Dissertações em Ciências Farmacêuticas (Mestrado) - PPGCF/ICS
URI Permanente para esta coleçãohttps://repositorio.ufpa.br/handle/2011/2313
O Mestrado Acadêmico em Ciências Farmacêuticas teve início em 2005 e homologado pelo CNE e funciona no Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF) do Instituto de Ciências da Saúde (ICS) da Universidade Federal do Pará (UFPA).
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Item Acesso aberto (Open Access) Ação antimicrobiana do óleo essencial de Piper Aduncum e dilapiol em infecções de pele(Universidade Federal do Pará, 2015-06-25) FERREIRA, Roseane Guimarães; MAIA, José Guilherme Soares; http://lattes.cnpq.br/1034534634988402Piper aduncum L. is a plant with several biological properties such as antimicrobial activity, which is mainly associated with the action of its essential oil rich in dilapiolle. In recent years, the occurrence of skin infections caused by bacteria and fungi increased considered shape. Thus, this study aimed to evaluate the antimicrobial activity of essential oil of P. aduncum (OEPA) and dilapiolle, its major constituent, against pathogenic skin micro-organisms and their attachments. The antimicrobial activity was performed using the microdilution method and Forming Units count Cologne (UFC) for determining the Minimum Inhibitory Concentration (MIC), the Bactericidal Concentration Minimum (CBM) and Minimum Fungicidal Concentration (CFM). These plant compounds were tested against the filamentous fungi dermatophytes (FFD) and not dermatophyte (FFND), gram-positive bacteria and yeast. The results showed Trichophyton mentagrophytes front (ATCC and clinical isolate), MIC values of 500μg.mL-1 for OEPA and dilapiolle and CFM 1500 and 1000 µg.mL-1 , respectively. For clinical isolates of Trichophyton rubrum and Epidermophyton floccosum the MIC values of 500μg.mL-1 and CFM 1500μg.mL-1 , were similar for the two compounds as well as Microsporum canis and Microsporum gypseum with MIC values of 250μg.mL-1 and CFM 500μg.mL-1 . The Aspergillus fumigatus ATCC FFND showed an MIC of 3.9μg.mL-1 and 7.8 μg.mL-1 and the clinical isolate strain MIC of 3.9μg.mL-1 and CFM 15.6 μg.mL-1 for both. However showed no activity against Candida albicans and the yeast bacteria Staphylococcus aureus in the concentrations used.Item Acesso aberto (Open Access) Análise do remédio artesanal “tintura de pata-de-vaca” tendo a tintura de Bauhinia monandra Kurz como referência(Universidade Federal do Pará, 2016-03-17) SILVA, Ana Paula Paiva da; SILVA, Marcos Valério Santos da; http://lattes.cnpq.br/0379783635000306; BARBOSA, Wagner Luiz Ramos; http://lattes.cnpq.br/1372405563294070Diabetes mellitus is one of the various pathologies can be controlled with the use of medicinal plants, which exhibit hypoglycemic activity through different mechanisms. In Marudá, Marapanim-PA, the Women's Group "Erva Vida", produces and markets the "Tintura de pata-de-vaca" consumed by tourists and locals to treat diabetes. This remedy is prepared from leaves of Bauhinia monandra Kurz (pata-de-vaca). Different metabolic classes of plant already had a proven hypoglycemic action, for example flavonoids. Thus, the aim of this study was to characterize the handmade medicine through pharmacobotanic parameters pharmacognostic, phytochemicals and chromatographic in compararação with a tincture of Bauhinia monandra, for the presence of flavonoids. Both the preliminary phytochemical analysis, and the analysis by Thin Layer Chromatography, phenolic metabolites detected, possibly flavonoids in handmade medicine and hydroethanolic extract of plant species. In the analysis by HPLC, it revealed the presence of rutin in handmade medicine as well as in hydroethanolic extract of Bauhinia monandra.Item Acesso aberto (Open Access) Atividade anticolinesterásica dos óleos essenciais e componentes majoritários de Piper spp e Aniba canelilla e docagem molecular do 1-nitro-2-feniletano(Universidade Federal do Pará, 2013-05-28) SILVA, Nayla Nunes dos Santos; ANDRADE, Eloisa Helena de Aguiar; http://lattes.cnpq.br/3827055876022373; MAIA, José Guilherme Soares; http://lattes.cnpq.br/1034534634988402Currently, Alzheimer's disease (AD) is considered a significant public health problem worldwide and the major complication of the disease is the deficit of cholinergic neuron activity, a fact that can be reversed and/or mitigated by raising levels of the neurotransmitter acetylcholine (ACh). The most effective way to increase the available amount of acetylcholine is the inhibition of the acetylcholinesterase enzyme (AChE). In the search for new natural cholinesterasic inhibitors, the essential oils and major components of five aromatic plants occurring in the Amazon region were investigated using the AChE inhibition test by direct bioautography. The oils and major components were obtained from Aniba canelilla (1-nitro-2-phenylethane), P. aduncum (dillapiole), P. callosum (safrole), P. divaricatum (methyleugenol) and P. marginatum (safrole+3,4-methylenedioxipropiophenone). The oils of A. canelilla and P. aduncum showed enzyme inhibition zone in