https://repositorio.ufpb.br/jspui/handle/tede/5445 PPGPN Sat, 06 Jun 2026 17:41:39 GMT 2026-06-06T17:41:39Z http://repositorio.ufpb.br:443/jspui/retrieve/33645/ https://repositorio.ufpb.br/jspui/handle/tede/5445 https://repositorio.ufpb.br/jspui/handle/123456789/38092 Título: Estudo fitoquímico e farmacológico de Ruehssia caatingae (Morillo) F. Esp. Santo & Rapini (Apocynaceae) com avaliação in vitro das atividades anti inflamatória e citotóxica Autor(es): Lins, Jociano da Silva Orientador: Barbosa Filho, José Maria Abstract: The Apocynaceae family comprises approximately 5,350 species distributed across 378 genera, with widespread occurrence in tropical and subtropical regions. In Brazil, the family includes approximately 94 genera and 974 species, including shrubs, trees, herbs, and lianas. Among these is Ruehssia caatingae, a shrubby plant characteristic of Brazil's semiarid region, widely distributed on rocky outcrops in the Caatinga. Until the completion of this study, there were no records of phytochemical or pharmacological investigations of this species. Therefore, this study aimed to expand chemical and pharmacological knowledge of the Apocynaceae family by isolating and characterizing secondary metabolites from the aerial parts (leaves and branches) and roots of R. caatingae, as well as evaluating their cytotoxic and anti-inflammatory activities. For this study, the aerial parts and roots of R. caatingae were collected in the municipality of Pocinhos, Paraíba. The aerial parts and roots were dried and ground separately and subjected to maceration with 95% ethanol for 72 hours, this process being repeated four times, obtaining the crude ethanolic extracts (CEE). The CEE of the aerial parts (28 g) was subjected to Partition Chromatography using the solvents hexane, chloroform, ethyl acetate and n-butanol. The n-butanolic and ethyl acetate phases were subjected to successive fractionation steps using Sephadex LH-20 Chromatography, Medium Pressure Chromatography and High Performance Liquid Chromatography (HPLC), resulting in the isolation of three compounds: 3-methyl-N-pentanoic acid-β-D-galactofuranoside, described for the first time in the literature; (-)-conduritol F, isolated for the first time in the genus; and thymidine, isolated for the first time in the family Apocynaceae. The isolated compounds were evaluated for their cytotoxic potential against the U87-MG, SH-SY5Y, and MDA-MB-231 cell lines, showing no significant cytotoxic activity. The CEE from the roots was subjected to a partition process as previously described. The chloroform phase was subjected to successive fractionation steps by Sephadex LH-20 chromatography, column chromatography and HPLC, resulting in the isolation of eighteen new pregnane glycosides named Ruehssioside A-R. These compounds were evaluated for their anti- inflammatory potential in activated macrophage models, showing anti-inflammatory activity by significantly inhibiting the production of IL-1β, IL-6 and nitric oxide. Among them, Ruehssioside J stood out for having the highest potency (IC50 = 17.5 μM). The structure-activity relationship highlighted the importance of substitutions at C-3 and C-20, as well as the presence of a hydrogen at C-8, as determining factors for potency and efficacy. This work expands the chemical and pharmacological knowledge of the Apocynaceae family, highlighting the isolation of new compounds, particularly pregnane glycosides, demonstrating the family's relevance as a source of unique and biologically active structural metabolites. Editor: Universidade Federal da Paraíba Tipo: Tese Fri, 10 Oct 2025 00:00:00 GMT https://repositorio.ufpb.br/jspui/handle/123456789/38092 2025-10-10T00:00:00Z https://repositorio.ufpb.br/jspui/handle/123456789/38085 Título: Hidrogel de Aloe vera contendo óleo de copaíba encapsulado em carreadores lipídicos nanoestruturados para tratamento da dermatite