Mestrado em Ciências Farmacêuticas (FF)

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Desenvolvimento de carreador lipídico nanoestruturado contendo filtro UV avobenzona
(Universidade Federal de Goiás, 2022-09-30) Sousa, Isabelly Paula; Silva, Luís Antônio Dantas; http://lattes.cnpq.br/0999722983963121; Diniz, Danielle Guimarães Almeida; http://lattes.cnpq.br/6801755844853116; Diniz, Danielle Guimarães Almeida; Silva, Lorena Maione; Mendanha Neto, Sebastião Antônio
Introduction: Avobenzone (AVB) is an organic filter, acting in the ultraviolet (UV) A spectrum. It is a cosmetic ingredient that presents photo-instability, impairing its photoprotective activity. For AVB photoprotection, its molecule must be in conformation, however, exposed to a UV photoisomerization it undergoes, passing to a keto form, which has no protection against UVA radiation. Objective: To develop and characterize a nanostructured lipid carrier (NCL) containing AVB and to evaluate its photostability. Methods: The High Performance Liquid Chromatography (HPLC) method was validated to evaluate the AVB. The AVB compatibility with the selected components was the premeans evaluation of thermal analysis of spectrogravimetry and Fourier transformed infrared (FT-IR) porscopy. AVB solubility was for 24 hours by temperature test, under temperature of 37°C, for 24 hours. Afterwards, the components for the composition of the recommended formulation were selected as reasons according to the literature. For the maintenance of the CLN, the method of inversion of phases with application of microfluidization was used. To characterize the performance of the tests: preliminary stability for 14 days, average stability and follow-up of the formulation, evaluation of polydispersity, 30 days, evaluation of pH parameters, particle size, index index (Pd) and content. The encapsulation efficiency (EE%) was performed by the indirect method. The photo stable study lasted 24 hours and consisted of the evaluation of the NLC containing AVB under UVA radiation. The surface of the nanoencapsulated skin surface, AV was projected for 24 hours, using the Franz interface. Results and discussions: the studies of definition of average size, corroborate for the definition of the components of the CLN, isopropyl myristate, 80 and span 85. After the conclusion of the white CLN, the results of size and PdI of 145.9 ± 57 were obtained. .32 nm and 0.196 ± 0.04, respectively. When an AVB was incorporated into the CLN, 135.77 ± 7.27 nm of mean size and 0.150 ± 0.09 of PdI were obtained. For EE%, the value of 72.82± 1.81% of asset encapsulation was generated. Subsequently, the capacity test was performed, to which the solubilized AVB test was presented and the solubilized AVB presentation of solubilized AVB was presented and tested in how much AVB sampled the sample not presented to exposure. The AVB, did not show permeation of clothes in the skin CLN, having its actions in the skin of the CLN, having its skin. Conclusion: Thermal studies will allow the proper selection of formulation constituents. The functional treatment system developed, with protected CLN photo treatment features, and CLN photo treatment features protective conditions, thus, face to face UV. As for its safety, it is seen that the AVB remained mostly retained in the stratum corneum, it did not present permeation to the skin.
Perspectivas em pesquisas sobre o gênero Campomanesia; estudos fitoquímicos e investigação de atividades biológicas em Campomanesia guazumifolia (Cambess) O. Berg - Myrtaceae
(Universidade Federal de Goiás, 2022-07-05) Steckelberg, Rosa Maria de Brito; Paula, José Realino de; http://lattes.cnpq.br/3191837532986128; Paula, José Realino de; Cardoso, Cláudia Andrea Lima; Morais, Mariana Cristina de
Introduction: One of the challenges of public policies to encourage the use of herbal medicines is the inclusion of more native species, such as those of the Campomanesia genus, among the options for taking advantage of Brazilian biodiversity. Identifying research trends on the genus and species may arouse the interest of researchers so that more native species, such as Campomanesia guazumifolia (C.g) can be integrated into health systems where exotic species predominate. Objectives: To evaluate the scientific production of the genus Campomanesia and main species, especially C.g, in which the leaves of cultivated specimens were the object of pharmacognostic studies, phytochemical profile, essential oil characterization, antioxidant potential and biological activities. Methodology: Scientific production on the genus and species was evaluated using scientometric tools using the Web of Science database and the VOSviewer application. The experimental part consisted of traditional pharmacognostic studies; the essential oil was characterized by means of gas chromatography coupled to a mass spectrometer (GC-MS); the antioxidant potential was evaluated by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method; larvicidal activity by mortality of Aedes aegypti L3 larvae and the antimicrobial activity was tested by a broth microdilution test. Results and discussion: Brazil leads research on gender and most of them occurred after the implementation of herbal medicine policies. C.g was the species with the highest proportional volume of publications in the last 5 years. The species presented flavonoids, tannins, saponins and triterpenes in its composition. The major compound of the essential oil (EO) was β-caryophyllene. The species showed good antioxidant (leaf extract and powder), larvicidal (EO) and antimicrobial activity, mainly against Candida sp and Micrococcus luteus strains. Conclusions: C. guazumifolia is a promising species for further research on biological activities and other studies that can support the traditional use and also as a phytomedicine.
Validação de técnica analítica em LC-MS/MS para quantificação da ivermectina em plasma canino
(Universidade Federal de Goiás, 2022-11-17) Toledo, Ney Ramos; Cunha, Luiz Carlos da; http://lattes.cnpq.br/6349547031976679; Cunha, Luiz Carlos da; Rodriguez Salazar, Vânia Cristina; Rodrigues, Caroline Rego
Ivermectin is an antiparasitary drug with endectocide activity, which is derived from avermectin, a macrocyclic lactone isolated from actinomycete Streptomyces avermectinus. This study aims to validate a new ivermectin’s analytical methodology, in dog plasma, with pharmacokinetic and bioavailability studies as objectives, regarding the still necessary clinical studies in dogs for veterinary products approval. Moreover, the optimized and developed method had as objective to have analytical benefits over the existent methods. The chosen analytical technique was High Performance Liquid Chromatography coupled to Mass Spectrometry (HPLC-MS/MS) with a Zorbax® C18 column from AgilentTM and, as mobile phase, 90:10 (Methanol:water) with 0,1% formic acid and 5 mM ammonium formate being added to aqueous and organic phases. The internal standard of choice was abamectin due to high similarity with ivermectin. Analytical validation was performed through a calibration curve with 7. Precision and accuracy intra-day and inter-day results were obtained through triplicate concentrations of quality control samples. Intra-day precision had 4,0 – 14,9% CV values and inter-day 6,4 – 11,6%. Intra-day accuracy had values between 95,0 and 114,61% and inter-day 98,1 and 109,0%. Stability studies had values between 88,8 and 98,2%. All results agree with parameters stablished by RDC nº27/2012. The analytical technique was used to determine ivermectin’s p.o. kinetic profile of a 2-year-old female mongrel dog weighting 14 kg, and proved adequate to quantificate typical concentration variations of pharmacokinetic data: Cmáx = 17,85 ng/mL; Tmáx = 1,00 h; AUC0-inf_obs = 2113,21 ng/mL*h; Vd = 41,24 L/Kg. The optimized and developed method had reduced use of organic solvents in its extraction method, faster analytical run, lower sample volume and can be used in pharmacokinetical studies.