amounts of 0.01 ng and 1ng, respectively. The oil of P.marginatum showed weak activity (~ 100 ng) and the oils of P. callosum and P. divaricatum were inactive. Among the major constituents, who showed activity are the phenylpropanoids 1-nitro-2-phenylethane, isolated from the oil of A. canelilla, and safrole and elemicin, isolated from the oil of P. callosum, which inhibited the AChE in amounts of 0.01, 1000 to 1000 ng, respectively. The results indicate that the oil of A. canelilla and 1-nitro-2-phenylethane inhibited AChE in the same proportion as the pattern physostigmine. The molecular docking study was added to the experimental results, showing that the nitro group of 1-nitro-2-phenylethane can establish hydrogen bonds with the hydroxyl group of the serine residue existing in the catalytic AChE molecule, suggesting that the electronegative character of 1-nitro-2-phenylethane may be responsible for this strong chemical interaction.Item Acesso aberto (Open Access) Avaliação da atividade dos extratos hidroetanólico de Chenopodium ambrosioides L. e de Eucalyptus alba Reinw ex Blume, frente a cepas de Mycobacterium sp(Universidade Federal do Pará, 2014-10) VALÉRIO, Erika da Silva; BARBOSA, Wagner Luiz Ramos; http://lattes.cnpq.br/1372405563294070; TEIXEIRA, Francisco Martins; http://lattes.cnpq.br/7648303522085382Chenopodium ambrosioides and Eucalyptus alba are species used in folk medicine for the treatment of tuberculosis and sputum. This study aimed to determine the physical-chemical, microbiological parameters, define phytochemical screening and evaluate antimycobacterial, cytotoxicity, immunomodulation, and toxicity in vivo activities of extracts and fractions. In physical-chemical and microbiological evaluation of C.ambrosioides and E. alba extracts, were found parameters in accordance with the specific literature for medicinal plants. The phytochemical screening of the extracts revealed the presence of saponins, steroids, triterpenoids, phenols and tannins, C. ambrosioides extract also showed proteins and amino acids, while the E. alba extract was positive for organic acids and lactones. The results of broth microdilution assay and microplate alamar blue assay showed moderates activities against the Mycobacterium fortuitum of E. alba extract and ethyl acetate fraction (FAcE) of E. alba; the chloroform fraction (FCl) of C.ambrosioides and the ethyl acetate fraction (FacEA) of E. alba were moderately active against the Mycobacterium tuberculosis. The cytotoxic activity, evaluated by MTT method, showed that the extracts did not reduce cell viability in the concentrations tested. In the immunomodulation assay, E. alba extract presented potential anti-inflammatory effect, by the methods of inhibition the production of NO and TNFα. No signs of acute oral toxicity of the extracts at a dose of 2500 mg/kg in mice were detected. These results suggest the potential antimycobacterial the FAcE of E. alba and immunomodulatory of E. alba extract and can serve as a resource for future studies, aimed at isolation of active compound and elucidation of their mechanisms of action.Item Acesso aberto (Open Access) Diagnóstico situacional e análise espacial da logística reversa de medicamentos domiciliares vencidos ou em desuso em uma rede varejista do Brasil(Universidade Federal do Pará, 2023-07-05) OLIVEIRA, Camila Martins; SENA, Luann Wendel Pereira de; http://lattes.cnpq.br/6233488431016391; https://orcid.org/0000-0001-9363-5766Introduction: The reverse logistics process of disused or expired medicine for the general population makes the reverse flow, returning along its production and distribution chain, to have its final disposal environmentally sound. In this sense, the pharmacist is fundamental because he plays the role of knowledge multiplier, qualifying, training, and instructing employees and consumers about good environmental practices related to health waste. Objective: To carry out a situational diagnosis of reverse logistics and spatial analysis of expired or disused household medications in a pharmaceutical retail chain in Brazil. Method: It is an exploratory, cross sectional, and prospective study that used product/waste information obtained at different collection points in a network of pharmacies with 400 establishments in Brazil, from 2020 to 2022. Results: The study showed that the network collected a volume of 4,519.74 kg of expired medicines from the population between 2020 and 2022, concentrating the largest collection volume in the North region (69.1%). It is also noteworthy that Belem was the municipality with the highest collection, concentrating 92.5% of the collection in the state of Pará. Another important point was the presentation of a manual for the implementation of reverse logistics for expired medicines for the population. Conclusion: The findings of this study should contribute to the improvement and application of reverse logistics for expired medicines for the population in Brazil.Item Acesso aberto (Open Access) O efeito in vitro dos compostos ácido alfa-lipoico e resveratrol em parâmetros do estresse