30 and 48 h of contact. The alveolar repair process induced by the PCL/OTC nanofiber was evaluated histomorphologically and histomorphometrically after the treatment of dry socket in rat molars, and compared to the treatment with plain PCL nanofibers and AlvogylTM, 7, 14 and 21 days after extraction. Finally, the identification and counting of osteoclasts were performed through the tartrate resistant acid phosphatase (TRAP) staining, at the same evaluation time points. PCL/OTC nanofibers presented random orientation in layers and multiform morphology. The release profile of the PCL/OTC system showed a burst effect within the first 8 hours, followed by a prolonged slow release period. The PCL/OTC nanofiber at a concentration of 132 ?g OTC/mL reduced more than 50% of the biofilm colonies in the first few hours of release, followed by a maintenance period in which the percentage of bacterial colonies remained low. The PCL/OTC group presented the highest percentage of connective tissue on the 7th day (p<0.05), and of newly formed bone on the 14th and 21st days (p<0.05) after dental extraction, compared to the other groups. The treatment of dry socket with the PCL/OTC fiber allowed almost complete tissue regeneration up to the 21st day, and the chronology of tissue regeneration with this material was faster than with the plain PCL fiber, and the latter was more rapid than the positive control AlvogylTM. The PCL/OTC group presented a lower amount (p<0.05) of osteoclasts per area than the other two groups in the three experimental periods. The prolonged release profile of OTC and the relevant biological properties presented by the PCL/OTC nanofibers suggest that these may be considered as an alternative treatment of dry socket.

Introdução: Feridas neoplásicas malignas (FNM) são resultantes da invasão direta do câncer na pele que, ao se exteriorizarem, adquirem características de ferida. Com incidência variando de 0,6 a 9,0%, são mais comuns nos cânceres de mama e cabeça e pescoço. Dentre os sinais e sintomas, destaca-se o odor que tem sido descrito como intolerável e nauseante, acarretando impacto negativo sobre o paciente, familiares e equipe de saúde. O odor em FNM ocorre em consequência da interação das microbiotas aeróbica e anaeróbica que colonizam e infectam as feridas. Objetivando reduzir a carga microbiana local e, assim, controlar o odor, tem-se descrito o uso de antissépticos e antibióticos tópicos, dentre os quais destaca-se o metronidazol. Objetivo: Identificar as evidências científicas sobre a utilização do metronidazol para controle do odor em FNM, por meio de revisão sistemática (RS) de ensaios clínicos controlados e não controlados. Método: A partir da questão norteadora do estudo: Qual a eficácia da terapia tópica de metronidazol para o controle do odor em feridas neoplásicas malignas?, realizou-se a busca dos artigos nas bases de dados BIREME, LILACS, COCHRANE, CINAHL e EMBASE, com auxílio da estratégia PICO, utilizando-se descritores indexados e não indexados. Os estudos foram selecionados por duas pesquisadoras de forma independente e os estudos incluídos na RS foram analisados segundo o enunciado CONSORT, grau de recomendação e nível de evidência. Para o estudo randomizado utilizou-se também a Escala de Jadad. Resultados: Recuperaram-se 384 artigos, sendo selecionados 14 para leitura na íntegra, sendo incluídos, ao final, apenas três estudos na RS. Destes, um estudo é randomizado (grau de evidência e recomendação = 2b, Jadad = 2) e dois não são controlados (grau de evidência 4 para ambos). Quanto ao método de avaliação e/ou classificação do odor, não se identificou um instrumento formal, sendo empregada apenas escala analógica de 0 a 10 ou presença/ausência de odor. O tempo necessário para o emprego da terapia tópica foi de 1 a 14 dias, com troca do curativo 1 ou 2 vezes ao dia; e a aplicação do metronidazol foi em gel de 0,75% a 0,8%. Os estudos não mencionaram ou descreveram reações adversas. Os estudos apresentam limitações e fragilidades metodológicas importantes, destacando-se as amostras reduzidas e a falta de descrição de aspectos como o cegamento e randomização no único estudo randomizado, além dos procedimentos empregados nos curativos, dentre outros. Conclusão: Apesar dos três estudos concluírem que o metronidazol tópico é eficaz no controle do odor em FNM, não há forte evidência científica para corroborar essa eficácia. / Introduction: Malignant wounds (MW) are the result of direct invasion of cancer in the skin that, when exteriorized, acquire characteristics of the wound. With an incidence ranging from 0.6 to 9.0%, are more common in breast and head and neck . Among the signs and symptoms, there is the odor that has been described as intolerable and sickening, causing negative impact on the patient, family and healthcare team. The MW odor occurs as a result of the interaction of aerobic and anaerobic bacteria that colonize and infect wounds. In order to reduce local