Mestrado em Ciências Farmacêuticas (FF)

URI Permanente para esta coleçãohttp://200.137.215.59/tede/handle/tde/208

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Desenvolvimento e avaliação de um produto contendo canabidiol para aplicação tópica
(Universidade Federal de Goiás, 2025-07-07) Ferreira, Beatriz Xavier Almeida Matteucci; Conceição, Edemilson Cardoso da; http://lattes.cnpq.br/7193007113950510; Conceição, Edemilson Cardoso da; http://lattes.cnpq.br/7193007113950510; Silva Júnior, Arnóbio Antônio da; http://lattes.cnpq.br/2593509584288129; Oliveira, Gerlon de Almeida Ribeiro; http://lattes.cnpq.br/7985896725376640
Embargada.
Determinação simultânea de pesticidas em sangue post mortem por LC-MS/MS e aplicação em casos reais de suicídios por intoxicação exógena
(Universidade Federal de Goiás, 2024-03-21) Martins, Mayara Cardoso da Silva; Cunha, Luiz Carlos da; http://lattes.cnpq.br/6349547031976679; Cunha, Luiz Carlos da; http://lattes.cnpq.br/6349547031976679; Gouveia, Jhessica Cavalcante de Souza; http://lattes.cnpq.br/1218513275529526; Cruz, Alessandro de Carvalho; http://lattes.cnpq.br/5987649795108956
Embargada.
Efeito neuroprotetor do inibidor do transportador de prolina (LQFM164) em modelo animal de isquemia cerebral
(Universidade Federal de Goiás, 2025-05-23) Paula, João Elias Pinheiro Sousa de; Lima, Onésia Cristina de Oliveira; http://lattes.cnpq.br/5040685433940401; Pinto, Mauro Cunha Xavier; http://lattes.cnpq.br/0868250984727943; Pinto, Mauro Cunha Xavier; http://lattes.cnpq.br/0868250984727943; Torres, Bruno Benneti Giunta; http://lattes.cnpq.br/7060242425070126; Oliveira, Gisele Augusto Rodrigues de; http://lattes.cnpq.br/6221735418479539
Introduction: Cerebral ischemia is a debilitating neurological condition associated with high rates of mortality and morbidity. This highlights the importance of studying new prototypes for treatment. Objective: To investigate the neuroprotective potential of the prototype LQFM164 (an inhibitor of the L-proline transporter PROT/SLC6A7) in an animal model of middle cerebral artery occlusion (MCAO), as well as the compound's pharmacokinetics and pharmacodynamics through in silico analyses. Methods: C57BL/6 mice were subjected to the MCAO model and treated with different doses (1.25 mg/kg, 2.5 mg/kg, and 5 mg/kg) for five days. Evaluations included molecular docking and molecular dynamics simulations, as well as motor assessments (Limb Clasping and Cylinder Test) and morphological analysis (TTC staining). Results and Discussions: The results indicate that LQFM164 significantly reduces the cerebral infarct area at doses of 2.5 mg/kg (9.33 ± 1.80%) and 5 mg/kg (4.70 ± 0.91%), and improves motor function in behavioral tests, suggesting a neuroprotection effect. Conclusion: The prototype LQFM164 demonstrated a neurorestorative effect in a territorial cerebral ischemia model, highlighting its potential as a promising candidate for future therapies in neurological disorders.
Desenvolvimento e validação de métodos analíticos eco-eficientes para avaliação de azitromicina em comprimidos
(Universidade Federal de Goiás, 2025-07-01) Oliveira, Aline Sinzervinch de; Kogawa, Ana Carolina; http://lattes.cnpq.br/6638857912920334; Kogawa, Ana Carolina; http://lattes.cnpq.br/6638857912920334; Taveira, Stephânia Fleury; http://lattes.cnpq.br/0382450621383005; Bonfilio, Rudy; http://lattes.cnpq.br/0694401174796400
Embargado
Avaliação do perfil eletroquímico e fitoquímico de extrato de pitangas
(Universidade Federal de Goiás, 2025-07-29) Diniz, Elgia Procópio; Gil, Eric de Souza; http://lattes.cnpq.br/3218622824233303; Gil, Eric de Souza; Machado , Fábio Bahls; Paula, José Realino de
Pitanga (Eugenia uniflora) and pitangatuba (Eugenia selloi) belong to the Myrtaceae family, are native to Brazil and are considered superfruits due to their high nutritional value. The pitanga is available in a variety of colours, from red (the most popular) to black (purple) and yellow (less common). The pitangatuba has a bright yellow colour and an intense bittersweet flavour. Apart from the difference in pigmentation, the chemical richness in bioactive constituents of medicinal interest of each fruit is still an under-explored area. Both species have remarkable therapeutic properties, mainly due to their ability to inhibit free radicals. Therefore, due to the importance of determining the antioxidant capacity in relation to the therapeutic effect of these fruits, this study aimed to evaluate the antioxidant potential of the pitanga and pitangatuba varieties by electrochemical methods, as well as to verify the vasorelaxant activity and correlate these results with the phenolic composition determined by mass spectrometry. For the electrochemical experiments, the electroanalytical methods used were differential pulse voltammetry and square wave voltammetry. Additionally, a biosensor in carbon paste electrode using the enzyme polyphenoloxidase, obtained from the branches of the Cordia superba plant, was applied to the selected extracts. The vasorelaxant activity of the Eugenia uniflora varieties (red and purple) was evaluated in aortic artery rings of male Wistar rats, using arteries with intact vascular endothelium. The endothelial nitric oxide synthase (eNOS) pathway and the inhibitor N-nitro-L-arginine-methyl-ester (L-NAME) were used in this analysis. In the electrochemical tests, a similar profile was observed, with anodic peak c.a. Epa1 = 0.26 V for red and purple pitangas and 0.18 a 0,26 V for pitangatuba, which are indicative of polyphenolic compounds with high antioxidant potential. The extracts applied to the biosensor demonstrated significant improvement in the electroanalytical signal of red and purple Eugenia uniflora and Eugenia selloi when compared to the electrode without modification. The phenolic composition of Eugenia fruits determined by mass spectrometry revealed the predominance of cyanidin 3-O-glucoside in purple pitanga, myricetin 3-Ohexoside, apigenin and delphinidin 3-O-glucoside in red pitanga and gallic acid in pitangatuba. Pharmacological tests showed that Eugenia uniflora presented induction of nitric oxide production by endothelial cells and reduction of oxidative damage caused by KCl. On the other hand, purple pitanga presented better antioxidant capacity, corroborating the results obtained in other studies, highlighting its importance as a functional food.