Modelos de aprendizado de máquina para avaliação preditiva de toxicidade dérmica aguda de compostos químicos
(Universidade Federal de Goiás, 2020-12-16) Hall, Steven Umualê Silva; Alves, Vinicius de Medeiros; http://lattes.cnpq.br/7314022014345242; Andrade, Carolina Horta; http://lattes.cnpq.br/2018317447324228; Andrade, Carolina Horta; Scotti, Marcus Tullius; Neves, Bruno Junior
Introduction: Acute dermal toxicity is a collection of adverse effects that a substance can cause in the first 24 hours of dermal exposure to this chemical. This toxicological property using animals by estimating the lethal dose (LD50), the dose required to kill 50% of individuals of a test population. However, due to public and political pressure on issues related to animal testing, alternative methods are becoming essential to reduce the costs and number of test animals. Computational methods such as machine learning methods have been presented as a reliable alternative to animal testing for hazard assessment. Objectives: The main goal of this study was to develop machine learning models capable of predicting acute dermal toxicity of chemicals, and to make these models available in an online server for the scientific community. Methodology: Acute dermal toxicity datasets where compiled from literature and rigorously curated. Classificatory and multi-classificatory QSPR (Quantitative Structure-property Relationships) models were developed using molecular descriptors and machine learning algorithms and where then used to screen the CosIng library as a case study. Results and discussion: After data curation, 2,622 compounds were kept in the dataset (384 toxic and 2238 non-toxic). To avoid developing biased models, the dataset was balanced, and 768 (384 toxic and 384 non-toxic) were kept for the modeling. The best classificatory models were generated with random forest algorithm and achieved CCR of 79%, SE of 80%, SP of 78%. The best models were used in an integrated hierarchical strategy that obtained ACC= 74% and Recall =74%. In total 33 compounds from CosIng were correctly predicted as toxic. Conclusions: The developed QSPR models were robust and predictive and are capable of predicting acute dermal toxicity efficiently. These are thde first models developed for this endpoint which passed by a rigorous data curation and validation process, being valuable in the prediction of toxicity from new untested compounds. These models are available in a web server through the address https://stoptox.mml.unc.edu .
Desenvolvimento de nanopartículas híbridas polímero lipídeo contendo cloridrato de topotecano
(Universidade Federal de Goiás, 2012-04-24) Silva, Emmanuelle de Jesus; Marreto, Ricardo Neves; http://lattes.cnpq.br/6127043775208484; Marreto, Ricardo Neves; Magalhães, Nereide Stela Santos; Lima, Eliana Martins
Topotecan (TPT) is a water-soluble derivative of camptothecin clinically approved for treatment of ovarian cancer and lung cancer. This drug acts by inhibiting topoisomerase I, an enzyme related to nuclear DNA replication. Thus, TPT is a drug that acts in S phase of cell cycle and, therefore, requires prolonged contact with its biological target to achieve maximum effectiveness. Nanoencapsulation of TPT can prolong its contact with therapeutic target and maximize clinical efficacy. Another characteristic to highlight is that lactonic form of topotecan, active form, undergoes rapid hydrolysis pH dependent when in plasma pH, with rapid structure formation of carboxylate, which is less active. Lactonic ring may be stabilized by drug incorporation into lipid matrices, because lipid matrix provide insulation of surrounding aqueous medium. Polymer-lipid hybrid nanoparticles (PLN) are systems designed to enlarge incorporation of hydrophilic drugs into lipid matrices, as well as to extend control of drug release from such systems. In this paper, polymer-lipid hybrid nanoparticles containing topotecan were prepared by mixing the lipids stearic acid, dodecanoic acid and oleic acid using dextran sulfate as polymeric component. These PLN were compared to nanostructured lipid carriers (NLC), with same lipidic components, but obtained without polymer addition. Both, PLN and NLC were obtained by dilution technique of microemulsion and then characterized by their size, zeta potential, encapsulation efficiency, drug loading, in vitro release and drug chemical stability. Selected PLN showed drug loading of 5.48%, average diameter of 121.75 nm and polydispersity index of 0.277. Encapsulation efficiency was high (97.27%) as well as yield process (94.12%). PLN released 4.48% of drug in 24 hours, while the nanostructured lipid carriers (NLC) released five times more drug in that period (22.49%). However, release rate of PLN can be controlled by amount of ions in the medium and adding calcium chloride greatly increased release of topotecan from PLN. Both, NLC and PLN significantly increased topotecan stability when compared to free drug and PLN were superior due to possibility of controlling release and because of its greater efficiency in obtaining by dilution technique of microemulsion.