microbial load and thus control the odor, there has been described the use of topical antiseptics and antibiotics, among which stands out metronidazole. Objective: To identify the scientific evidence on the use of metronidazole for odor control in MW, through systematic review (SR) of randomized controlled trials and uncontrolled. Method: From the main question of the study: \"What is the efficacy of topical metronidazole therapy for odor control in malignant neoplastic wounds,\" there was the search for articles in the databases MEDLINE, LILACS, Cochrane Library, CINAHL database and EMBASE, using the PICO strategy, using descriptors indexed and unindexed. Studies were selected by two researchers independently and studies included in the RS were analyzed according to the CONSORT statement, strength of recommendation and level of evidence. For the randomized study also used the Jadad Scale. Results: 384 articles were recovered, 14 were selected for full reading, being included in the end, only three studies in SR. Of these, a study is randomized (level of evidence and recommendation= 2b, Jadad= 2) and two are not controlled (evidence grade 4 for both). As to the method of assessment and / or classification of odor, did not identify a formal instrument, being used only analog scale of 0 to 10, or the presence / absence of odor. The time required for the use of topical therapy was 1 to 14 days, with change of the dressing 1 or 2 times a day, and the application of metronidazole was 0.75% gel 0.8%. Studies have not mentioned or described adverse reactions. The studies have important methodological limitations and weaknesses, highlighting the small sample size and lack of description of aspects such as blinding and randomization in the only randomized, besides the procedures used in dressings, among others. Conclusion: Although the three studies conclude that topical metronidazole is effective in controlling odor in MW, there is no strong scientific evidence to support its effectiveness

A following study on vancomycin demonstrated the differing pharmacokinetics during the course of a septic insult, day 2 pharmacokinetics differing from day 7. / An important study showed that some septic patients with "normal" serum creatinines can have very high creatinine clearances. It follows that drugs which are renally excreted will have high clearances and illustrates why many of the above patients had low serum levels of antibiotic, a reason why some ICU patients require different dosing to ward patients. / Due to the required fluid loading and inotropic use in septic patients, creatinine clearances and drug clearances are often raised. This results in low serum concentrations at the end of a standard dosing interval. / My beta-lactam antibiotic work has repeatedly demonstrated low serum levels at the end of the standard dosing interval. In view of beta-lactam time-dependent kill characteristics we designed a continuous infusion protocol which we validated in a follow-up paper. / The inflammatory response of infections involves endothelial damage and capillary permeability. With associated fluid shifts of severe sepsis and treatment thereof, the volume of distribution (Vd) of antibiotics that distribute into the extracellular space (aminoglycosides, glycopeptides) is high. Peak serum levels for these antibiotics are therefore lower than those found in non-critically ill and in normal volunteers. It is noteworthy that this change in Vd is not apparent with drugs that have good tissue penetration (e.g. ciprofloxacin). / This thesis is a compilation of 11 of my prospectively designed studies plus extracts from 5 published reviews, focusing on pharmacokinetic (PK) aspects of antibiotics in ICU patients, all published in internationally peer-reviewed journals. / Two large PK studies on ciprofloxacin (a drug that has excellent tissue penetration) designed to address possible PK differences over time, could not demonstrate this difference in adults nor in two groups of paediatric patients where differences in body water are significant. / Two papers investigated the pharmacokinetics of amicakin in adult and paediatric patients documenting the benefit of extended interval dosing. / We automatically assume that antibiotic prescribing data, collated from healthy volunteers and not so ill patients, can be transcribed into the Intensive Care Unit. This is not so. / Jeffrey Lipman. / "April 2005." / Source: Dissertation Abstracts International, Volume: 68-03, Section: B, page: 1548. / Thesis (M.D.)--Chinese University of Hong Kong, 2005. / Includes bibliographical references (p. 235-254). / Electronic reproduction. Hong Kong : Chinese University of Hong Kong, [2012] System requirements: Adobe Acrobat Reader. Available via World Wide Web. / Electronic reproduction. [Ann Arbor, MI] : ProQuest Information and Learning, [200-] System requirements: Adobe Acrobat Reader. Available via World Wide Web. / School code: 1307.