Desenvolvimento de nanopartícula biomimética recoberta com membrana celular para a captação de patógenos como alternativa terapêutica para a COVID-19
(Universidade Federal de Goiás, 2023-03-20) Salomão, Mariana Arraes; Mendanha Neto, Sebastião Antonio; http://lattes.cnpq.br/0114608950477525; Lima, Eliana Martins; http://lattes.cnpq.br/7248774319455970; Lima, Eliana Martins; http://lattes.cnpq.br/7248774319455970; Fialho, Silvia Ligório; http://lattes.cnpq.br/6277013725246341; Feres, Valéria Christina de Rezende; http://lattes.cnpq.br/8089054699896454
Emabrgada.
Preparo e avaliação de dispersões sólidas contendo rutina por leito fluidizado e termoextrusão
(Universidade Federal de Goiás, 2025-11-26) Porfírio, Amanda Oliveira; Marreto, Ricardo Neves; http://lattes.cnpq.br/6127043775208484; Marreto, Ricardo Neves; Cunha Filho, Marcílio Sérgio Soares da; Taveira, Stephânia Fleury
embargado
Síntese e avaliação farmacológica de um novo candidato a protótipo de fármaco ansiolítico
(Universidade Federal de Goiás, 2011-11-24) Brito, Adriane Ferreira de; Costa, Elson Alves; Costa, Elson Alves; Lião, Luciano Morais; Landman, Maria Teresa Riggio de Lima
This paper aimed the design, synthesis and pharmacological evaluation in the central nervous system of a new piperazine derivative (LQFM008) using animal’s behavioral models. The proposed synthetic route to obtain the final compound consisted of three reactions, where the first key intermediate was the phenyl-1H pyrazole (98%) and the second key intermediate was phenyl-1H-pyrazole-4- carbaldeyde (98%) and the final compound, ethyl-4-(( phenyl-1H-pyrazole-4- yl)methyl)piperazine-carboxylate, was obtained in 55% yield. The key intermediates and the final compound were identified by infrared spectroscopy and nuclear magnetic resonance of one and two-dimensional (HSQC and HMBC). Treatment with LQFM008 at doses greater than or equal to 1.1 mmol/kg p.o., s.c or i.p. was neurotoxic, leading to convulsions and death. But the treatment with LQFM008 100, 200 or 400 µmol/kg p.o. did not alter the number of falls in the rota rod, and increased the number of crossings in the center of the open field at 25.46, 24.38 and 28.56%, respectively, and the two highest doses increased the time spent in the center in 47.72 and 45.00%, respectively. All three doses of LQFM008, increased the sleep duration from 107.62±6.30 min (control) to 137.17±10.64, 139.67±10.50 and 171.57±8.32, respectively, without any change in the latency. Treatment with LQFM008 50, 100, 200 and 400 µmol/kg p.o. increased the number of entries in open arm from 36.7±2.86% (control) to 48.5±1.61, 52.8±2.12, 51.1±4.01 and 49.4±4.20%, respectively, as well as increased the time spent in open arm from 31.8±2.33% (control) to 43.3±2.94, 47.8±2.67 and 47.1±5.25%, respectively, and decreased the time spent in central platform from 37.9±2.21% (control) to 29.5±3.01, 28.2±2.90, 26.7±4.70, 26.5±2.01 and 26.4±2.31%, respectively. In the elevated plus maze test, 60 and 90 min after the treatment, LQFM008 200 µmol/kg p.o. increased the number of open arm entries in 63.20 and 60.38%, and the time spent in these arms in 72.39% and 69.31%, respectively, the time spent in central platform was reduced in 28.00% after 15 min, 27.89% after 30 min, 55.32% after 60 min and 45.48% after 90 min. In the light-dark box, 60 and 90 min after the treatment, LQFM008 increased the number of transitions in 95.57% and 141.20%, respectively, and the time spent in the light area in 173.56% after 60 min, and in 216.10% after 90 min. In the elevated plus maze test, treatment with LQFM008 100 µmol/kg p.o. increased the number of entries in the open arms from 25.96±3.01% (control, pre treated with saline i.p. and treated with Tween 2.0% p.o.) to 44.38±3.03%, as well as the time spent in the open arms from 16.60±2.20% (control) to 32.96±2.13% and decreased the time spent in central platform from 51.2±2.56% (control) to 39.1±1.31%. The pre-treatment with a antagonist 5-HT1A NAN-190 1.3 µmol/kg i.p. reverted the effect of LQFM008, decrease the number of entries in open arms to 29.99±3.01%, and the time spent in these arms to 16.78±3.20%, and increase the time spent in central platform in 50.7±2.12%. Animals pre-treated with flumazenil 6.6 µmol/kg i.p. did not differ in any parameters evaluated in relation to controls animals. The anxiolytic-like activity of the compound LQFM008 seems to involve the serotoninergic pathway and but not the GABAA receptor the benzodiazepine sites.