oxidativo durante o uso da poliquimioterapia para hanseníase(Universidade Federal do Pará, 2014-10-20) PESSÔA, Mariely Cristine Amador; MONTEIRO, Marta Chagas; http://lattes.cnpq.br/6710783324317390The leprosy is an infectious disease that represents a major preoccupation in global public health in 21st century. The treatment with Multi Drug Therapy (MDT) approved by the World Health Organization (WHO) is the best treatment to Mycobacterim leprae infection; however, is one of the factors of increasing Reactive Oxygen Species (ROS) production and the development of methemoglobinemia and hemolytic anemia in these patients. The aim of this study was to verify the oxidative damage in leprosy patients receiving MDT, by evaluation of hematological and oxidative stress biomarkers, and identify the effects of in vitro treatment with antioxidants alpha-lipoic acid (ALA) and resveratrol (RSV) in antioxidant enzymes activity and prevention of methemoglobinemia. The results revealed a decrease in RBC count and reticulocytosis in patients receiving MDT during the 4th and 7th month of treatment. The percentual of methemoglobin increased since the fifth month of treatment with MDT, and the treatment with 100 μM RSV-treated and ALA-treated preserved the values similar to control group only in 4th to 6th month of MDT samples. The leprosy patients presented values of SOD activity similar to the control group and a decreased CAT activity, leading to an inbalance in the ratio of both enzymes and possibly resulting in an over-producing of H2O2. The treatment with RSV and ALA in 100 μM and 500 μM concentrations increases twice the SOD activity in 4th month patient samples; however, these concentrations did not change CAT and SOD activities found in leprosy patients. Such results demonstrate that RSV and ALA did not show antioxidant activity in installed oxidative stress, and subsequent studies are necessary to evaluate dose-dependent and time-dependent concentrations of RSV and ALA to prevent oxidative damage in chronic infectious diseases.Item Acesso aberto (Open Access) Efeitos neurocomportamentais e no estresse oxidativo em ratos tratados com extrato etanólico de própolis amarela(Universidade Federal do Pará, 2015) SILVEIRA, Cinthia Cristina Sousa de Menezes da; MAIA, Cristiane do Socorro Ferraz; http://lattes.cnpq.br/4835820645258101Propolis is a resinous substance produced by bees that collect raw material from different parts of plants, through the addition of salivary secretions and wax. In Brazil, 13 types of propolis were chemically characterized. In the yellow propolis of Mato Grosso do Sul were identified 15 compounds, all belonging to the class of triterpenoids, and low levels of phenolic compounds and flavonoids. This work aims to conduct behavioral and biochemical assays with acute administration of yellow propolis ethanolic extract. 8 groups of male Wistar rats, 3 months, were used (n = 10 per group) and were divided into control (Tween 5%), positive control for anxiolytic activity (diazepam), positive control for antidepressant activity (fluoxetine), positive control for mnemonic effect (caffeine), 4 doses of the extract (1, 3, 10, 30mg/kg). The extract administration was performed acutely, intraperitoneally. Behavioral tests were open field, elevated plus maze, forced swimming and inhibitory avoidance. After the behavioral testing was performed to collect blood in the intracardiac area of the animals for determination of nitric oxide, malondialdehyde, catalase, superoxide dismutase and total antioxidant capacity. The results obtained in the open field test showed spontaneous locomotion preserved and anxiolytic-like activity, confirmed result with the elevated plus maze. In the forced swimming test, the yellow propolis ethanolic extract demonstrated action of antidepressant-like. In the inhibitory avoidance test showed mnemonic activity at 30 mg/kg. In the evaluation of oxidative biochemistry, the extract reduced the production of nitric oxide and malondialdehyde without changing level of total antioxidant, catalase and superoxide dismutase, induced by stress. With these results it is concluded that the yellow propolis ethanolic extract has anxiolytic, antidepressant, mnemonic and antioxidant activity.Item Acesso aberto (Open Access) Efeitos no comportamento motor após intoxicação subcrônica de metilmercúrio na presença de etanol (padrão binge) em ratas adolescentes à fase adulta(Universidade Federal do Pará, 2015-11-06) OLIVEIRA, Aline do Nascimento de; MAIA, Cristiane do Socorro Ferraz; http://lattes.cnpq.br/4835820645258101Exposure to methylmercury through the contaminated seafood diet, concomitant abusive alcohol intake, in binge pattern, is quite common in gold mining communities of gold extraction, especially in the Amazon. The association between these two neurotoxicantes is also evident among adolescent women and creates the need to understand its effects on the central nervous system, especially in motor coordination, balance and spontaneous locomotion, because the studies are advanced only for the effects of exposure in