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CLARICE FLEXA DA ROCHA
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REPRODUCTIVE TOXICOLOGY OF CHRONIC®, ORMONA® SI AND ORMONA® RC- NUTRACEUTICS WITH GERANYLGERANIOL, TOCOTRIENOL, ANTHOCYANINE AND ISOFLAVONE MARKERS
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Data: 09/12/2022
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Introduction: Currently, concerns related to aging include cognitive, ocular, bone, joint, cardiovascular and reproductive functions. In order to improve the quality of life, the Brazilian company Ages Bioactive Compounds Co., eveloped the nutraceuticals Chronic® (CHR), Ormona® SI (OSI) and Ormona® RC (ORC), which have in their formulations bioactive components such as isoflavones, carotenoids, tocotrienols, geranylgeraniol and anthocyanins. However, in the case of OSI and ORC, due to the presence of phytoestrogens, for pregnant and lactating women the use of these nutraceuticals is not being recommended. Objective: to study the effects of the use of these new nutraceuticals during the stages of reproductive development in animal species, rodents and non rodents. Material and Methods: The protocols used in this study are established by regulatory agencies (ANVISA, OECD). In zebrafish, acute and reproductive toxicity was evaluated at doses of 500, 1,000 and 2,000 mg/kg, through the observation of behavioral changes, lethality and tissue changes (intestine, liver, kidney, and sexual gonads). The results obtained in the different analyzes were expressed (mean ± SEM), Kruskal-Wallis test, followed by Dunn's post hoc test (p <0.05). In rodent species, young rats were used, divided into critical periods of development, with five experimental groups (n=4), Polysorbate (POL, 1ml), Lecithin (LEC, 5%/kg), CHR, OSI and ORC (200mg/ kg, respectively). He critical periods of development were pre-implantation (d0-d5), post-implantation (d6-d15) and postnatal (dpn13-dpn19), evaluating acute toxicity, water intake, food intake, weight development and reproductive performance, hormone dosage for thyroid markers, dosage of biochemical markers, in addition to macroscopic and microscopic analysis of vital and reproductive organs. The results obtained in the different analyzes were expressed (mean ± SDM), ANOVA, followed by the Tukey test (p < 0.05). All analyzes were performed using the GraphPad Prism® software (5.03). Results and discussion: Treatment with OSI and ORC in zebrafish caused a decrease in fertility, and this effect was also reproduced in rodents, in the pre-implantation period, suggesting a reduction in reproductive capacity and implantation of blastocysts in the uterus. In the post-implantation test, treatment with CHR, ORC and OSI, for ten days, provided fetal development without abnormalities, mainly in the ossification and visceral process of the offspring. In the postnatal period, no toxicity was observed in lactating females or in their descendants, being observed that the treatment with CHR, OSI and ORC, responsible for the significant decrease of the plasma concentration of the lipid profile. Treatment for seven days with CHR, OSI and ORC did not trigger signs of behavioral or physical alterations in the evaluated parameters of the offspring. Conclusions: The presence of isoflavones in Ormona® formulations (OSI and ORC) caused negative effects on the decidualization process, increasing the occurrence of pre-implantation losses in young female rats. However, the results show that the lactation CHR, OSI and ORC were safe for lactating animals and their offspring for all evaluated parameters.
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WALTER DE SOUZA TAVARES
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DEVELOPMENT, BIOPHARMACEUTICAL CHARACTERIZATION AND HEALING EVALUATION OF POLYMERIC SYSTEMS NANOSTRUCTURED BASED ON ZEIN AND ELAGIC ACID
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Data: 21/11/2022
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Introduction: Zein protein has demonstrated the ability to carry therapeutic molecules in different drug delivery systems, such as nanoparticles (NPs) and films. Ellagic acid (EA) is a polyphenol that has relevant biological activities, such as antimicrobial, antioxidant, antienzymatic and healing. In view of these properties and the benefit of its association with zein, described in our previous study, the preparation of nanoparticles could improve their functionality to be used in controlled release systems. Objectives: To develop, characterize and evaluate the biopharmaceutical and healing properties of nanostructured controlled release polymeric systems based on zein and ellagic acid for the treatment of skin disorders. Material and Methods: EA-loaded zein NPs were designed, characterized by size, polydispersion index, zeta potential, pH, encapsulation efficiency, drug loading, release efficiency and stability. Its antimicrobial activity was evaluated based on the minimum inhibitory and bactericidal concentration and antibiofilm activity against Staphylococcus aureus and Pseudomonas aeruginosa. Its antioxidant capacity was assessed by DPPH and ABTS radical scavenging methods. The antienzymatic activity against key enzymes related to the skin regenerative process was also evaluated: hyaluronidase, lipoxygenase, elastase, collagenase and tyrosinase. The photoprotective activity and cytotoxicity against human keratinocytes, squamous carcinoma cells and erythrocytes were also evaluated. The EA-zein interaction was evaluated by 1H NMR, FTIR and fluorescence. The NPs were loaded into chitosan/gelatin/zein films, subjected to physical, mechanical and biopharmaceutical characterizations. Finally, the healing activity of these novel formulations was evaluated in vivo. Results and discussion: The characterization of the NPs allowed to select the most stable formulations. These were stable up to 365 days, presented a sustained release profile until 20 days, showed satisfactory antimicrobial activity, high antioxidant effect after 24h, relevant antienzymatic activity for use in different therapeutic targets related to skin disorders, high photoprotective activity, limited cytotoxicity and were found to accelerate the healing process in an animal model. The films containing the nanoparticles were uniform and presented favorable characteristics, antimicrobial effect and were found to accelerate the healing in vivo. Conclusions: The nanoencapsulation of EA has improved its pharmacological activity in important therapeutic targets, showing great potential for use in the treatment of skin disorders. The films proved to be a robust release system for carrying the NPs, with functional features that enables their application in the treatment of skin lesions. Both devices were effective in reducing wounds in an animal model, being, therefore, important candidates to become new therapeutic products.