Utilização do óleo obtido de resíduos agroindustriais de goiaba (Psidium guajava L.) na nutrição de poedeiras comerciais
(Universidade Federal de Goiás, 2014-10-31) Barbosa, Nathalia Pedroso; Stringhini, Jose Henrique; http://lattes.cnpq.br/8505634095383289; Mello, Heloísa Helena de Carvalho; http://lattes.cnpq.br/5510965166352073; Conceição, Edemilson Cardoso da; http://lattes.cnpq.br/7193007113950510; Conceição, Edemilson Cardoso da; Bara, Maria Teresa Freitas; Café, Marcos Barcellos
Psidium guajava L. is a plant originated in Mexico, belonging to mytarceae family. The guava fruit is growth in economic value for the production of derivatives in the Brazilian agribusiness. However the use of guava pulp generates waste discarded in the environment, without the correct use, ie an environmental liability. The guava residue consists of pulp, peel, but mainly seeds. Yet is not described in the literature depth studies on its chemical composition or a suitable waste recovery. Thus, this study aimed to characterize the dust of organic residues of guava (donated by Food Predilecta ® - Matão, São Paulo), followed by obtaining the ethanol extract of the percolation method. The ethanol extract was characterized as the fatty acid profile, density and acid number and came to be known as: Powder oil waste processing Guava (OWG) from the OWG obtained the volatile fraction by hydrodistillation and characterization was carried out by gas chromatography coupled to mass spectrometry (GC / MS), followed by characterization of β-caryophyllene marker for high performance liquid chromatography (HPLC) and the identification of ORG constituents by GC / MS. We evaluated the antioxidant potential by free radical trapping methods 2,2-diphenyl-1- picryl hydrazyl (DPPH) and the capture of ferrous sulfate (FRAP). And finally, evaluated the implementation of the OWG, in laying hens Bovans White to verify the performance, posture, egg quality, digestibility and chemical composition of eggs and lipid oxidation of gems. The analysis of the volatile fraction of the OWG by GC / MS resulted in the identification of 25 compounds having as the major, the β-caryophyllene with 21.15%. Thus, an analytical HPLC method was revalidated in accordance with the criteria of Resolution 899/03 of ANVISA for quantification of β-caryophyllene (26.26%) in the OWG, to then be used for monitoring and characterization of OWG. Moreover, GC / MS, were identified in OWG, vitamin E and phytosterols such as α- tocopherol and the β-tocopherol, β-sitosterol and campesterol. OWG showed potential antioxidant activity, with EC50 31.24 mg / mL for the capture of DPPH and a content of 3,67.10-6 mM of ferrous sulfate per gram of capture OWG. Performance reviews and posture did not differ between treatments. The eggs of the birds supplemented with ORG and BHT had favored characteristics in relation to egg weight, yolk weight, White egg weight, suggesting the replacement of BHT, a commercial antioxidant with potential carcinogen by OWG. In supplementation in the diet digestibility analysis of OWG and BHT favored the absorption of protein and feed lipids, suggesting that because the oil antioxidant potential in preserving the laying of the power of nutritional constituents as well as to preserve the moisture content, low value caloric albumen and the lipid content in the yolks. The results showed an egg production with superior quality compared to conventional production. The work generates natural antioxidant additive application alternatives that results in improved quality, productivity and reduction in production costs. Moreover favors the export in view of the new requirements of importing countries products of Brazilian poultry.
Estratégias computacionais e experimentais para identificação de inibidores das proteínas helicase e protease dos vírus Dengue e Zika
(Universidade Federal de Goiás, 2020-03-17) Sousa, Bruna Katiele de Paula; Mottin, Melina; http://lattes.cnpq.br/4062617848341219; Andrade, Carolina Horta; http://lattes.cnpq.br/2018317447324228; Andrade, Carolina Horta; Neves, Bruno Junior; Rodrigues, Daniel Alencar
Introduction: Dengue (DENV) and Zika (ZIKV) viruses are flaviviruses that infect millions of people each year causing epidemics, which can cause mild to severe consequences in infected patients and can even lead to death. However, to date there are no effective ways to prevent or treat infections caused by these viruses. Thus, the development of antiviral drugs for DENV and ZIKV is urgent. Objective: The aims is identify drug candidates against DENV and ZIKV NS3 helicase and NS2B-NS3 protease proteins, which are essential in the viral life cycle, using an integration of computational and experimental strategies. Methods: This dissertation was divided in two projects. In the first project a virtual screening (VS) based on molecular docking and machine learning models (ML) was used to prioritize compounds that inhibit DENV helicase and protease proteins. To do this, binary ML models were developed and validated to select potential compounds with activity against DENV proteins. In the virtual screening of compounds against DENV protease, in addition to docking and ML models, models based on the molecular shape and volume (shape-based) generated and validated from DENV NS2B-NS3 protease inhibitors identified in the literature were also used. In the second project, we used a molecular docking approach and ML models to prioritize compounds against ZIKV NS2B-NS3 protease and NS3 helicase. Results: At the virtual screening performed in project 1, it was possible to prioritize 19 compounds, 9 compounds for NS3 helicase and 10 for NS2B-NS3 protease. These compounds have already been purchased and are in the experimental evaluation phase. In project 2, 22 compounds were selected, 15 for NS3 helicase and 7 for NS2B-NS3 protease. Phenotypic assays in ZIKV infected cells, showed that 6 compounds demonstrated inhibitory activity against the virus and are being validated in enzymatic assays. Conclusion: the present work demonstrated the potential of integration of computational techniques and experimental assays to accelerate the identification of potential candidates for Dengue and Zika virus antiviral candidates.
Bioconversão e degradação da venlafaxina em seu metabólito ativo
(Universidade Federal de Goiás, 2010-03-03) Carneiro, Wilsione José; Oliveira, Valéria de; http://lattes.cnpq.br/6300240031300604; Oliveira, Valéria de; Nóda Perez, Caridad; Cunha, Luiz Carlos da; Menegatti, Ricardo
The venlafaxine, 1-[2-dimethylamino-1-(4-methoxyphenyl)-ethyl] cyclohexanol, is a antidepressant drug of second generation. This is one of the most potent reuptake inhibitor of serotonin and noradrenaline, and its therapeutic effect is attributed to this activity. Venlafaxine is biotransformed in the liver to O-desmethylvenlafaxine (desvenlafaxine), N, O-desmethylvenlafaxine, N-desmethylvenlafaxine. Enzymes CYP2D6, CYP2C19 and CYP2C9 metabolize venlafaxine and major metabolite is the O desmethylvenlafaxine. This is pharmacologically active and contributes significantly to the pharmacological effect of venlafaxine, as is found in plasma at high concentrations. The investigation of the formation of degradation products is of great importance, because the products formed may be less active, more active or toxic. Bioconversion or the application of microbial models is a strategy to mimic the mammalian metabolism produces significant quantities of metabolites for studies of pharmacological activity and toxicological. This work represents a forced degradation study of venlafaxine extended release capsules in different stress conditions (acid and alkaline hydrolysis, oxidative and thermal) and select strains of filamentous fungi, to identify those able to metabolize venlafaxine and produce in a semi-preparative major metabolites. The filamentous fungi used were: Aspergillus candidus ATCC 2023, Beauveria bassiana ATCC 7159, Cunninghamella echinulata ATCC 9244, Cunningamella elegans ATCC 6169, Mortierella isabelina ATCC 1757 and Rhizopus arrhizus ATCC 11145. Was developed and validated method stability indicating HPLC using reverse phase for the analysis of venlafaxine in pharmaceutical formulation. The metabolites prepared by bioconversion were used for structural elucidation and later as a reference chemical in the analysis of stability studies and future studies of pharmacological and toxicological activity. The fungus Cunninghamella elegans ATCC 6169 was selected and produced O desmethylvenlafaxine (desvenlafaxine) and dihydroxy-venlafaxine, similar to those found in mammals, reinforcing the application of microbial models for the study of animal metabolism. The study indicated the stability of the acid condition of venlafaxine, formed two degradation products, the products found were similar to those obtained by bioconversion. The O-desmethylvenlafaxine, corresponds to the active metabolite of venlafaxine in humans and was recently approved for the treatment of major depressive disorder. Those studies, one can get the O-desmethylvenlafaxine in bioconversion reactions by Cunninghamella elegans ATCC 6169 and forced degradation studies of venlafaxine. The method developed and validated HPLC method was considered indicative of stability analysis of venlafaxine extended-release capsules, it is sensitive, specific (interference < 2%), precise (RSD < 2%), linear (r > 0.99), accurate (98.0 to 102.0%) and reproducible (RSD < 2%).