by Kok Dick Shun, Louis. / Thesis (M.Phil.)--Chinese University of Hong Kong, 1993. / Includes bibliographical references. / Acknowledgements --- p.I / Table of Contents --- p.II / Abbreviations --- p.V / Aim and Scope of This Dissertation --- p.IX / Abstract --- p.X / Chapter Chapter One： --- General Introduction --- p.1 / Chapter 1.1 --- An Overview of the Immune System --- p.2 / Chapter 1.1.1 --- Innate Immunity --- p.2 / Chapter 1.1.2 --- Adaptive Immunity --- p.3 / Chapter 1.1.2.1 --- Humoral antibody immune response --- p.4 / Chapter 1.1.2.2 --- Cell- mediated immune response --- p.5 / Chapter 1.2 --- Immunomodulation --- p.6 / Chapter 1.3 --- An overview of the Host-mediated response against tumours --- p.9 / Chapter 1.3.1 --- T and B lymphocytes --- p.9 / Chapter 1.3.2 --- M acrophages --- p.14 / Chapter 1.3.3 --- Natural killer cells --- p.17 / Chapter 1.3.4 --- Lymphokines-activated killer cells --- p.20 / Chapter 1.3.5 --- Tumour infiltrating lymphocytes --- p.22 / Chapter 1.3.6 --- Cytokines --- p.23 / Chapter 1.4 --- Carbohydrates as Potential Immunostimulating agents --- p.33 / Chapter 1.5 --- General Properties of Bupleuri radix (B.R.) --- p.35 / Chapter Chapter Two： --- Materials and Methods --- p.36 / Chapter 2.1 --- Materials --- p.37 / Chapter 2.1.1 --- Animals --- p.37 / Chapter 2.1.2 --- Bupleuri radix --- p.37 / Chapter 2.1.3 --- "Buffers, culture media and chemicals" --- p.37 / Chapter 2.1.4 --- Cell lines --- p.48 / Chapter 2.2 --- Methods --- p.49 / Chapter 2.2.1 --- Extraction and fractionation of Bupleuri radix --- p.49 / Chapter 2.2.2 --- Purification of Bupleuri radix --- p.54 / Chapter 2.2.3 --- Characterization of Bupleuri radix --- p.55 / Chapter 2.2.4 --- In vivo Drug Treatment --- p.59 / Chapter 2.2.5 --- Isolation and preparation of cells --- p.59 / Chapter 2.2.6 --- Assays for the immunomodulatory activities of Bupleuri radix --- p.62 / Chapter 2.2.7 --- Assays for the immunorestorative properties of Bupleuri radix --- p.74 / Chapter 2.2.8 --- Assays for the anti-tumour activities of Bupleuri radix --- p.75 / Chapter 2.2.9 --- Statistical analysis --- p.83 / Chapter Chapter Three： --- "Fractionation, Purification and Characterization of Bioactive Compounds from Bupleuri radix" --- p.84 / Chapter 3.1 --- Results / Chapter 3.1.1 --- Extraction and Fractionation of Bupleuri radix --- p.85 / Chapter 3.1.2 --- Purification of Bupleuri radix --- p.85 / Chapter 3.1.3 --- Carbohydrate and Protein Contents of B.R. Fractions --- p.87 / Chapter 3.1.4 --- Lack of cytotoxicity of Bupleuri radix to Mouse Splenocytes --- p.91 / Chapter 3.1.5 --- LC50 of B.R. Fractions determined by Brine Shrimp Bioassay --- p.91 / Chapter 3.1.6 --- Heat stability of B.R. Fractions --- p.93 / Chapter 3.1.7 --- "Uronic Acid Content of BRIai, BRIaii, BRIbi and BRIbii" --- p.93 / Chapter 3.2 --- Discussion --- p.93 / Chapter Chapter Four： --- The Immunomodulatory Activities of Bupleuri radix --- p.96 / Chapter 4.1 --- Results / Chapter 4.1.1 --- Effect of Bupleuri radix on the Specific and Nonspecific Immunity --- p.97 / Chapter 4.1.1.1 --- Mitogenic effect of B.R. Fractions on Murine Splenocytes in vitro --- p.97 / Chapter 4.1.1.2 --- Mitogenic effect of B.R. Fractions on Murine Splenocytes ex vivo --- p.97 / Chapter 4.1.1.3 --- In vitro Mitogenic effect of B.R. Fractions treated with Periodate --- p.103 / Chapter 4.1.1.4 --- In vitro Mitogenic effect of B.R. Fractions treated with Acetic Acid --- p.103 / Chapter 4.1.1.5 --- In vitro Co -mitogenic effect of B.R. Fractions with Polymyxin B Sulphate --- p.107 / Chapter 4.1.1.6 --- Effect of B.R. Fractions on Lymphocyte sub-populations --- p.107 / Chapter 4.1.1.7 --- Primary Humoral Immune Response to SRBC in B.R.-treated mice --- p.107 / Chapter 4.1.1.8 --- Activity of cytotoxic T cells in B.R-treated mice --- p.111 / Chapter 4.1.1.9 --- Effect of B.R. Fractions on Interleukin-1 - like Factors Production --- p.111 / Chapter 4.1.1.10 --- Effect of B.R. Fractions on Interleukin-2 Production --- p.116 / Chapter 4.1.1.11 --- Effect of B.R. Fractions on Interleukin-2 Receptor Expression on Murine Splenocytes --- p.116 / Chapter 4.1.1.12 --- Effect of B.R. Fractions on GM-CSF Production --- p.119 / Chapter 4.1.1.13 --- Immunopotentiating effects of B.R. Fractions on Macrophages: --- p.119 / Chapter 4.1.1.13.1 --- In vivo Migration of Macrophages in B.R.-treated mice --- p.119 / Chapter 4.1.1.13.2 --- Effect of B.R. Fractions on the Fc Receptor Expression on Murine Resident Peritoneal Exudate Cells --- p.123 / Chapter 4.1.2 --- Immunorestorative Properties of Bupleuri radix --- p.123 / Chapter 4.1.2.1 --- Effect of B.R. Fractions on Lymphocyte Blastogenesis in Aged Mice --- p.123 / Chapter 4.1.2.2 --- Effect of B.R. Fractions on Lymphocyte Blastogenesis in Tumour-bearing Mice --- p.125 / Chapter 4.2 --- Discussion --- p.125 / Chapter Chapter Five： --- The Anti-tumour Activities of Bupleuri radix --- p.132 / Chapter 5.1 --- Results / Chapter 5.1.1 --- Cytostatic Effect of B.R. Fractions on Murine Tumour Cell Lines in vitro --- p.133 / Chapter 5.1.2 --- Effect of B.R. Fractions on the Growth of Tumour Ceils in vivo --- p.133 / Chapter 5.1.3 --- Effect of B.R. Fractions on the Survival of EAT-bearing mice --- p.140 / Chapter 5.1.4 --- Ex vivo Induction of Natural Killer Cell Activity by B.R. Fractions --- p.146 / Chapter 5.1.5 --- In vitro Induction of Lymphokine-activated Killer Cell Activity by B.R Fractions --- p.149 / Chapter 5.1.6 --- In vivo Induction of Tumour Infiltrating Lymphocytes by B.R. Fractions --- p.149 / Chapter 5.1.7 --- In vitro Induction of Macrophage-mediated Cytostatic Effect on Tumour Cells by B.R. Fractions --- p.151 / Chapter 5.1.8 --- In vitro Induction of Macrophage-mediated Cytostatic Eifect on Tumour Cells by B.R. Fractions --- p.153 / Chapter 5.1.9 --- Effect of B.R. Fractions on γ-interferon Production in vitro --- p.156 / Chapter 5.2 --- Discussion --- p.156 / Chapter Chapter Six： --- "General Discussion, Conclusion and Future Prospects" --- p.164 / Bibliography --- p.i