Efeitos da acariçoba (Hydrocotyle umbellata L.) sobre as vias aéreas isoladas de ratos
(Universidade Federal de Goiás, 2022-05-23) Cardoso, Juliana Rodrigues; Rocha, Matheus Lavorenti; http://lattes.cnpq.br/7459866708740096; Rocha, Matheus Lavorenti; Porto, Hellen Karine Paes; Paula, José Realino de
Although the acariçoba Hydrocotyle umbellate L. – Araliaceae has important biological effects, including reports in the literature for the treatment of asthma, its actions on the respiratory system have not been verified. The goals of this work were to determine the effects of the hydro-alcoholic extract of the underground H. umbellata (HEHU) on tracheal smooth muscle isolated from rats. For this, tracheal rings were prepared separately in an organ bath to record the isometric tension. The relaxing effects of HEHU on tracheas, the influence of NO/GCs and COX/prostanoid pathways, K+ channels, extracellular Ca2+ influx and synergism between HEHU and nitric oxide donor drug and β-adrenergic agonist were also evaluated. The results show that HEHU induces airway smooth muscle relaxation in a dose-dependent manner (0-700 µg/mL). The pre-treatment with NO synthase and guanylyl ciclase inhibitors (L-NAME and ODQ, respectively), K+ channel blockes (tetraethylammonium) and COX inhibitor (sodium diclofenac) did not alter the relaxation induced by HEHU. Carbachol-stimulated contraction was impaired by previous treatment with HEHU. The HEHU also inhibited the contraction caused by the influx of Ca2+ stimulated by carbachol and KCl (75 mM). No synergism was observed between nitric oxide-stimulated relaxation or activation of β-adrenergic receptors and HEHU. In conclusion, HEHU induces airways smooth muscle dilatation isolated from rats and the blocking of Ca2+ influx through the cell membrane seems to be the main mechanism of action responsible for this effect.
Fitoquímica, Atividades Antimicrobiana e Antioxidante do Extrato Etanólico e Frações das Folhas de Jacaratia spinosa (Aubl.) A. DC. (Caricaceae)
(Universidade Federal de Goiás, 2015) Oliveira, Joelma Coelho Pina de; Paula, José Realino de; Paula, José Realino de; Borges, Leonardo Luiz; Santos, Pierre Alexandre dos
Jacaratia spinosa (Aubl.) A. DC. is a species of the Caricaceae family, popularly known as “jaracatiá” and “mamão-do-mato”. Widely distributed throughout the country, from the south of Bahia to Rio Grande do Sul. It occurs in rainforest and Cerrado, in gallery forest. It is a big tree to bloom in September and fruiting in January. In folk medicine Jacaratia spinosa is used as antimicrobial, anthelmintic, being displayed against hookworm. It is still used in wound healing and skin ulcerations. Studies in the literature suggest the presence of tannins and phenolic compounds in this plant with possible antimicrobial activity. The objectives of this study were dose the content of phenolic substances, perform the phytochemical from the leaves of Jacaratia spinosa and evaluate the antimicrobial and antioxidant activities of ethanol extract and fractions of leaves Jacaratia spinosa. The polyphenols, tannins and flavonoids content were determined in ethanol extract, acetone extract and its fractions. The antimicrobial activity was conducted on the same samples according to the recommendations of the Clinical and Laboratory Standards Institute (CLSI) to microdilution tests on broth, which allowed to determine the Minimum Inhibitory Concentration (MIC) against strains of Gram positive and Gram negative bacteria. In tests broth dilution also were applied to the determination of the antifungal sensitivity. For the antioxidant activity were used the DPPH methods, Co-oxidation of β-carotene / linoleic acid, FRAP, ABTS and differential pulse voltammetry to verify the antioxidant activity in the ethanol extract and the hexane, dichloromethane, ethyl acetate fractions, and the tannin aqueous fraction concentrated of the J. spinosa leaves. The results indicate that the highest amount of phenolic compounds in the leachate ethanol extract, wherein the total phenol content was found to be 13.86% and 12.72% total tannins (expressed in g tannic acid / 100 g material). In the antimicrobial tests, the tannins aqueous fraction concentrated (FAqCT) showed good activity to Gram-positive, bacteria Micrococcus luteus ATCC 9341 (MIC = 62.5 mg / mL) and Micrococcus luteus ATCC 10240 (MIC = 62.5 mg / mL ). The best result of antifungal activity was to Candida tropicalis ATCC 28707 in tannins aqueous fraction concentrated (MIC = 7.81 mg / mL) and aqueous fraction (MIC = 15.62 mg / mL). The antioxidant activity was tested by five methods, and for the DPPH method, the best result was found in the aqueous fraction (3.29 ol), the FRAP the most significant result was the ethanol extract (19.49 micromols Fe 2+ / mg) . In ABTS and β-carotene / Linoleic Acid methods the best results were to butanol fraction, 4.33 micromol Trolox / g for the ABTS method, and 98.42% for the β-carotene / linoleic acid. The differential pulse voltammetry showed the best results for the butanol fraction and ethyl acetate fraction, the voltagramas showed oxidation and reduction, indicating regenerative capacity. Therefore the data indicated that the leaves of Jacaratia spinosa are sources of phenolic compounds, making potential for use as antifungal and natural antioxidant.
