http://www.tede2.ufrpe.br:8080/tede2/handle/tede2/4359 2025-09-27T20:03:58Z 2025-09-27T20:03:58Z AGUIAR, Deivson Ferreira http://www.tede2.ufrpe.br:8080/tede2/handle/tede2/8994 2023-05-25T15:16:11Z 2021-09-15T00:00:00Z

Título: Síntese de novos derivados de 3-aril-5-adamantano-1,2,4-oxadiazol e N’-hidróxi-carboximidamida-2-amino-1,4-naftoquinonas com potencial atividade citotóxica e antitumoral Autor: AGUIAR, Deivson Ferreira Primeiro orientador: OLIVEIRA, Ronaldo Nascimento de Abstract: Heterocyclic compounds are present in numerous drugs. Heterocycles such as oxadiazole and imidazole have contributed to the development of new drugs with possible applications such as antiviral, antitumoral, anti-inflammatory and antimicrobial. In this work we propose the synthesis of a molecular diversity of 1,2,4-oxadiazoles and imidazol-naphthoquinones and evaluate their cytotoxic and antitumor potential. O-Acylamidoximes (3a-k) were synthesized via reaction of arylamidoximes (1a-k) with 1-adamantanecarbonyl chloride. Then, cyclocondensation of the O-acylamidoximes employing various methodologies provided the 1,2,4-oxadiazoles (4a-k). For the synthesis of N'-hydroxy-carboximidamide-2-amino-1,4-naphthoquinones (7a,c,f) and (8a-j) was used the reaction between 2-bromo-1,4-naphthoquinone (5) or to 2,3-dibromo-1,4-naphthoquinone (6) with the arylamidoximes (1a-j). In vitro cytotoxic assays were performed in Vero cells and murine fibroblasts, and in tumor cell lines: prostate adenocarcinoma, acute promyelocytic leukemia, colorectal carcinoma, glioblastoma, chronic and acute myeloid leukemia. O-Acylamidoximes (3a-k) were obtained in moderate-to-good yields (50-80%). The 1,2,4-oxadiazoles (4a-k) were obtained from 52 to 90% of yields. N'-hydroxy-carboximidamide-2-amino-1,4-naphthoquinones were synthesized in yields from 36 to 72% (7a,c,f) and from 47 to 82% (8a-j). In cytotoxic assays in Vero cells, 1,2,4-oxadiazoles were less toxic than O-acylamidoximes, having the compound 4g CC50 = 1797.0 μM. In assays with tumor cell lines, O-acylamidoximes (3a,d-h) showed a selective activity against leukemic cells. For acute promyelocytic leukemia (HL-60) cells, the tested compounds showed an inhibition above 90% at concentrations of 10 μg/ml and 25 μg/ml, and the compound 3e was the most active with IC50 = 19.50 μM for chronic myeloid cells (K562). Instituição: Universidade Federal Rural de Pernambuco Tipo do documento: Tese

2021-09-15T00:00:00Z FELIX, Daniele Mendes http://www.tede2.ufrpe.br:8080/tede2/handle/tede2/8993 2023-05-25T15:15:00Z 2020-11-20T00:00:00Z

Título: Ponto quântico de grafeno (Graphene Quantum Dot) decorado com imatinibe para o tratamento da leucemia Autor: FELIX, Daniele Mendes Primeiro orientador: OLIVEIRA, Ralph Santos Abstract: Leukemia is a myeloproliferative disease characterized by symptoms such as anemia, weight loss, lethargy, and abnormal bleeding. Imatinib is one of the drugs used for treatment and targets the BCR-ABL protein, a tyrosine kinase that promotes the translocation of chromosomes 9 and 22. The treatment of leukemia has major challenges such as the high incidence of adverse effects and the lack of specificity of the drugs. Several studies have used nanoparticles, including graphene quantum dots (GQD) in chemotherapy drug delivery increasing specificity and decreased toxic effects. Therefore, this study aimed to associate imatinib with GQD forming the nanoparticle GQD@imatinibe to evaluate its activity in leukemic cells. Thus, GQD was synthesized and conjugated to imatinib by functionalization with carbodiimide. The association was confirmed by Fourier-transform infrared spectroscopy and toxicity was tested in cell lines (RPMI 8226 and NCI-ADR/RES). The induction of apoptosis was evaluated by flow cytometry and the diffusion of the conjugate through the cellular membrane was verified in MDA-MB-231 cells. Spectroscopy analyses showed the formation of new bands that correspond to the bond formed between imatinib and GQD, these datas corroborate by atomic force microscopy assay results. Cytotoxicity assay showed by the conjugate was lower than imatinib citotoxycity. GQD@imatinibe was able to cross the cell membrane and showed lower cellular toxicity in relation to imatinib. GQD showed the lowest toxicity, presenting safety to use in biological systems. Regarding the induction of apoptosis, cell apoptosis was observed in diferente percentagens in the cell treatment with imatinib and GQD@imatinibe. Therefore, The GQD proved to be safe in vitro and compatible to be associated with imatinib, in addition, GDQ@imatinibe is capable of reaching the intracellular medium and causing the death of leukemic cells. Instituição: Universidade Federal Rural de Pernambuco Tipo do documento: Tese