Desenvolvimento de nanopartículas lipídicas e associação de iontoforese para administração transdérmica do lopinavir
(Universidade Federal de Goiás, 2020-03-30) Moura, Rayssa Barbary Pedroza; Andrade, Lígia Marquez; http://lattes.cnpq.br/9862318690104720; Taveira, Stephânia Fleury; http://lattes.cnpq.br/0382450621383005; Taveira, Stephânia Fleury; Marreto, Ricardo Neves; Gelfuso, Guilherme Martins
Introduction: Lopinavir (LPV) is one of the antiretrovirals used to combat the human immunodeficiency virus (HIV). It has low oral bioavailability, a complex therapeutic regimen, and adverse effects, which affect the efficiency of the therapy. Transdermal administration can circumvent or reduce these problems. However, it requires strategies that facilitate the permeation of the drug. It is believed that nanostructured lipid carriers (NLC) combined with iontophoresis can increase the permeation of LPV to the deeper layers of the skin to be absorbed systemically. Objective: Develop NLC containing LPV and evaluate the permeation of the drug with and without iontophoresis. Methodology: The analytical method was adapted and validated. The solubility of the drug in surfactants was evaluated to select those that most solubilize LPV. NLC with different concentrations of LPV (0.5 - 1.5 mg/mL) were produced. Full characterization was performed (mean diameter, polydispersity index (PdI), zeta potential, encapsulation efficiency (EE), recovery (REC), drug loading (DL), and morphology). Electrical stability studies of the drug and NLC were carried out, as well as studies of electronic paramagnetic resonance (EPR), release and permeation in vitro, with and without electric current. Results and discussion: The method was linear, precise, and accurate. The NLC was spherical (145.83 ± 5.229 to 179 ± 2.551 nm). The PdI and zeta potential indicated good homogeneity and stability of the NLC. EE was around 80%, and, therefore, particles with 1.5 mg/mL of LPV were selected for subsequent studies. The stability studies of NLC-LPV concerning electric current demonstrated that the application of iontophoresis significantly reduced EE. The EPR spectra showed a significant increase in the nanoparticles' stiffness when an electrical current was applied. The electrical current also significantly increased the drug release in 6 h study compared to studies without electrical current. These data demonstrate that the electric current is a trigger in the drug release since it increases the rigidity of the lipid matrix. Iontophoresis also significantly increased the permeation of LPV. With an electrical current, LPV quantification was 14,49 ± 3,98 and 21,85 ± 2,28 μg after cathodic and anodic iontophoresis. These permeation data are significantly higher than the drug's EC50 values for various strains of the virus, reported in the literature. Conclusion: The combination of iontophoresis with NLC enabled higher permeation of LPV and proved to be a promising strategy for transdermal drug administration. However, in vivo, and pharmacokinetic studies are needed to assess the effectiveness of the strategy used in this study.
Aproveitamento da casca e polpa de Baru (Dipteryx alata Vogel) no desenvolvimento de um protótipo de suplemento alimentar, enriquecido com selênio
(Universidade Federal de Goiás, 2019-06-28) Santos, Cláudia Maria Barbosa; Santiago, Raquel de Andrade Cardoso; http://lattes.cnpq.br/0424807117498265; Conceição, Edemilson Cardoso da; http://lattes.cnpq.br/7193007113950510; Santiago, Raquel de Andrade Cardoso; Nóbrega, Andréa Bezerra da; Morais, Carla Cristina de
Introduction. Baru is a plant typical of the Cerrado Biome, whose nutritional potential is little explored, especially in the case of bark and pulp. It is known that baru has a fibrous pulp, and despite the benefits it can provide such as, reduced food consumption by increasing satiety power and consequent reduction in waist hip ratio, control of arterial hypertension and improvement of intestinal functioning , 68% of the population has less fiber intake than recommended. For this reason your supplementation may be beneficial. In addition to fiber, another important nutrient for health is selenium, given its association with changes or malfunctioning of the digestive tract. Objective. Develop a prototype food supplement in sachets, from bark and pulp of baru, that meets the daily nutritional needs of fiber and selenium. Methods. The raw material was obtained and characterized. The microbiological quality, centesimal composition, evaluation of the accelerated stability study of bark pulp powder and baru pulp and the prototype of the supplement were evaluated. Results and discussion. The raw material was adequate for the quality parameters. With the addition of excipients the prototype remained stable, with respect to the microbiological profile, humidity, fibers, selenium and other parameters. Two sachets with 30 g of supplement provides an energy value of 67.40 kcal, 1.56 g of protein, 0.82 g of lipids, 13.44 g of carbohydrates, 9.42 g of fibers, 200.32 g of selenium, 24.20 mg of calcium, 144.90 μg of copper, 0.98 mg of iron, 0.018 mg of phosphorus, 9.86 mg of magnesium, 0.283 mg of manganese, 211.468 mg of potassium, 6.591 mg of sodium and 0.225 mg of zinc. The labeling of the prototype of the supplement may be attributed as: source of fibers, source and / or selenium-rich, source of copper and low sodium content. Conclusion. The elaborated formulation was able to meet the recommendations for food supplement in relation to dietary fiber and selenium, for the population group above 19 years of age, can be used for other food purposes and also contribute to the use of parts of the fruit that are discarded.