Obtenção de formulações fitocosméticas com atividade fotoprotetora a partir de pterodon sp. vogel fabaceae (sucupira)
(Universidade Federal de Goiás, 2015-03-24) Carvalho, Wannessa Lenyse Rocha de; Diniz, Danielle Guimarães Almeida; Bara, Maria Teresa Freitas; Bara, Maria Teresa Freitas; Zampieri, Ana Lúcia Teixeira de Carvalho; Taveira, Stephânia Fleury
The use of natural products photoprotective cosmetic formulations have attracted consumers. This study aimed to get formulations with sunscreen and antioxidant activity, from the merger of the oil and hydroalcoholic extract of Pterodon sp. in semi solid formulations (Focus Gel®, LANETTE®, Polowax®) containing chemical filter Eusolex 2292®. Initially it was held potential of the evaluation study sunscreen with oil resin Pterodon sp. incorporated at a concentration of 15% in the formulation containing 0.06% of chemical filter Eusolex 2292. Subsequently followed investigations using the hydroalcoholic extract of Pterodon sp. (EHS) obtained by water bath under reflux at 50 ° C. Determined the sun protection factor extract solubilized in absolute ethanol and when incorporated in semi-solid formulations (Focus Gel®, LANETTE®, Polowax®) with 0.01% Eusolex 2292. This extract was characterized chemically-evaluating physical parameters density, solid content, moisture content, chromatographic profiles and determination of antioxidant activity by the methods of DPPH and FRAP. Finally we conducted a preliminary stability study only formulations containing extract, which were stable against exposure to extremes of freezing and thawing and thermal stress, with statistical comparison (p <0.05) in all evaluated parameters (pH , density, viscosity, electrical conductivity and FPS). The formulation containing SPF results Pterodon sp oil. was obtained FPS> 5.0, formulation containing the chemical filter FPS> 6.0 and formulation containing oil and chemical filter FPS> 12.0. For formulations containing extract incorporated in the bases (Focus Gel®, LANETTE®, Polowax®) were respectively found FPS 9.44 ± 0.508, 14.72 ± 0.304, 14.22 ± 0.503 and formulations containing chemical filter presented FPS of 10.52 ± 0.676, 8.75 ± 0.04, 8.18 ± 0.172 and formulations containing chemical extract and filter was obtained FPS of 27.74 ± 0.756, 24.77 ± 0.613, 23.87 ± 0.259 respectively. The data from the characterization of the extract were 0.910 ± 0.003 density, pH 6.05 ± 0.456, solids 9.73 ± 0.04, moisture content 92.97% ± 0.568, chromatographic profile for CCD indicative of the presence of flavonoids and phenolic acids. It was possible to verify that the SPF values were maintained within 30 days. It was determined the antioxidant activity by the methods of DPPH and FRAP and EC50 values were found 19.3 ± 1.5 uL / mL and 14 880 uM / mL. It was first confirmed the FPS additive effect in formulations with oil and Pterodon sp extract. in semisolid formulations. The analysis allowed confirming the EHS antioxidant activity, tending towards fotoquimioprotetora activity after the preliminary stability study confirmed the achievement of stable formulations. It concludes that the EHS has potential for the development of photoprotective cosmetic formulations.
Estudo comparativo da liberação e permeação cutânea do clotrimazol em formulações semissólidas disponíveis no mercado farmacêutico brasileiro
(Universidade Federal de Goiás, 2015-03-30) Mendes, Patricia Hauschildt de Oliveira; Lima, Eliana Martins; Lima, Eliana Martins; Gratieri, Taís; Alves, Carina Pimentel Itapema
Clotrimazole (CTZ) is an antifungal drug used to treat superficial mycoses, and there are many topical drug products with clotrimazole approved in Brazil. The generic drugs can be registered in Brazil with formulations qualitative and quantitative different from the reference list drug, and the chemical composition of formulations is determinant for drug release from the drug product, for percutaneous absorption and to exert pharmacological effect, so the evaluation of in vitro drug release and skin permeation of CTZ on generic drug products in comparison with the reference list drug Canesten® show relevance to evaluate the generic drug products equivalence. The aim of this study was to compare the generics A, B, C and D and the reference list drug through in vitro drug release and skin permeation to evaluate the formulations interference on drug release and skin permeation as well as the evaluation of in vitro drug release as a regulatory tool. It was necessary the development and validation of the analytical quantification method of CTZ. The method showed linearity (0,8 µg/mL a 20 µg/mL), selectivity for peak purity evaluation, no interfering dermal and epidermal and also proven to be precise and accurate. The in vitro drug release and skin permeation were performed in vertical diffusion cell “Franz” type of 1,86 cm2 diffusional area. The in vitro drug release studies were performed according the USP 37, used cellulose ester membranes, receptor fluid sodium lauryl sulfate 1,5% and the assay was conducted at 32°C. The flux results from in vitro drug release of generics A, B, C and D in comparison with Canesten® during 6 hours of the studies are not within 75%-133,33%, corresponding the 90% confidence interval, therefore in accordance to the method, the generics and reference cannot be considered similar. The in vitro skin permeation studies were carried out using 750 µm dermatomized pigs ears skin, lasted 24 hours and the results showed that the CTZ epidermal penetration in generic D was statistically different from the other drug products studied; there was even dermal permeation, which was not showed for the other drug products. The pH and droplet size distribution were also evaluated in all formulations, however it was not possible to verify the influence of these parameters on in vitro drug release and skin permeation, whereas the generic D had the highest droplet size and in vitro skin permeation 2 times higher than the other tested drug products. The results of the studies demonstrated the influence of formulations on in vitro drug release and skin permeation of CTZ and the possibility of using the in vitro drug release method as a regulatory tool for approval and post approval changes of topical generic drug products.