isolation. Therefore this study aims to evaluate the effects on motor behavior resulting of subchronic exposure to methylmercury in the presence of alcohol, in binge pattern, in adolescents female rats until early adulthood (37-72 postnatal day), through behavioral motors tests, like Open Field, Pole Test, Rotarod and Beam Walking Test. The testing occurred 24 hours after the last intoxication of rats, which received methylmercury (0.04 mg / kg / day) for 35 days, concomitant with alcohol (3g / kg / day), 3 intermittent days, 1 time per week (binge), totaling 5 binges. The results showed a decrease in spontaneous locomotion in Open Field test through the parameters of the total distance traveled and number of rearing. In the Pole test was increased fall time, evidencing the bradykinesia. In the Rotarod there was a decrease in latency in the first three exhibitions, as well as Beam Walking Test was increased latency and number of slips, especially in thinner beams, showing that subchronic exposure to methylmercury in the presence of alcohol, in the binge, in adolescent female rats was able to produce behavioral damages related to coordinating motor, balance and spontaneous locomotor activity.Item Acesso aberto (Open Access) Estudo teórico do complexo cefoxitina-proteína 5 de ligação à penicilina da Escherichia Coli por dinâmica molecular com método híbrido de mecânica quântica/ mecânica molecular(Universidade Federal do Pará, 2014-12-12) SILVA, Thaís Boulhosa Barros da; BARROS, Carlos Augusto Lima; http://lattes.cnpq.br/8902921733540173; MONTEIRO, Marta Chagas; http://lattes.cnpq.br/6710783324317390The Penicillin Binding Proteins (PBPs) are important for the development of new drugs against bacterial infections biological targets. This study was aimed to understand the interaction between the protein and cefoxitin 5 Penicillin-Binding (PBP5) of Escherichia coli (deposited in the PDB under the code 3MZE) through simulation Molecular Dynamics (MD), using the approach hybrid quantum molecular mechanics (QM/MM) and mechanical. As well as develop a prototype to evaluate, through computer simulation, the susceptibility of Gram negative bacteria against antibiotics. The analysis of antimicrobial susceptibility to antibiotics tested has shown that this strain of E. coli ATCC 8739 was sensitive to 5 antimicrobials study. The strain of E. coli derived from the clinical isolate was resistant to ciprofloxacin 5 μg and gentamicin 10 μg, intermediate sensitivity to cefepime 30 μg and ceftazidime 30 μg, and sensitivity to cefoxitina 30 μg. The difference in susceptibility of E. coli strain ATCC 8739 and strain of E. coli isolated from a clinical can show a molecular immunological memory of the bacteria. We observed no production of β-lactamases by the strain of E. coli derived from clinical isolate, suggested because no observed difference in antimicrobial susceptibility with respect to the presence or absence of EDTA on the disks containing the antibiotics. The analysis has revealed that protonation of the deprotonated His146, His151, His216 and His320 residues. The stabilization of the complex was studied after 0,6 ns of MD simulation. Moreover, a decomposition analysis in terms of energy was performed to determine the contributions of individual amino acid residues for protein-ligand interactions. The results revealed that cefoxitin has a strong interaction with Lis44, Lis210, Ser41, Gli212, His213, Glu246 residue, apart from water, which are important for stabilizing cefoxitin-PBP5 complex. The electrostatic potential map Molecular cefoxitin revealed a highly electrophilic center corresponding to the β-lactam ring, which promotes hydroxyl attack nuceofílico the serine residue of the E. coli PBP5 active site region. These results can give support the planning of new more selective and effective drugs to control bacterial infections. The experimental results were statistically consistent with the theoretical results thus this work can be used as a prototype for computing theoretical evaluate the antimicrobial susceptibility to Gram negative bacteria. This study may find applications in future planning and development of new and potent compounds with antimicrobial activity. Mainly in attempts to modify an inhibitor, particularly of the cephalosporin class in order to improve its selectivity and its activity.Item Acesso aberto (Open Access) Geoprópolis produzida por diferentes espécies de abelhas: atividades antimicrobiana e antioxidante e determinação do teor de compostos fenólicos(Universidade Federal do Pará, 2015-05-15) LIMA, Marcus Vinicius Dias de; MONTEIRO, Marta Chagas; http://lattes.cnpq.br/6710783324317390Among meliponineos or stingless bees the most important are Melipona quadrifasciata (Mandaçaia), Melipona marginata (Manduri) and Tetragonisca angustula (Jataí). One of their product is geopropolis, a balsamic and resinous substance with complex chemical composition, collected from shoots, seepage and other parts of the plant tissue by these bees, which transformed it through enzymatic process by adding secretions and earth or clay, alone