Estudo do potencial antitumoral do complexo de Rutênio (II) coordenado com alopurinol em células de carcinoma mamário
(Universidade Federal de Goiás, 2017-09-29) Travassos, Ingrid Oliveira; Lacerda, Elisângela de Paula Silveira; http://lattes.cnpq.br/9390789693192751; Lacerda, Elisângela de Paula Silveira; Oliveira, Alisson Martins de; Correa, Rodrigo de Souza
Introduction: Ruthenium-based metallo complexes have been established as antineoplasic compounds with excellent activity, greater selectivity and lower toxicity, being able to coordinate with several different ligands and acting in several biological targets. Objective: This study aims to evaluate the antineoplastic potential of Ruthenium (II) complexes coordinated with allopurinol in mammary carcinoma, Ehrlich ascites tumor, MDA-MB-231 and non-tumor L-929. Methodology: Complexes of Ruthenium (II) coordinated with allopurinol were denominated Complxo 1 [RuCl2(alo)2(PPh3)] and Complex 2 [RuCl2(alo)2(dppb)]. Complexes 1 and 2 and Allopurinol were evaluated and compared in relation to antiproliferative activity by the MTT method. Effects of complex 2 on cell cycle kinetics were evaluated in TAE cells as well as the cell death profile through the apoptosis assay by flow cytometry and fluorescence microscopy. To determine the interaction of complex 2 with DNA the comet assay was performed. The antimetastatic potential was determined by the long-term migration and cytotoxicity assay in MDA-MB-231 cells. The expression of apoptotic proteins was performed via Western blotting. Results and discussions: Complex 2 showed better antitumor activity against lineages tested compared to complex 1 and Allopurinol, being selected for other tests. Complex 2 was able to act on the cell cycle interrupting its progression in the G0 / G1 phase. It has been shown a strong interaction of complex 2 with DNA, being proved by the evaluation of the characteristics of cellular death triggered by complex 2. A possible antimetastatic potential in MDA-MB-231 cells was also observed. Conclusions: Therefore, this new Ruthenium (II) complex associated with allopurinol may be considered a promising compound for antitumor purposes, resulting from its peculiar apoptotic mechanism.
Extrato líquido padronizado em capsantina a partir de Capsicum chinense Jacq. (Variedade Biquinho) e suas aplicações no desenvolvimento de um produto cosmético anti-aging
(Universidade Federal de Goiás, 2018-12-13) Brito, Lucélia de Sousa; Conceição, Edemilson Cardoso da; http://lattes.cnpq.br/7193007113950510; Conceição, Edemilson Cardoso da; Borges, Leonardo Luiz; Silva, Luis Antônio Dantas
Introduction: The pepper Capsicum chinense Jacq., popularly known as "biquinho pepper", has been outstanding in Brazil for presenting low pungency and a strong aroma. Its fruits are composed of several secondary metabolites, especially carotenoids, with important antioxidant properties. Objective: Develop a cosmetic product from the liquid extract of Capsicum chinense Jacq. standardized on capsanthin, evaluate its anti-aging efficacy in vivo and antioxidant activity. Methodology: The fruits of the "biquinho pepper" were sanitized, weighed, dehydrated, ground in a knife mill and hammers and stored at room temperature. The physico-chemical characterization of the pulverized vegetable raw material was carried out using the methods of microscopic analysis of the powder, determination of the volatile content, total ash, granulometric distribution and swelling index. Afterwards, the raw material was applied in the preparation of the liquid extract, using the techniques of maceration, percolation and concentration by forced ventilation, using the ethyl alcohol 96o GL as solvent extractor. The liquid extract was then characterized for solids content, pH, density and viscosity. Subsequently, total phenol concentration was determined by the technique of complexation of the phenolic compounds with ferric chloride solution, and also, the assay of total flavonoids and carotenoids by spectrophotometric methods. In addition, an analytical method by HPLC was validated for the quantification of the capsanthin in the concentrated liquid extract. Two cosmetics formulations were developed to perform comparative efficacy tests, a phytocosmistry developed from the liquid extract standardized on capsanthin, and another placebo formulation composed only of the galenic base of the product, without the addition of the extract. The cosmetics formulations were then evaluated for their accelerated stabilities and clinical efficacy anti-aging in vivo, evaluated in humans. The antioxidant activity was determined for the vegetable raw material, standardized liquid extract in capsanthin and the cosmetic formulation, using the DPPH radical capture, β-carotene / linoleic acid capture and ABTS radical capture assays. Results and discussion: For the physical-chemical characterization of the pulverized vegetable raw material, the microscopic analysis of the powder demonstrated the intimate nature of the sample as well as its purity, presented a volatile content of 4.62% (m / m), total ash content of 6.341%, the determination of the granulometric distribution classified the sample as coarse powder and the intumescence index was 1.27 ml ± 0.12 using alcohol 96o GL as an intumescent agent. In the physical-chemical characterization of the liquid extract the solids content was 19.16%, pH 3.7 ± 0.06, density 1.040 ± 0.0014 g / mL and viscosity of 3.22 mPas. The total phenolics, flavonoids and carotenoids contents for the raw material and concentrated liquid extract samples were respectively: 18 mg / 100 g and 168 mg / 100 g phenols, 10 mg / 100 g and 90.7 mg / 100 g flavonoids, 10mg / 100g and 83,70 mg / 100g of carotenoids. The validation of the analytical method by HPLC used in the quantification of capsanthin proved to be selective, linear (in the range of 0.48 to 7.2 μg / ml for the capsanthin standard and 26.93 to 404 mg / ml for the liquid extract), accurate, exact and robust. The content of capsanthin found in the liquid extract of C. chinense Jacq. was 1.126% (m / m). Both the standardized liquid extract and the cosmetic formulations were stable against accelerated stability tests, with results of organoleptic and physico-chemical characteristics within the parameters established for the tests. The analysis of the clinical anti-aging efficacy in vivo for cosmetic formulations has demonstrated the potentiation of efficacy for the cosmetic formulation consisting of the standardized liquid extract of Capsicum chinense Jacq., Compared with the placebo cosmetic, showing improvements in wrinkles, expression lines and sagging skin. The antioxidant activity in vitro for the vegetable raw material, standardized liquid extract in capsanthin and cosmetic formulation were respectively: 194.6μg / ml, 73.7μg / ml and 100μg / ml for capturing the DPPH radical relative to the IC50, 33.03%, 42.08% and 19.35% for inhibition of β-carotene oxidation, 22.87 μM Trolox / g, 51.81 μM Trolox / g, 900 μM Trolox / g for the ABTS radical capture. The values obtained for evaluations of antioxidant activities in vitro indicated that all the samples showed to be effective by antioxidant action, although the results have been lower if compared to their respective positive controls. Conclusions: The cosmetic product developed showed antioxidant activity and intended anti-aging efficacy, proving of potential use of the standardized liquid extract of biquinho pepper (Capsicum chinense Jacq.) in technological and innovative phytocosmetic formulations.