Preparação de metabólitos humanos do montelucaste através da bioconversão
(Universidade Federal de Goiás, 2012-02-17) Braga, Rodolpho de Campos; Oliveira, Valéria de; Oliveira, Valéria de; Lima, Eliana Martins; Magalhães, Mariana Torquato Quezado de
The biotechnological processes based on the use of microbial enzyme arsenal have great application in the pharmaceutical industry. Microbial models may represent an alternative to using animals in metabolism studies in mammals, providing valuable information on drug metabolism. Montelukast promotes increased lung function and is one of the most prescribed drugs for the treatment of asthma. In 2010, ranked fifth among the best-selling drugs in the world. Considering that in 2012 its patent will expire, it’s necessary the determination of its metabolites, to conduct trials to evaluate the therapeutic efficacy both in the stage of pharmaceutical equivalence and bioequivalence. The aim of this work was the application of bioconversion for the production of human metabolites of montelukast using filamentous fungi as microbial model of mammalian metabolism. Twenty-five microorganisms strains were examined for their ability to transform the antiasthmatic drug montelukast to the phase I metabolites that are found in humans. Metabolomic fingerprinting was used to select the strains that can mimic human metabolism of montelukast. Biostatistical methods were applied to classify the twenty-five strains of microorganisms regarding the type of reaction and products formed. We developed analytical separation strategies and purification of the metabolites using preparative high-performance liquid chromatography (HPLC). Cunninghamella elegans ATCC 36112 and Beauveria bassiana IP98 produced the major variety and quantity of metabolites and were selected to scale up the preparation of the metabolites of montelukast. Seven oxidation metabolites were identified using LC-MS and 1 H and 13C-NMR spectroscopy. The metabolite carboxylic acid (M4) was the major product being converted by both mammalian and microbial systems. Other metabolites were identified as diastereomeric sulfoxides (M2a and M2b), 11-hydroxy (diastereomers of a benzylic alcohol, M5a and M5b), and 3-hydroxy (diastereomers of a methyl alcohol, M6a and M6b). Of the twenty-five strains examined, seventeen transformed montelukast to the main human metabolite carboxylic acid (M4), and the majority also produced the diastereomeric methylhydroxylated metabolites (M6a and M6b). The results support the potential of using the fungus Cunninghamella sp., which can transform a broad range of xenobiotic compounds in an analogous fashion to mammals. The up scaling of the biotransformation may also have potential as a method of generating the metabolites as analytical standards.
Obtenção e caracterização de extrato seco padronizado das folhas de goiabeira (psidium guajava l. cultivar pedro sato, myrtaceae)
(Universidade Federal de Goiás, 2012-02-24) Oliveira, Thiago Levi Silva; Conceição, Edemilson Cardoso da; Paula, José Realino de; Paula, José Realino de; Paula, Joelma Abadia Marciano de; Verde, Giuliana Muniz Vila
Psidium guajava L. is a plant the Myrtaceae family leaves are popularly used to treat cramps and diarrhea. The chapter sought to perform a quality control of dust from the leaves and get the standardized ethanol extract of P. guajava Pedro Sato cultivar, using ellagic acid as a marker of the process and carried out chemical analysis of soil and plant tissue. The investigation of the macroscopic and microscopic leaf powder showed compliance with the specifications described in the monograph of the plant of Brazilian Pharmacopoeia 4th Edition. The result of particle size distribution, content of total ash, acid insoluble ash, volatile content, swelling index and content of ellagic acid are respectively 391.548 ± 1.532 mm, 6.266 ± 0.011%, 0.003 ± 0.002%, 6.666 ± 0.057%, 4.733 ± 0.152 ± 0.006% and 0.04%. %. The plant tissue and soil present micronutrients such as copper, iron, zinc and manganese which are needed for a composition rich in phenolic compounds. The extract presented pH of 5.61 ± 0.02, relative density of 1.01 ± 0.001 mg / mL, viscosity of 15 ± 0,001 mPas, solids content of 4.73 ± 0.03% and ellagic acid content resulting from hydrolysis of ellagitannins 0.50 ± 0.02. The antimicrobial activity of ethanol extract was determined by the Minimum Inhibitory Concentration (MIC) and showed moderate activity (MIC between 100-500 mg / mL) against the fungi Cryptococcus neoformans, Cryptococcus gattii and Cryptococcus neoformans L2. Chapter 2 describes the extraction and characterization of the dry extract of P. guajava Pedro Sato cultivar by spray drying technique and evaluates the use of adjuvants such as colloidal silicon dioxide, starch and maltodextrin in obtaining this intermediate product, following a full factorial design 23 + 3. The data obtained indicated that the dried extracts of both adjuvants showed levels of volatile and water activity below 5% (w / w) and 0.5, respectively. These results indicate improved microbiological stability of the dried extract. The micrographs showed particles of variable size and irregular shape. Analysis of Variance (ANOVA) revealed that the proportion of adjuvant, inlet temperature air drying and flow of extract and some of its interactions, power significantly affect the amount of ellagic acid, and the best condition to be used to obtain standardized dried extracts of P. guajava involves the use of adjuvant such as silicon dioxide 20%, flow 2mL/min extract power and temperature of the incoming air drying 110 ° C. Chapter 3 sought to establish and validate a methodology able to identify and quantify ellagic acid amid a complex mixture of herbal extract of P. guajava cultivar Pedro Sato, employing high performance liquid chromatography (HPLC). This validation was used as mobile phase solvent A - 50% methanol and B - 50% aqueous solution of ortho-phosphoric acid 0.5%, injection volume 10 mL, isocratic flow of 1mL/min-1 detector, diode array (PDA), λ = 252.3 nm, C18 column chromatography (RP18) 5 mm (4.6 x 155 mm). Subsequently, the methodology was co-validated by assessing the selectivity and accuracy parameters following the same chromatographic conditions of validation for ethanol extract. The results of the validation proposal for the determination of ellagic acid in ethanol extract indicated that the method is selective, linear over the concentration range of 4-64 mg / mL, robust and has a sensitivity of detection and quantification.