or in combination. Among the chemicals components, highlights the presence of phenolic compounds, diterpenes, triterpenes, essential oils and many other. The most studied propolis activity are antibacterial and antifungal, in addition to antiviral, immunomodulatory, anti-tumor, anti-inflammatory and antioxidant. Therefore this work aim to evaluate the antimicrobial activity, through determination of Minimum Inhibitory Concentration (MIC), Minimum Bactericidal Concentration (MBC) and Trolox equivalent antioxidant capacity assay (TEAC), beyond the determination of the levels of flavonoids and phenolics compounds (Folin-Cioucalteu method and complexation with aluminum chloride, respectively) using geopropolis samples from different bees species (Melipona quadrifasciata, Melipona marginata and Tetragonisca angustula). All the geopropolis samples exhibit antimicrobial activity against gram-positive bacteria, wherein the Manduri Bee showed the lowest MIC and MBC; only Mandaçaia species showed moderate activity against gram-negative bacteria. The Manduri's geopropolis showed higher content of phenolics compounds and flavonoids, followed by Mandaçaia's geopropolis and both were in accordance with the parameters established by current legislation, wherein the Manduri's geopropolis also present high total antioxidant levels compared with other bees. It was noted that the antimicrobial activity of geopropolis extracts were not directly associated with high levels of phenolic compounds, including flavonoids.Item Acesso aberto (Open Access) Nanocápsulas de PLGA e gordura de murumuru contendo β-lapachona: preparação, caracterização e atividade citotóxica(Universidade Federal do Pará, 2016-09-30) PONTES, Anna Carolina Avelar de Araujo; SILVA, Jaqueline Rodrigues da; http://lattes.cnpq.br/8336745480297714; OLIVEIRA, Alaide Braga de; http://lattes.cnpq.br/3719659803766075The β-lapachone (β-lap) is a natural naphthoquinone, found as a minor constituent in some species of ipe (gender Handroanthus Mattos) with pharmacological properties such as antimicrobial, anticancer and trypanocidal activities. However, their therapeutic application is challenging due to its low aqueous solubility, and high toxicity. In order to improve the bioavailability of this compound and increase its safety, different carrier systems with nanometric sizes have been developed. The nanocapsules (NC's) PLGA with oil core of murumuru fat (NCMM) were the choice for this study to encapsulate and load the β-lap. The extraction and synthesis of β-Lap of ipe sawdust lapachol promoted a yield of 92.3%. Using the nanoprecipitation method, the produced nanocapsules containing β-lap (NCMMβ-lap) showed spherical shape, surface roughness, average size between 2.0 and 132.5 ± 1.3 ± 149, polydispersity <0.2, zeta potential of -0.009 ± 0.2 and 0.15 ± 0.2 and an encapsulation efficiency of 94.3%. The NCMMβ-lap cytotoxicity showed dose- and time-dependent for the cell lines NIH/3T3 and MCF7, being more toxic than free β-lap in the same concentrations, and selective for tumor cell line MCF7. The mechanisms of cell death of free β-lap and NCMMβ-lap were very similar, observing ROS, DNA fragmentation, interlock of cells in check phases, and indication of late apoptosis and necrosis. In short, the encapsulation of β-lap potentiated the anticancer activity and suggested greater certainty in the application of this drug, pointing NCMMβ-lap as a promising alternative to enable the use of β-lap at the clinic.Item Acesso aberto (Open Access) Nocicepção em prole adulta de camundongo em exposição à morfina no período gestacional e lactação(Universidade Federal do Pará, 2014-10-18) CASTRO, Nair Correia de Freitas; MAIA, Cristiane do Socorro Ferraz; http://lattes.cnpq.br/4835820645258101The use of morphine as a drug of abuse during pregnancy and lactation induces effects on the developing fetus are still not well elucidated, in which the perinatal exposure to morphine showed increased sensitivity to morphine reinforcement effect in the adult offspring. The present study investigated whether exposure to morphine during pregnancy and lactation can change nociception in adult offspring offspring of mothers treated with morphine. Pregnant female mice were exposed to morphine (10 mg / kg / day) subcutaneously for 42 days (21 days of pregnancy to 21 days of lactation). Upon completion 21 days, the progeny is sexed in males and females, then at 75 days of age, subjected to the open field test and nociception by the methods of writhing induced by acetic acid, hot plate and formalin. In the test of the total locomotion, the animals showed no motor changes. In nociception tests, we observed increased nociceptive response in male mice and female morphine group tested for contortion. Males who have been exposed perinatally to morphine decreased the nociceptive threshold in the second phase (inflammatory phase) of formalin. In the hot plate, the male and female animals showed abnormalities in pain sensitivity, reversing the sensitivity profiles of its controls, in which the group of males exposed perinatally to morphine showed increased sensitivity to thermal stimulus at 120 min test and the group of females exposed perinatally to morphine decreased thermal sensitivity when compared to their controls. These results suggest that exposure to morphine in the intrauterine period and lactation affects nociceptive thresholds in the offspring in later life and that this change is dependent on the type and length of exposure to noxious stimuli.Item Acesso aberto (Open Access) Obtenção e caracterização de carreadores lipídicos nanoestruturados a partir de gordura vegetal de murumuru (Astrocaryum murumuru Mart.)