Avaliação do processo eletroquímico na degradação de amoxicilina e determinação de toxicidade dos subprodutos gerados
(Universidade Federal de Goiás, 2019-03-22) Caetano, Marcos Pereira; Gil, Eric de Souza; http://lattes.cnpq.br/3218622824233303; Gil, Eric de Souza; Garcia, Luane Ferreira; Comalti Júnior, Flávio
Introduction: Amoxicillin (AMX) is one of the world's most widely prescribed antibiotics for the treatment and prophylaxis of bacterial infections, in both human and veterinary medicine. The incomplete removal of this drug during the treatment of wastewater has attracted the attention of several researchers due to the risks of its bioaccumulation and consequent bacterial resistance. The electroemediation of drugs is of great value in the environmental scope, since electrochemical methods have several advantages when compared to the tools commonly used in the treatment of pharmaceutical and urban effluents. Objective: To evaluate the efficiency of the electrochemical process in the degradation of AMX using different electrolytic media and electrodes, as well as to investigate the adverse effects of the antibiotic before and after the electrochemical remediation. Methodology: The electrochemical tests were performed in three electrolytic media (tap water, Na2SO4 or NaCl solutions) and three anodes (carbon [C], titanium [Ti] and carbon modified with titanium oxide [TiO2 @ C]). The samples analyzed before and after the electro-oxidation were monitored by UV-visible, mass spectrometry and differential pulse voltammetry. After the electrooxidation process, the treated AMX solutions were analyzed by the ecotoxicity test with Danio rerio (zebrafish; paulistinha) and the minimum inhibitory concentration was calculated to determine the antimicrobial potential after treatment. Results and discussion: The titanium oxide modified carbon anode [TiO2 - C]) showed high efficiency, leading to the complete removal of amoxicillin in less than 10 minutes, in the order: [TiO2 @ C]> [Ti]> [C]. The dose of the electrolytes is supported in the following order: 0.1 M NaCl> Na 2 SO 4> 0.01 M NaCl> tap water. Amoxicillin does not pulse cardiac impressive of zebrafish during long term exposure. Conclusions: The electrooxidation of amoxicillin using TiO2 electrode in 0.01 M NaCl solution was able to decrease the antimicrobial activity of amoxicillin. At a high concentration of electrolyte, there is an increase in the rate of drug removal, there is why it is not the habitat that the zebrafish has become a toxic environment. The technique has been serous in the degradation of amoxicillin and can be applied to other organic pollutants.
Avaliação dos efeitos de irritantes inalatórios no modelo alveolar 3D Tox In-Pulmonar
(Universidade Federal de Goiás, 2021-03-29) Rodrigues, Marcella Miranda Siqueira Furtuoso; Valadares, Marize Campos; http://lattes.cnpq.br/6157755243167018; Valadares, Marize Campos; Silva Neto, Benedito Rodrigues da; Fernandes, Caio Pinho
Introduction: The Respiratory System has direct contact with the external environment, making it one of the main entry routes for chemical compounds and/or particles in the human organism. Inhalation toxicity analyzes are performed through in vivo tests, however, the toxicology of the 21st century seeks to replace, reduce and refine the use of animals in research. Currently, the emergence of new substances and particles with the most diverse purposes is increasing, being necessary for the toxicological investigation of these. With the advancement of science and the emergence of new technologies, some companies have commercially made available in vitro models for assessing inhalation toxicity, however, these models are not commercially available in Brazil. With this in mind, the research group Tox In developed a 3Dmodel with human pulmonary alveolar cells A549 (Tox In-Pulmonar) to mimic human exposure through culture in an air-liquid interface and conduct in vitro inhalation toxicity assessments in Brazil. Objective: To investigate the effects of exposure of lung cells to inhaledtoxicants directly on the tissue, using the Tox In-Pulmonar model. Methods: Inhaled toxicantswere prepared according to the determined concentrations and according to the physical and chemical characteristics of each compound. The construction of the Tox In-Pulmonar model occurred by cultivating the A549 cell in an air-liquid interface. In the present study, the exposure of inhaled toxicants in liquid form directly on the tissue was evaluated and PBS was used as a negative control. After exposure, the tissues were incubated in the culture oven at 37ºC for 3 hours and evaluated using the MTT assay. Morphological evaluation of the Tox In-Pulmonar model was also performed through histological processing. Results: The results suggest that the Tox InPulmonar model responds to exposure to inhaled toxicants according tothe GHS classification and that from this model a prediction for LC50 concentrations in animals can be made. Discussion: The model proved to be promising in the responses to inhaled toxicants, obtaining responses similar to the commercially available model EpiAirway. Also, the model can predict the value of LC50 in animals, which can drastically reduce their use in research. Conclusion: It is concluded that the 3D alveolar model developed can be a promising alternative to acute inhalation toxicity tests.