2020-11-20T00:00:00Z GOMES, Ayala Nara Pereira http://www.tede2.ufrpe.br:8080/tede2/handle/tede2/8992 2023-05-25T15:13:06Z 2021-11-30T00:00:00Z

Título: Análise dos constituintes químicos dos polens apícolas monoflorais de dendê (Elaeis guineensis Jacq.), piaçava (Attalea funifera Martius) e sensitiva (Mimosa pudica Linn) Autor: GOMES, Ayala Nara Pereira Primeiro orientador: SILVA, Tania Maria Sarmento da Abstract: Bee pollen is produced by collecting hundreds of pollen grains from plant flowers plus salivary secretions from Apis mellifera bees. The Northeast of Brazil is the region that most stands out in the production of bee pollen, mainly monofloral bee pollen from palm trees. From an economic, nutritional and therapeutic point of view, monofloral bee pollen has the advantage of always presenting the same characteristics In this sense, the objective of this work was to analyze the chemical constituents of monofloral bee pollen collected from oil palm (Elaeis guineensis), piassava (Attalea funifera) and sensitive (Mimosa pudica) species by UPLC-DAD-qTOF-MS/MS, to determine the total phenolic content, mineral content and evaluate the scavenging activity of free radicals. The leishmanicidal activity was evaluated for the biflavonoid rhusflavone, isolated from sensitive bee pollen. The palynological analysis of the samples showed an average pollen frequency of 62% of A. funifera, 90% of M. pudica and 62% of E. guineensis. Through the analysis by UPLC-DAD-qTOF-MS/MS it was possible to identify three main classes of compounds: spermidine derivatives, lipids and flavonoids. From the bee pollen of M. pudica, the biflavonoids rhusflavone, amentoflavone and rhusflavanone were isolated. Rhusflavone showed leishmanicidal activity against the promastigote and amastigote forms of L. amazonensis. The pollens had the predominant minerals: magnesium followed by potassium, sodium, calcium and manganese, in addition to traces of zinc, iron and selenium. The samples also showed anti-radical activity that may be related to phenolic compounds, mainly flavonoids. The results show that the monofloral bee pollens of the species Elaeis guineensis, Attalea funifera and Mimosa pudica are potential sources of bioactive compounds. Instituição: Universidade Federal Rural de Pernambuco Tipo do documento: Tese

2021-11-30T00:00:00Z SALVI, Roberto Paulo Camara http://www.tede2.ufrpe.br:8080/tede2/handle/tede2/8253 2024-02-23T20:06:33Z 2019-08-23T00:00:00Z

Título: Uso de micropartículas poliméricas com etoposídeo radiomarcadas com tecnécio 99 metaestável para o diagnóstico diferencial de câncer de pulmão Autor: SALVI, Roberto Paulo Camara Primeiro orientador: OLIVEIRA, Ralph Santos Abstract: The diagnosis of lung cancer mostly occurs when the cancer is already in an advanced stage. In this situation, there are few options for the treatment and most of them have few chances of success. In this study, we developed and tested etoposide microparticles as a diagnostic agent for imaging lung cancer at early stages of development. We tested etoposide microparticles labeled with technetium 99m in inducted mice. The results demonstrated that over 10% of the total dose used was uptake by the tumor site. Also, the results showed that the microparticles had a good renal clearance and low uptake by liver and spleen. The data suggest that these microradiopharmaceuticals may be used for lung cancer imaging exam, especially single-photo emission computed tomography (SPECT). Instituição: Universidade Federal Rural de Pernambuco Tipo do documento: Tese

2019-08-23T00:00:00Z