(Universidade Federal do Pará, 2016-05-16) SENA, Luann Wendel Pereira de; SILVA JÚNIOR, José Otávio Carréra; http://lattes.cnpq.br/4437885351749994The nanostructured lipid carrier (NLC) have been proposed as a carrier’s category for pharmaceutical and cosmetic ingredients and an increasing of interest due to a series of advantages when compared to conventional formulations. The Amazonian vegetable fats are considered lipids arrays of great potential for the production of NLC from topical administration, according to the low toxicity and biocompatibility, beyond their emollient properties, protector and moisturizer in the skin. The murumuru (Astrocaryum murumuru Mart.) is an amazon palm and the utility of its fat is promising, because it adds value to the products, favour the growth in the region, in addition to using these resources in a sustainable way. The objective of this research was to obtain and characterize the NLC from the vegetable fat of Murumuru (Astrocaryum murumuru Mart.) by the homogenization technique under high pressure to hot, using ketoconazole as a drug modelling. The gas chromatography showed lauric acid (48,1 %), myristic acid (26,6 %) and oleic acid (8,4 %), as main constituents. The physical-chemical characterization showed acid, iodine, saponification, peroxide, refraction and density values within the limits and standards recommended. The isolated raw materials and the NLC obtained were evaluated using differential scanning calorimetry, where the results about the isolated raw materials used support as was described in Literature and the NLC demonstrated a crystalline structure less ordained. In the tested formulations, the nanoparticles showed average size between 98,60 and 161,56 nm, polydispersibility index between 0,115 and 0,276, zeta potential higher than -30mV and encapsulation efficiency near 100 %. The Transmission Electron Microscopy indicated spherical aspect of the nanoparticles and the! clearance profile showed a zero order kinetic model, with the release of 70,9 % of the encapsulated drug in 8 hours. The nanoparticles remained stable during a period of 60 days. This research showed that the murumuru fat obtained an effective system, with small sizes particles and penetrability in the skin, making possible the formulation propagation in pharmaceutical and cosmetic uses.Item Acesso aberto (Open Access) Obtenção e caracterização de formulação fitoterápica contendo extrato e tintura padronizados de arnica montana l e aesculus hippocastanum l(Universidade Federal do Pará, 2015-12-18) ARNILLAS, Elyan Andrade Pueyo; VIEIRA, José Luiz; SILVA JÚNIOR, José Otávio Carréra; http://lattes.cnpq.br/4437885351749994Because of the wide dissemination and use of medicinal plants, industries are producing products based on plant species, such as extracts and tinctures, which are mainly used by pharmacy with handling. However, it is questionable collateral for the vast majority of these products as to their efficacy, safety and quality, and may bring risks to the user's health. So, it is important to perform quality control for herbal products, according to current legislation. The formulation that gave rise to the research is a carbopol gel containing Arnica montana L dye and Aesculus hippocastanum L extract. The present study aimed at obtaining and characterization of said formulation and validate the use of methods of pharmaceutical technology by performing the standardization of Aesculus hippocastanum L extract and Arnica montana L dye, to the physio-chemical evaluation were performed: microbiological control, organo-leptical characterization, determination of pH, density, dry, loss on drying, determine the level solids, rheological behavior, concentration, lyophilization and chemical prospecting of plant inputs. For the phytochemical analysis was performed Thin Layer Chromatography of Arnica tincture (TLC) and Thin Layer Chromatography In Comparative (TLCC) Aesculus extract, Infrared and Thermal Analysis of both extracts as the formulation. For physicochemical characterization and validation of analysis Reports of the two plant species suppliers the results are within the parameters established by the Brazilian Pharmacopoeia Fifth Ed. The microbiologic control was to prove the absence of pathogenic microorganisms, the results indicated microorganisms absence of, for microbial contamination of the inputs can change the stability of the final product and further characterize risk of infection to the user. The