Aplicação do modelo microbiano do metabolismo animal ao estudo da biotransformação de um potencial agente cardioativo
(Universidade Federal de Goiás, 2011-02-28) Carneiro, Emmanuel de Oliveira; Oliveira, Valéria de; http://lattes.cnpq.br/6300240031300604; Oliveira, Valéria de; Porto, André Luiz Meleiro; Andrade, Carolina Horta
Drug metabolism, or biotransformation, is the enzymatically catalyzed conversion of a drug to a chemically distinct product, known generically as metabolite. The biotransformation impact on drugs biological fate makes essential to study it in the early stages of drug development. Traditionally, in vivo metabolism are conducted in animal models, whose biological fluids are examined for metabolites identification. The observation that simple microorganisms can mimic most of the phase I and some phase II reactions performed in mammals has shown they represent an alternative to produce high amounts of metabolites in vitro. The main organisms used are filamentous fungi, with particular attention to Beauveria bassiana and the genus Cunninghamella. The aim of this work is the application of B. bassiana as a microbial model to study LASSBio-294 biotransformation profile in parallel to an animal model. This substance has demonstrated significant positive inotropic and vasodilatory properties, turning it a potential cardioactive prototype. A capsule with LASSBio-294 was administered to a dog in a pilot study and analyzed by High Performance Liquid Chromatography with Ultraviolet detection (HPLCUV). B. bassiana ATCC 7159 incubation supernatant samples were taken and analyzed by HPLC- UV. At the end of the process, formed metabolites were extracted and purified. One product was characterized by nuclear magnetic resonance (NMR) and mass spectrometry (MS). According to the HPLC-UV analysis, B. bassiana ATCC 7159 produced a major metabolite detected in higher concentration after 24 hours of incubation. This metabolite was the same detected in dog serum samples. The biosynthesis of this metabolite resulted in a yield of 6%. The spectral data show the produced metabolite by dog and B. bassiana ATCC 7159 is a LASSBio-294 sulfoxide derivative. In vitro biosynthesis allowed to obtain, in considerable yield, the main mammalian metabolite detected in the in vivo method.
Composição química e variabilidade sazonal dos óleos voláteis das folhas de Siparuna guianensis Aubl. (Siparunaceae)
(Universidade Federal de Goiás, 2022-03-07) Souza, Joaquim Aurélio Tomaz de; Paula, José Realino de; http://lattes.cnpq.br/3191837532986128; Paula, José Realino de; Fiuza, Tatiana de Sousa; Borges, Leonardo Luiz; Oliveira, Thiago Levi Silva
Introduction: Siparuna guianensis Aubl., known as “negramina, capitu”, is a species popularly used for headaches, colds, fevers, as a healing agent, insect, and tick repellents. Objectives: To evaluate the chemical composition and seasonal variability of volatile oil from the leaves of S. guianensis. Methodology: Botanical material was collected between April 2019 to March 2020, from 10 different individuals, in Monte do Carmo, Tocantins, Brazil. Climatic data for the period were obtained from the National Institute of Meteorology. The powder from the leaves was submitted to hydrodistillation in a Clevenger apparatus and the identification of the compounds was performed by GC-MS. Principal Component Analysis (PCA) was applied to analyze the interrelationships between the chemical constituents of volatile oils of the species collected in different months. Hierarchical cluster analysis (HCA) was used to study the similarity between samples according to the distribution of constituents. To validate the cluster analysis, canonical discriminant analysis (CDA) was performed. Results and discussion: In volatile oils, 21.32% to 55.44% of sesquiterpenes, 19.95 to 49.73% of oxygenated sesquiterpenes, 0.48 to 1.55% of oxygenated monoterpenes, 0 to 5.67% of monoterpene hydrocarbons, 0 to 48.2% of other compounds were identified in the volatile oils. The major compounds were γ-muurolene (13.99 to 35.97%), curzerene (7.22-19.15%), curzerenone (7.3-18.13%), 2-undecanone (3.99- 10.63%). The presence of two clusters was verified: cluster I, discriminated by the compounds curzerenone, β-selinene, δ-elemene, corresponding to the months with the lowest rainfall, and cluster II, discriminated by the β-burbonene, corresponding to the months with the highest rainfall. Comparing the present study with data from the literature, it is observed that S. guianensis presents chemical variability, related to the rainfall index, that can alter the production of metabolites. Conclusions: The essential oils of S. guianensis are mainly composed of sesquiterpenes and oxygenated sesquiterpenes. The chemical variability of the oil is related to the rainfall index. The results obtained may help in directing the best times to collect leaves of the species S. guianensis, in addition to understanding the chemical variability profile related to seasonality.
Desenvolvimento de modelo ex vivo (Nov-ex) de córnea bovina em inferface ar-líquido para avaliação de toxicidade ocular: padronização e aplicabilidade
(Universidade Federal de Goiás, 2021-07-13) Penha, Jaqueline Rodrigues da; Valadares, Marize Campos; http://lattes.cnpq.br/6157755243167018; Valadares, Marize Campos; Cunha, Luiz Carlos da; Andrade, Wanessa Machado
Introduction: The evaluation of ocular toxicity is a mandatory parameter for the classification and labeling of products that may come into contact with the ocular surface, and is carried out according to the extent and depth of the damage caused after exposure. Currently, no model is capable of predicting mild and reversible damage to the cornea that would allow continuous and repeated ex-posures. Objective:! Standardize the cultivation of bovine cornea, in an air-liquid interface, evaluat-ing parameters of tissue viability and cell proliferation, after exposure to chemical and pharmaceuti-cal products. Methodology: Bovine eyes were collected from recently slaughtered animals in a slaughterhouse (Goiânia-GO). Central parts of the corneas were removed and cultivated in DMEM culture medium, supplemented with 5% bovine fetal serum and 10ng/mL of epidermal growth factor at 37°C and atmosphere 5% CO2. Initially, the model was exposed to ten chemical substances of different categories and evaluated by tissue viability assay (MTT). The model was also exposed to samples of capillary straighteners of commercial use nebulized by the Vitrocell® Cloud 12 exposure chamber and evaluated for tissue viability via MTT. Hitological analysis and expression of intracellu-lar formation of Reactive Oxygen Species (ROs) were performed, via DCFH- DA. Results: The model was viable for six days in air-liquid interface and was able to distinguish categories1/2. Expo-sure to Category 2A/2B substances showed a more significant reduction in tissue viability in the 48 hours following exposure, and not immediately after exposure. All samples of commercial use of capillary straightener were cytotoxic. Furthermore, the analysis of one of the samples demonstrated histopathological changes and an increase in intracellular production of ROs. Conclusion: The model was viable during six days of cultivation, being able to distinguish substances from different categories of ocular irritation. In addition, the model enables support for studies with continuous and repeated exposures, being a promising model for occupational toxicity data.