Desenvolvimento e caracterização de lipossomas recobertos com quitosana para administração intranasal de montelucaste sódico
(Universidade Federal de Goiás, 2010-12-17) Nascimento, Thais Leite; Lima, Eliana Martins; Lima, Eliana Martins; Mosqueira, Vanessa Carla Furtado; Taveira, Stephânia Fleury
Chitosan is a biodegradable, non-toxic polymer, with favorable biological properties, that presents great potential for being utilized in safe and efficient formulation for intranasal administration. Sodium montelukast (MTK) is a drug which utilization is well known as an auxiliary in the treatment of asthma. However, oral therapy with MTK presents disadvantages that can potentially be circumvented by its administration via the nasal route, but its utilization through this pathway had not yet been investigated. The objective of this work was to develop chitosan-coated liposomes containing MTK for administration trough the nasal route, and characterize the obtained liposomes in terms of encapsulation efficiency, stability and drug release. The in vivo plasma concentration profile was also studied, as the histopathological characteristics of the nasal cavity and trachea after nasal administration of the chitosan-coated liposomes in healthy rats, comparatively to the administration of the drug suspension. The liposomal vesicles obtained were about 150nm in size. The increase in the diameter after coating with chitosan showed that the surface of the liposomes was coated, and this result was confirmed by the change in the zeta potential from negative before coating to positive after coating. MTK encapsulation efficiency in the liposomes was superior to 98% due to the lipophilicity of the MTK molecule, and the encapsulation efficiency remained high during the stability study. The pH and zeta potential results during the stability study suggest that the phosphatidylcholine of the non-coated liposomes was degraded during the analyzed stability time, thus forming a carboxylic acid that was responsible for the pH augmentation and zeta potential reduction. Meanwhile the chitosan protected the coated liposomes from this degradation. The in vivo study revealed that the administration through the nasal route prolonged the MTK plasma concentration profile compared to the oral route, and that the release of MTK from the liposomes appeared to be more sustained then the drug in suspension. No alteration in the nasal or tracheal epithelium was observed during the morphological analysis. The sustained release of MTK caused by the nasal administration of the liposomes when compared to the free drug administration suggest that this carrier system and this route of administration present potential benefits for the asthma treatment with MTK.
Avaliação das atividades hepatoprotetora e antioxidante; e da toxicidade aguda do extrato aquoso das folhas de apeiba tibourbou aubl (tiliaceae) em ratos (rattus norvegicus) e camundongos (mus musculus)
(Universidade Federal de Goiás, 2012-08-31) Melo, Dorcas Fernandes dos Anjos; Cunha, Luiz Carlos da; Cunha, Luiz Carlos da; Costa, Renata Mazaro e; Bozinis, Marize Campos Valadares
Liver performs many biological functions, especially the metabolism detoxification of xenobiotics and endogenous substances. However, this makes it a target for toxicants, which damage the liver’s production, mostly of reactive oxygen substances. In this context, the present study aimed to investigate, in vivo, the hepatoprotective and antioxidant activities of Apeiba tibourbou Aubl (Tiliaceae), and acute toxicity in vivo (mice and rats). Acute toxicity was measured with the aqueous extract from the leaves of Apeiba tibourbou (EAT) in mice (300 and 2000 mg.kg -1 , p.o.) and rats (2000 mg.kg -1 , p.o.). Hepatoprotective and anti-oxidant activities were performed in mice pretreated with EAT (400, 200, 100, 50 or 25 mg.kg-1 , p.o.) and 18 mg.kg-1 (p.o.) rosmarinic acid (RA), and subsequently exposed to CCl4:oil olive oil (1:1, 2 mg.kg -1 , i.p). The markers (AST, ALT, ALP and GGT and MDA) were measured in plasma, and (MDA) in liver lysate. The EAT, the acute toxicity test showed no signs of intoxication and even physiological changes, with LD50 (median lethal dose) estimated greater than 2000 mg.kg -1 (GHS Class 5 of the OECD). In the hepatoprotective test, higher doses (400 and 200 mg.kg -1 ) did not protect the liver from aggression produced by CCl4. However, lowest doses (50 or 25 mg.kg -1 ), in particular of 50 mg.kg -1 decreased by 31.50% and 20.63% concentration of AST and ALT, respectively, while the dose of 25 mg.kg -1 decreased by 57.18% compared to the GGT positive control. In lysate of the liver, the EAT showed only moderate antioxidant effect at the dose of 50 mg.kg -1 . Rosmarinic acid demonstrated antioxidant activity and hepatoprotective. In conclusion, the EAT in low doses, was able to protect the liver from damage caused by CCl4, showed antioxidant activity and has moderate trend in high doses, possibly be potentiator and/ or inducing liver damage.