Orientador: Jean Leandro dos Santos / Banca: Cleverton Roberto de Andrade / Banca: Marcos Antonio Correa / Resumo: A acne é uma doença autolimitada de componente multifatorial, caracterizada pela presença de inflamação e colonização bacteriana pelo microrganismo Propionibacterium acnes. Atualmente, o tratamento tópico e/ou oral, inclui fármacos com propriedades anti-inflamatórias, antimicrobianas e queratolíticas. Apesar dos efeitos benéficos no tratamento da acne, a terapia atual apresenta limitações que justificam a busca de novos fármacos. Furoxanos e benzofuroxanos são compostos heterocíclicos contendo a função N-óxido e que apresentam uma grande diversidade de propriedades farmacológicas, incluindo antimicrobiana. Neste trabalho investigouse o efeito antimicrobiano de compostos furoxanos e benzofuroxanos pertencentes à biblioteca de moléculas do laboratório de Química Farmacêutica e Medicinal da Faculdade de Ciências Farmacêuticas. Para fins de caracterização do espectro de ação, além do P. acnes foi realizado screening do perfil de atividade antimicrobiana frente às cepas fúngicas, bactérias Gram positivas e Gram negativas usando as técnicas de microdiluição. Os furoxanos e benzofuroxanos foram testados em concentrações que variaram de 0.03 a 100 μg/mL. Foram usados controles como a cefazolina (0.39 μg/mL) para P. acnes, o imipenen (<0.39 μg/mL) para as bactérias Gram positivas, aztreonan (<0.39 μg/mL) para as Gram-negativas, anfotericinaB (0.25 μg/mL) e o fluconazol (65 μg/mL) para as espécies de Candida e Cryptococcus, respectivamente. Após incubação, foram realizadas leituras vis... (Resumo completo, clicar acesso eletrônico abaixo) / Abstract: Acne is a self-limiting disease of multifactorial component characterized by the presence of inflammation and bacterial colonization by Propionibacterium acnes. Currently, topical and oral treatments include drugs presenting anti-inflammatory, antimicrobial, exfoliating and keratolytics properties. The current treatment has shown adverse effects that justify the search for new anti-acne drugs.Furoxan and benzofuroxan are heterocyclic compounds containing the N-oxide function that exhibit a wide range of pharmacological properties, including antimicrobial. Here, we investigated the antimicrobial effect of furoxans and benzofuroxans derivatives from a library of compounds belonging to the Medicinal Chemistry Laboratory on the School of Pharmaceutical Sciences - UNESP. In order to characterize the spectrum of action not only P. acnes, but also fungal, Gram positive and Gram negative strains of bacteria were used. Minimum Inhibitory Concentration (MIC) was determinate by microdilution technique. Benzofuroxan and furoxans were tested at concentrations ranging from 0.03 to 100 μg/mL. It was used as controls:cefazolin (0.39 μg/mL) for P. acnes; imipenem (<0.39 μg/mL) for Gram positive bacteria; aztreonan (<0.39 μg/mL) to Gram-negative; amphotericin B (0.25 μg/ml) and fluconazole (>65 μg/mL) for species of Candida and Cryptococcus, respectively. After incubation, visual readings... (Complete abstract click electronic access below) / Mestre

Ph.D.

Diss. (sammanfattning) Stockholm : Karolinska institutet, 2009. / Härtill 4 uppsatser.