chemical prospecting of plant species, was to identify relevant secondary metabolites, in the case of A. hippocastanum indicated the presence of saponins, represented by escin which is responsible for the pharmacological activity, was an important clue to the certification of the authenticity of the raw material in study. The viscosity of vegetable raw materials and formulation were determined by the rheometer of Brookfield, the extracts showed fluid behavior and Newtonian formulation showed a pseudo plastic behavior. The result of the Thin Layer Chromatography (TLC), assisted in the identification of the sample and possible tampering that could have occurred as well as the TLCC served to demonstrate the selectivity of the method as identified the presence of aescin, substance responsible for pharmacological activity Chestnut from India. In the validation of Arnica montana L. dye, it was detected by HPLC the presence of the rutin in the sample in nature with retention time 10.84 min. The infrared analyzes the plant species were observerd bands that may indicate the presence of the major chemical markers in the case Arnica indicated the presence of the rutin and escin in the presence of horse chestnut extract. In the thermal analysis TG / DTA, we can say that the first decomposition event occurred for the samples to 150 ° C, corresponding to weight loss, the values were 6.5 and 8% for the chestnut and arnica respectively. All results were significant for the characterization and quality control, used as benchmark for the standardization of the extract and tincture, the information obtained was also used for the certification of suppliers of extracts and tinctures for drugstores in Belém.Item Acesso aberto (Open Access) Planejamento e avaliação in sílica de análogos de lapachol em enzima alvo de Leishmania (Leishmania) amazonensis(Universidade Federal do Pará, 2017-11-09) FERREIRA, Érica Patrícia dos Reis; DOLABELA, Maria Fani; http://lattes.cnpq.br/0458080121943649; SANTOS, Lourivaldo da Silva; http://lattes.cnpq.br/3232898465948962The study aims to design and evaluate antiamastigote activity of Leishmania amazonensis and cytotoxicity Lapachol analogues. The studies predictive pharmacokinetic characteristics were performed, toxicological, biological activity and molecular docking or molecular docking. For pharmacokinetic and toxicological characteristics used the online program PreADMET while biological activities were assessed by online program Prediction Spectra of Activity is Substances (PASS). For the molecular docking analysis, the therapeutic target was selected Triponationa reductase, and the evaluation of interaction between the molecules and target this protein was performed by the virtual Molegro program docker (MVD). The extraction and isolation of Lapachol was performed and its identification was performed by nuclear magnetic resonance spectroscopy (NMR). All analogs Lapachol and are well absorbed from the intestine with the absorption ranging from 79.745% to 99.056%, furthermore inhibit the cytochrome P450 (CYP). Almost half of the molecules tested (42.1%) had moderate distribution into the central nervous system (CNS), including Lapachol, while the remainder have high distribution. The results of the toxicity of the molecules studied suggest that 63.16% are mutagenic and carcinogenic, which includes Lapachol and 10.5% and 5.26% are carcinogenic and mutagenic, respectively, but showed 21.05% not exhibit cytotoxicity. In molecular docking the substances studied showed less energy than the standard substance, although they have good interaction with energies between 94.343 to 115.635 kJ / mol. The Lapachol was isolated and identified. According with to the analogo results show that with the best characteristics was the 3,4-dihydroxy-2- (2-hydroxy-3-methylbutil) nafthalen-1 (4H) -one.Item Acesso aberto (Open Access) Simulação computacional de carreador lipídico nanoestruturado contendo gordura de cupuaçu (Theobroma Grandiflorum)(Universidade Federal do Pará, 2017-10-19) VIEIRA, Ana Paula Bastos Ferreira; SILVA JÚNIOR, José Otávio Carréra; http://lattes.cnpq.br/4437885351749994The constant evolution of the drug delivery systems boosted the search for new strategies, to obtain potentially promising formulations. Computational simulation and molecular modeling can provide effective contributions to the design and evaluation of complex systems, such as lipid nanocarriers containing natural inputs. In this work, a nanostructured lipid carrier (NLC) was proposed using triacylglycerols of cupuaçu fat and capric/caprylic acid, carnauba wax, tween 80®, pluronic® and an enantiomer of ketoconazole. Experimental tests were carried out to evaluate the crystallinity and thermal events of the lipid mixtures, which demonstrated that the M03 mixture had a lower enthalpy value (-15,17 J/g) and greater widening of the diffractogram peaks, suggesting a lower crystallinity structure. Computational simulations were performed to elucidate 3D structures, to study molecular and electrostatic properties, as well as intermolecular interactions