Fitoquímica e atividade antimicrobiana de Campomanesia adamantium (Cambess.) O. Berg (Myrtaceae)
(Universidade Federal de Goiás, 2014-12-15) Sá, Stone de; Paula, José Realino de; Paula, José Realino de; Santos, Pierre Alexandre dos; Morais, Sandra Ribeiro
Campomanesia adamantium (Cambess.) O. Berg is a native fruit species of the Cerrado biome, belonging to the Myrtaceae family, popularly known as guabiroba-do campo. Pharmacological studies and popular use of the plant indicate great antimicrobial potential. The present study aimed to phytochemical screening of the species, and to evaluate the antimicrobial profile. In phytochemical screening were used chromatographic and spectrometric techniques and for antimicrobial activity, microdilution test broth. It was possible to evaluate chemical composition and percent yield of the essential oil of leaves and flowers Campomanesia adamantium and volatile terpene compounds of the hexane fraction. In addition, novel compounds were identified in species such as estictano-3,22-diol, hydrolyzable tannins precursors such as gallic acid and valoneico acid. The phytochemicals results contribute to the scientific validation of etnomedicinal use of the species also add phytochemical information that cooperate for the study of genus. To evaluate the antimicrobial activity test was used microdilution broth, which allowed to determine the minimum inhibitory concentration (MIC) against strains of Gram positive and Gram negative bacteria and fungi Evaluation of the antimicrobial activity of C. adamantium, obtained in the present study revealed great potential antibibacteriano (hexane fraction) and antifungal (aqueous fraction, concentrated aqueous fraction of tannins and the compound isolated vanoleico acid). The isolated valoneico acid contributes to the antifungal activity of the extract.
Mecanismos envolvidos na atividade gastroprotetora do extrato hexânico das folhas de celtis iguanaea (JACQ.) sargent (cannabaceae)
(Universidade Federal de Goiás, 2012) Martins, José Luís Rodrigues; Costa, Elson Alves; Costa, Elson Alves; Menegatti, Ricardo; Safadi, Giuliana Muniz Vila Verde
Celtis iguanaea, is popularly known as esporão-de-galo, tela, taleira, sarã, gurrupiá and grão-de-galo. It is about 6-9 feet high with rounded crown and long flexible branches armed with thorns. Ethnopharmacological study of this species shows the use of its leaves in the form of tea for treating body aches, chest pain, asthma, colic and indigestion. Previous results from our laboratory have shown gastroprotection and anti-ulcerogenic activities of the aqueous leaf extract and the n-hexane fraction obtained after fractionation of the ethanol leaf extract of esporão-de-galo in different models of gastric ulcers. For this purpose, samples of Celtis iguanaea leaves were collected from Hidrolandia-GO. The voucher specimen was deposited in the Herbarium of UFG (N°. 40110). Male Swiss albino mice, weighing between 35-40 g and frogs (Rana castebiana) of both sexes, weighing between 80-120 g were used. In general test of pharmacological activity, no significant alteration among animals treated orally with EHEG (10, 30, 100, 300 and 1000 mg / kg) or vehicle (2% Tween 80, 10 mL / kg. No evidence of significant effect on CNS and antioxidant activity was recorded with EHEG in vivo and in vitro respectively. On the other hand, EHEG showed anti-ulcerogenic activity in acute ulcers (induced by indomethacin, 75% ethanol and pylorus ligation) and chronic gastric injury induced by acetic acid. The EHEG administered orally increased mucus adhered to the gastric mucosa. Involvement of the α2 receptor in the gastroprotection effect exerted by the EHEG was assessed with the yohimbine (α2 adrenergic receptor antagonist). This compound reduces effect of EHEG. The study of antisecretory activity in isolated frog mucosa in Ussing chamber showed that EHEG reduces basal secretion of gastric acid up to 98.27%, and reduced ACh - stimulated secretion by 39.45%. A similar effect was observed in the pyloric ligation model in rodents, where we observe systemic activity of EHEG. The EHEG also reduced volume, free acidity and total acidity of gastric acid secretion induced by various secretagogues. The results of this study suggest that EHEG has gastroprotective activity by a mechanism that involves in part, anti-ulcerogenic, antisecretory and an increase in mucus production.