Administração transdérmica de cloridrato de raloxifeno encapsulado em nanopartículas lipídicas: estudos de pré-formulação para seleção dos lipídeos e tensoativos
(Universidade Federal de Goiás, 2017-09-26) Alves, Guilherme Liberato; Taveira, Stephânia Fleury; http://lattes.cnpq.br/0382450621383005; Taveira, Stephânia Fleury; Marreto, Ricardo Neves; Gelfuso, Guilherme Martins
Introduction: Raloxifene hydrochloride (RLX) is a widely prescribed drug for the treatment of osteoporosis and breast cancer. However, RLX presents a low oral bioavailability (2%), being an excellent candidate for transdermal drug delivery. The aim of this work was to develop nanostructured lipid carriers (NLC) containing RLX for transdermal drug delivery. In order to choose proper excipients, a compatibility study was performed. Methodology: Compatibility study was performed with differential scanning calorimeter (DSC), thermogravimetric anaysis (TGA), derivative thermogravimetry (DTG), isothermal stress testing (IST) and solubility study. RLX quantification was performed by high performance liquid chromatography (HPLC). After choosing the excipients, CLN were obtained by the microemulsion technique. Characterization was performed for mean diameter, polidispersivity index (PdI), zeta potential, entrapment efficiency (EE%) and stability. In vitro release and permeation studies were performed in Franz diffusion cells. Results and discussion. Conclusions: Drug-excipient compatibility studies allowed the development of stable and monodisperse CLN, capable of controlling drug release and increase its permeation in the skin when compared to the non-encapsulated drug in the control formulation.
Análise temporal do perfil de doações e da taxa de inaptidão sorológica de um banco de sangue público no Brasil
(Universidade Federal de Goiás, 2018-03-06) Pessoni, Lívia Lara; Alcântara, Keila Correia de; http://lattes.cnpq.br/3089303305362001; Alcântara, Keila Correia de; Santos, Thalyta Renata de Araújo; Leles, Renan Nunes
Introduction: Rigor in the selection process of donors led to a decrease in the number of individuals who meet the criteria of clinical and serological suitability for blood donation. In contrast, advances in medicine and the life expectancy of the population have led to an increase in the consumption of blood components. These factors created a challenge for hemotherapy services to guarantee the fulfillment of transfusion demand, combining the availability of blood products in their quality. This scenario led to the search for strategies to attract donors, such as the introduction of incentives to increase the number of donations. Objectives: Conduct a temporal analysis of the profile of blood donations performed in a public blood bank. Materials and methods: Retrospective study of donations between 2010-2016. Part of the analysis was stratified into three periods: before, during and after changing the criteria of an incentive program. Multinomial and multivariate logistic regression was used to verify the association between the explanatory variables and the positive serologies. Trends was evaluated by Prais Winsten's Regression. The Kruskal Wallis test was used to evaluate the seasonality. Results: 149,983 donations (1.08% of the local population) were performed, with a reduction of 29% (p <0.05). 49% of the donations were of the voluntary modality, 30% of campaign, 18% of replacement and 3% of other types of donation. The campaign donations had a 5.67% increase during the first study period (p <0.05), a decrease of 0.85% in the 2nd period (p> 0.05) and 6.65% in the 3rd period (p> 0.05) resulting in a total decrease of 5.02% (p <0.05). The transfusional transmissible infections rate was 3.71%, with a stationary tendency and the chance of donors having a serological disability was lower (OR = 0.8628; CI: 0.8126 - 0.9161; p < 0.0001). Seroprevalences for HBV, syphilis, HCV, HIV, Chagas disease and HTLV were 1.63%, 0.87%, 0.46%, 0.21%, 0.21% and 0.09%, espectively. The prevalence of HBV decreased (b = -0.021, p <0.001), while syphilis increased (b = 0.112; p = 0.001). Conclusion: The amount of blood donation is decreasing, which may be related to the decrease in campaign donations.
Glicosilação regiosseletiva da hesperetina catalisada por Cunninghamella echinulata ATCC 9244, em biorreator
(Universidade Federal de Goiás, 2019-03-19) Carvalho, Pedro Henrique de Oliveira; Oliveira, Valéria de; http://lattes.cnpq.br/6300240031300604; Oliveira, Valéria de; Arruda, Evilanna Lima; Bara, Maria Teresa Freitas; Santiago, Mariângela Fontes
Introduction: Hesperetina is a flavonoid, belongs to flavanones class, with several pharmacological activities, the most cited being the antioxidant potential. However, it presents low solubility and consequently low bioavailability, making it difficult to apply it in a systemic pharmaceutical formulation. Glycosylation of hesperetin effectively modifies its pharmacokinetic properties, increasing its antidiabetic, antitilipidemic activity and efficacy against helicobacter pylori. Filamentous fungi are used in biotechnological processes to increase the activity of molecules, being able to glycosylate, regio and stereoselective derivatives, with less cytotoxicity. Cunninghamella belongs to the class of filamentous fungi capable of catalyzing glycosylation reactions. With the demand of scale-up the production of bioactive compounds, bioreactors are a promising strategy, providing a controlled environment. Aim: The objective of this work was to scale-up the regioselective glycosylation of hesperetin catalyzed by Cunninghamella echinulata 9244 in a bioreactor, with pharmacological activities improved. Methods: Hesperetin was incubated with the microorganism in PDSM medium on two scales, semi-preparative (100 mL) and preparative (2 L). HPLC-MS was used to monitoring and the caracterization of the product formed was confirmed by 1H13C NMR. Tests of anticancer and cytotoxicity were realized. Results and Discussion: The glycosylation yield in the semi-preparative scale was 0.8%, while in the preparative scale the result was 22.9%. The increase in yield can be explained by the automated control of the main parameters such as pH and oxygenation. The ideal time for biosynthesis of the glycosylated derivative in bioreactor was 72 hours. The purified product glycosylated was identified by NMR in hesperetin 7-O-β-D-glucopyranoside, not exhibiting anticancer activity, but with reduction of cytotoxicity, with IC 50 9.5 times lower than the starting compound. Conclusions: Regioselective glycosylation of hespertin was performed in a single step in bioreactor, significantly increasing the yield. The chromatographic procedure proposed by the HPLC-MS allowed a fast and efficient identification and characterization of the derivative.

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