with the drug. The molecular docking of M03 with ketoconazole showed interaction of the hydrogen bond type, with bond distance of 2,62 to 3,50Å and affinity energy of -5,3 Kcal/mol. The three-dimensional CLN model showed good molecular distribution and after simulation of molecular dynamics, the system remained stable (energy -1895,47 KJ / mol), with moderate to weak hydrogen bonding interactions and a distance of 2,45 to 3,50Å. RDF profiles established demonstrate strong interactions between ketoconazole and tween 80, between water and pluronic, between pluronic and SOO, and between tween 80 and SOO, all interactions occurring within the radius ≥2Å of distance. These results can be used as support to guide the future development of a CLN formulation, anticipating the experimental tests and helping to obtain thriving formulations.Item Acesso aberto (Open Access) Síntese, capacidade antioxidante e estudo comparativo entre fenilhidrazonas e chalconas como derivados do paracetamol(Universidade Federal do Pará, 2014) BELEZA FILHO, Raimundo Ferreira Gouvea Pimentel; BORGES, Rosivaldo dos Santos; http://lattes.cnpq.br/4783661132100859The prostaglandin-endoperoxide synthase (PGES) and cytochrome P-450 are key enzymes in human, which are responsible for analgesic effect and toxicity of acetaminophen, respectively. Acetaminophen or paracetamol is a widely used over-the-counter analgesic and antipyretic drug and appears to be safe if used in normal therapeutic doses, but large doses of ACP produce hepatic and/or renal injury in humans and in experimental animals. At moment, the design of new acetaminophen derivatives has few impacts for its clinical applications of safe acetaminophen derivative. Thus, in this work a series of acetaminophen derivatives based on chalcone and hydrazone analogy was been investigated using quantum chemical calculations at the DFT/B3LYP theory level, with the 6-31G* basis sets. The HOMO, IP, BDEOH, and spin density contribution for the oxidation of an initial electron or hydrogen atom abstraction from the phenolic hydroxyl group was related with the quenching reactivity of tyrosyl radical to give N-acetyl-p-benzosemiquinone imine (NAPSQI). The second hydrogen abstraction was related with the chemistry reaction between amide group and hydroxyl radical to give N-acetyl-p-benzoquinone imine (NAPQI). The lowest BDEOH values were related with higher quenching values of the tyrosyl radical and the stability was related with the spin density for the initial electron or hydrogen abstractions. The highest BDENH values were related with small NAPQI formation and LUMO values with reactivity of NAPQI-like Michael system. Our results showed that some analogous may be a good strategy for safer drug design of analgesic compounds. The compounds were synthesized and their antioxidant property was estimated using theoretical methods. Some compounds can be good antioxidant. A proposed mechanism for the interaction between hydrazone derivatives and PGES was realized using molecular properties.Item Acesso aberto (Open Access) Validação, atividade antifúngica e avaliação sinérgica de nitroestirenos in vitro(Universidade Federal do Pará, 2014-09-29) OLIVEIRA, Juliana Pantoja; BORGES, Rosivaldo dos Santos; http://lattes.cnpq.br/4783661132100859; MONTEIRO, Marta Chagas; http://lattes.cnpq.br/6710783324317390Nitro compounds have been used in therapy from the 40s, when they were widely synthesized and tested against various diseases as well as the discovery of their cytotoxic effects. Thus different groups, derivatives and analogs which could prove safer and more effective were studied. Some studies have shown that nitrostyrenes, like the nitrofenileteno possess diverse biological activities such as antifungal, antibacterial, anti-inflammatory, antinoceptive, etc. Additonally, there is currently a growing interest in new antifungal agents. Among the fungi of the genus Aspergillus is the most common Aspergillus fumigatus which is transmitted through the air causing aspergillosis. Dermatophytes are clinically relevant and cause various skin diseases, Trichophyton mentagrophytes being quite prevalent. The objective of this study was to validate the chemical structure of synthesized nitrostyrenes and evaluate its antifungal activity in two species of fungi, including a filamentous dermatophytes and opportunistic as well as evaluation of the synergistic effects among nitrostyrenes and amphotericin B (AB). The results confirm the infrared spectral and nuclear magnetic resonance of 1H nitrostyrenes analogues as correspond with the proposed structure. Test microdilution demonstrated in vitro antifungal activity of nitrostyrenes with MIC values for 4'-methyl-1-nitro-2- phenylethene (7B) of 0,05 mg/ml against A. fumigatus. For T. mentagrophytes the most active compound was 4'-methoxy-1-nitro-2-phenylethene (7C) with MIC of 0,22 mg/mL. Regarding the analysis of the combination of AB and nitrostyrenes in vitro by the checkerboard test showed antagonist compound 7A and 7C. The 7B compound was indifferent against the standard strain of A. Fumigatus.