atópica Autor(es): Uchôa, Ana Flávia Chaves Orientador: Xavier Júnior, Francisco Humberto Abstract: Atopic dermatitis (AD) is a chronic inflammatory skin disease characterized by barrier dysfunction, pruritus, and recurrent inflammation. Copaiba oil (CO) exhibits anti-inflammatory and wound-healing activity, while hydration and emollient replenishment are fundamental in AD management. In this study, copaiba oil-loaded nanostructured lipid carriers (NLCs) were developed and their in vitro performance was investigated, aiming at topical use through incorporation into Aloe vera-based hydrogels. Dialyzed NLCs were produced by hot emulsification followed by ultrasonication, containing 6% CO, and showed a size of 192.7 ± 2.2 nm, PdI 0.13 ± 0.04, and zeta potential −35.2 ± 1.0 mV. The cytotoxicity of the formulations was assessed by the MTT assay in HaCaT cells, with an IC50 of 73.59 ± 1.21 μg/mL. Aloe vera mucilage was extracted and structurally characterized, including the presence of aloin; a polysaccharide profile was confirmed, along with low-intensity peaks related to aloin. Hydrogels containing the mucilage were produced and demonstrated rheological and texture properties suitable for topical application, even after association with the NLCs. Oxidative stress was evaluated in RAW 264.7 cells using the formulations at a final concentration equivalent to 25 μg/mL of CO, in which the hydrogel containing NLCs (H-NLC) was the only one able to completely attenuate the oxidant state induced by PMA (200 ng/mL). Anti-inflammatory activity was investigated under stimulation with LPS (1 μg/mL). For NO2− quantification, NLC significantly reduced this marker compared with LPS. By ELISA, a reduction in IL-6 was observed for NLC (−43.9%) and CO (−34.0%), whereas for TNF-α, NLC showed a statistically significant reduction (−23.2%). Therefore, it is concluded that nanoencapsulation promoted superior antioxidant and anti-inflammatory effects compared with free copaiba oil, highlighting the potential of the developed system for the treatment of topical inflammation. Editor: Universidade Federal da Paraíba Tipo: Dissertação Thu, 29 Jan 2026 00:00:00 GMT https://repositorio.ufpb.br/jspui/handle/123456789/38085 2026-01-29T00:00:00Z https://repositorio.ufpb.br/jspui/handle/123456789/38048 Título: Estudo fitoquímico e avaliação antineuroinflamatória de Senna pluribracteata, uma nova espécie brasileira da família Fabacea Autor(es): Souza, Ranna Beatris de Lima Orientador: Tavares, Josean Fechine Abstract: Since the earliest civilizations, humans have used plants for food, construction, and disease treatment, with the Fabaceae family representing an important source of species with therapeutic properties. In Brazil, the genus Senna is widely distributed, especially in the Atlantic Forest, and holds great relevance in ethnomedicine due to the richness of its bioactive metabolites. In this context, this study aimed to expand knowledge about the Senna genus, specifically the species Senna pluribracteata, a newly identified species, by isolating its chemical constituents and evaluating its antineuroinflammatory potential. The aerial parts of the plant were dried, ground, and subjected to an ethanol extract (EEB), followed by a liquid–liquid partitioning (CLV) to fractionate this extract. The 100% ethyl acetate (AcOEt) and AcOEt:MeOH (1:1) phases, after being subjected to MPLC and HPLC, led to the isolation of several compounds. From the 100% AcOEt phase, sennaquinone A (Sep-1), vanillic acid (Sep- 8), protocatechuic acid (Sep-9), resveratrol (Sep-11), and vomifoliol (Sep-12) were isolated. From the AcOEt:MeOH (1:1) phase, quinquangulone (Sep-2), quinquanguline-6-O-[α-L-rhamnopyranoside-(1→6)-β-D-glucopyranoside] (Sep-3), rubrofusarin-6-O-[β-(6'-(E)-crotonylglucopyranoside)] (Sep-4), rubrofusarin-6-O-[α-L- rhamnopyranoside-(1→6)-β-D-glucopyranoside] (Sep-5), rubrofusarin-6-O-β-D- glucopyranoside (Sep-6), norrubrofusarin-6-O-β-D-glucopyranoside (cassiaside) (Sep-7), and quercetin-3-O-sambubioside (Sep-10) were obtained. The compounds were identified by high-resolution electrospray ionization mass spectrometry (HR-ESI- MS) and 1H and 13C NMR spectroscopy, using one- and two-dimensional techniques. Antineuroinflammatory activity was assessed through a cell toxicity assay (MTT reduction) using the BV2 microglial cell line, along with nitric oxide (NO) production measurement. Treatment with Sep-2, Sep-3, Sep-4 (200 μM), and Sep-3 (100 μM) reduced cell viability by more than 20%, and only Sep-5 significantly reduced NO levels. The results obtained in this study contributed to the phytochemical and pharmacological knowledge of the Senna genus and of the new species Senna pluribracteata. Editor: Universidade Federal da Paraíba Tipo: Tese Tue, 04 Nov 2025 00:00:00 GMT https://repositorio.ufpb.br/jspui/handle/123456789/38048 2025-11-04T00:00:00Z https://repositorio.ufpb.br/jspui/handle/123456789/37673 Título: Planejamento, síntese e avaliação do potencial antileishmania de novos 2-aminotiofeno-3-carboxamidas obtidas por modificação molecular Autor(es): Ferreira, Mirla Mirely Dantas Orientador: Mendonça Junior, Francisco Jaime Bezerra Abstract: Leishmaniasis is considered a public health problem, most of the cases are registered in emerging countries and in low-income populations, being still neglected tropical diseases which are not prioritized in research investments by large pharmaceutical companies, which results in few treatment options, in which they have several adverse effects, and long periods of treatment. In view of this, it became necessary to search for new effective and less toxic drugs, which is initiated by the understanding of Medicinal Chemistry, which allows the synthesis or isolation of better compounds. In addition, among the compounds with activity described in the literature, the 2-amino-thiophene derivatives are a versatile class of sulfur-containing compounds and an immense capacity to offer ligands for different molecular targets, with anti-leishmania potential. replacement of carbonitrile, which showed low solubility, by carboxamide at position-3, which showed activity against L. amazonenses in other studies. Thus, the objective of this work was to synthesize new 2-aminothiophene-3 carboxamide derivatives that are candidates for antileishmanial drugs, by carrying out the molecular modification of substituted 3-carbonitrile prototypes, in order to verify the importance of the substitution pattern of the C-3 position of the thiophene ring. Fifteen compounds were synthesized, with color varying between yellow and orange, yields from 20 to 98%, with the same synthetic route for all molecules. The compounds had their structures confirmed by NMR1H and 13C, their antileishmanial activities evaluated against the promastigote forms of Leishmania amazonensis, L. braziliensis, L. infantum and L. major, and their toxicities evaluated against RAW 264.7 macrophages. The 6BOC2 compound showed the highest inhibitory activity with IC50 values lower than 8μM for all species tested, and a selectivity index (SI) higher than 37.6. The comparison of the inhibition values and SI of the 3-carboxamide derivatives in relation to the 3- carbonitrile derivatives allows us to affirm that the presence of the 3-carbonitrile radical is not essential for antileishmanial activity. Although the substitution by the 3- carboxamide group did not result in compounds with activity superior to the 3- carbonitrile derivatives, obtaining new compounds with this substitution pattern should be taken into account when planning new antileishmanial drug candidates for this class of compounds. Editor: Universidade Federal da Paraíba Tipo: Dissertação Mon, 28 Mar 2022 00:00:00 GMT https://repositorio.ufpb.br/jspui/handle/123456789/37673 2022-03-28T00:00:00Z