Desenvolvimento de pellets mucoadesivos contendo pectina de solanum lycocarpum st. hill tiolada
(Universidade Federal de Goiás, 2015-07-28) Martins, André Luiz Lopes; Marreto, Ricardo Neves; Marreto, Ricardo Neves; Taveira, Stephânia Fleury; Fernandes, Kátia Flávia
The development of mucoadhesive systems can facilitate control of inflammatory bowel diseases by increasing local drug bioavailability. Pectin, a first generation mucoadhesive natural polymer, when subjected to the thiolation reaction is more mucoadhesive by the insertion of thiol groups to their structure. In particular, pectin extracted from Solanum lycocarpum St. Hill (lobeira) has interesting properties for pharmaceutical use. In this work, citrus pectin and pectin extracted from Solanum lycocarpum were chemically modified by reaction with thioglycolic acid and characterized by molecular weight and amount of thiol groups. Furthermore, ketoprofen pellets containing natural or thiolated pectins were developed by extrusion and spheronization technique, and subsequently the mucoadhesion evaluated in intestinal porcine ex vivo model. The molecular weights of citrus pectin (121 kDa) and pectin extracted from S. lycocarpum (57.5 kDa) were increased after thiolation reaction (thiolated citrus pectin 137 kDa and pectin extracted from S. lycocarpum, 64.5 kDa). In addition to molecular weight, the degree of methoxylation of different pectins (68% and 35% for citrus pectin and extracted from S. lycocarpum, respectively) exerted influence on the conditions necessary for the satisfactory development of the pellets.The two thiolated pectins presenteds 0.69 mM thiol / g polymer groups. For the development of ketoprofen pellets containing citrus pectin it was necessary to add PVP K-30 in the wetting liquid, resulting in the formation of spherical products (projected spherical shape; sphericity of 0.83). The pellets were obtained with ratio of wetting liquid: solid of 1: 1. The pellets containing other pectins were developed based on the formulation containing citrus pectin. For those containing thiolated citrus pectin the ratio of wetting liquid: solid necessary for obtaining spherical pellets of appropriate size was 0.75: 1. The pellets containing pectin extracted from S. lycocarpum required smaller amount of wetting liquid (0.5: 1), very probably due to higher solubility of this polymer in water. The pellets containing the thiolated pectin extracted S. lycocarpum showed the same behavior of their peers not thiolated.The mucoadhesion testing of the pellets showed time increased adherence onto porcine mucosa when unmodified pectin S. lycocarpum was incorporated, which shows the highest adhesive strength of this material when compared with citrus pectin. The thiolation of pectins significantly increased mucoadhesion of the pellets with remaining 60% of the units on the membrane surface after 480 minutes of testing. There was no statistical difference between the pellets containing thiolated citrus pectin and thiolated pectin from S. lycocarpum. The overall results showed that the pectin from S. lycocarpum showed favorable technological properties to obtain pellets by extrusion-spheronization process, and the pellets obtained were more mucoadhesive compared to pellets containing citrus pectin. Finally, the thiolation reaction proved to be an effective strategy to improve mucoadheviness of the pellets. Thus, it was concluded that the sustainable exploitation and utilization of the pectin from S. lycocarpum is a strategy with great economic and technological potential.
Isolamento, quantificação e avaliação das atividades leishmanicida e tripanocida de furanoditerpenos do oleorresina de Pterodon spp. Vogel (Fabaceae)
(Universidade Federal de Goiás, 2014-02-28) Oliveira, Leandra de Almeida Ribeiro; Bara, Maria Teresa Freitas; Bara, Maria Teresa Freitas; Paula, Joelma Abadia Marciano; Menegatti, Ricardo
Pterodon (Fabaceae) plant species known as white “sucupira” are widespread in Brazilian savannah. Their therapeutic use is mainly due to the analgesic and antiinflamatory properties, essentially attributed to the furanic diterpenes with vouacapanic skeleton, found in their fruits. Researches carried out with diterpenes from other plant species have shown promising activity against the causative agents of neglected diseases. It is necessary to implement a HPLC method for the achievement and quantification of these diterpenes, because the methods available to date are multi-step and laborious. This research aimed to isolate (chapter I) and quantify furanic diterpenes from sucupira’s fruit by HPLC (chapter II) and assess their in vitro leishmanicidal and trypanocidal activity (chapter III). First, the oil was fractionated through liquid-liquid partition, and so it was undergone to preparative reverse phase HPLC separation. Three compounds were isolated: two new furanic diterpenes: 6α-acetoxy- 7β,14,18-trihydroxyvouacapan and 6α-acetoxy-7β,14-dihydroxyvouacapan and methyl-6α- acetoxy-7β-hydroxyvouacapan-17β-oate (MAHV), as established by NMR and mass spectroscopy. MAHV, the major compound in the oil, and β-caryophyllene (Sigma®) were chosen as chemical markers for the quality control of the oil, by reverse phase HPLC. A method was developed and validated. Mobile phase consisted of a gradient of acetonitrile, acidified with phosphoric acid 0.2 % (v/v), methanol, and phosphoric acid 0.5 % (v/v) in water, at 1 mL/min. A C18 column at 30ºC was used. Chromatograms were recorded at 210 nm. MAHV was present in the sample at the concentration of 15.98% (w/w), and β- caryophyllene at 8.01% (w/w). The oil, the isolated MAHV and the compound methyl-6α-7β- dihydroxyvouacapan-17β-oate (MHV), a synthesized furanic diterpene also present at sucupira’s fruit, was assessed against the promastigote form of the Leishmania braziliensis e Leishmania amazonensis species, and against the epimastigote form of the parasite Trypanosoma cruzi, through the in vitro MTT colorimetric assay. The MAHV revealed to be more active than both the MHV and the oil. It showed an EC50 < 30 µg/mL at all of the assays. The results indicated the potential of the diterpenes of sucupira’s fruits in the control of neglected diseases, as leishmaniosis and trypanosomiasis. Further studies should be carried out to investigate the cytotoxicity of these compounds in mammalian cells.

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