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AGERDANIO ANDRADE DE SOUZA
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Chemical-pharmacological validation of the hydroethanolic extract of leaves and resin of the species Trattinnickia rhoifolia (Willd): ethnopharmacological studies, acute toxicity and anti-inflammatory in zebrafish
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Data: 28/10/2022
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Introduction: Plant-derived products are promising agents in the treatment of various diseases. The species Trattinnickia rhoifolia (Willd), (T. rhoifolia), belonging to the Burseraceae family, is present in the cultural practices of ethnomedicine and ethnopharmacology of the Peoples and Traditional Communities (PCTs) of the Brazilian Amazon and is used for anti-inflammatory purposes, sometimes as the only therapeutic resource. Despite this, the species is still unexplored in its pharmacophoric potential. Therefore, the objective of this study was to evaluate the acute toxicity and anti-inflammatory action of the hydroethanolic extracts of leaves (HELTr) and resin (HERTr) of the species T. rhoifolia with non-target organism zebrafish (Danio rerio). In Methodology, the extracts were analyzed by gas chromatography coupled to mass spectrometry (GC-MS). The assessment of the acute toxicity of HELTr and HERTr in adult zebrafish was determined using the Limit Test (2000 mg/kg), with behavioral and histopathological assessments, in addition to the analysis of anti-inflammatory potential in carrageenan-induced abdominal edema, followed by use of the computational method of molecular docking. The chemical-pharmacological profile of the species showed the presence of propanoic acid, ethyl ester; hexadecanoic acid, ethyl ester; 2-methyl 1-propanol; propane, 2,2-diethoxy; n-hexadecanoic acid; n-propyl acetate; benzophenone; propane,1,1,3-triethoxy; 1-butanol, 3-methyl; acetic acid ethenyl ester; decanoic acid; ethyl ester; 3-hydroxybenzoic acid. In studies with zebrafish, HELTr and HERTr did not show toxicities in behavioral and histopathological assessments, according to the IAH, as there was no change in the functioning of the organs studied. Carrageenan-induced abdominal edema, at all doses of HELTr and HERTr, (100, 200 and 500 mg/kg), were significantly reduced in relation to the negative control (DMSO), whereas the doses of 200 and 500 mg/kg were significantly reduced. kg showed expressive anti-inflammatory activity in relation to the positive control (indomethacin) of the tested extracts. As the activities were confirmed by molecular docking studies, they showed a high profile for the inhibition of the Cyclooxygen-nase-2 enzyme, since the interactions established in the receptors used in the docking study were similar to the controls used. HELTr and HERTr had an acceptable degree of safety for acute toxicity, defined in the analysis of behavioral changes, mortality and histopathology, with significant anti-inflammatory action in zebrafish at all doses, which demonstrates the high pharmacological potential of the species.
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PEDRO HENRIQUE FAURO DE ARAÚJO
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PLANNING OF NEW COX-2 INHIBITORS FOR THE TREATMENT OF INFLAMMATORY DISEASES: THEORETICAL AND EXPERIMENTAL STUDY
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Data: 21/10/2022
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Introduction: Non-steroidal anti-inflammatory drugs are selective inhibitors of cyclooxygenase-2 (COX-2) and were developed with the aim of avoiding the side effects of non-selective inhibitors via COX-1. Objective: According to the research already developed, the objective of this work is to design new drug candidates based on the inhibitors Indomethacin and Rofecoxib, with anti-inflammatory potential in the COX-2 receptor via virtual screening, molecular docking and in vivo study in a Zebrafish model. (Danio rerio). Methodology: At first, selection of inhibitors was performed in the BindingDB database based on the lowest IC50 values, pharmacophores were generated using the PharmaGist online server and Pearson's correlation with statistical quality determined by: correlation coefficient (R), squared correlation coefficient (R2), explanatory variance (adjusted R2), standard error of the estimate (SEE) and variance ratio (F). The compounds obtained were compared against the selected pivot (Rofecoxib) using Tanimoto's similarity, and the most promising compounds were submitted to prediction of pharmacokinetic properties and molecular coupling (docking) study. In a second moment, 11 molecules were selected from a database of the Center for Studies and Selection of Bioactive Molecules (NESBio-UFPA) and validated through pharmacokinetic screening and docking, for further analysis against Zebrafish. Results and discussions: The QSAR analysis showed fit with R = 0.9617, R2 = 0.9250, SEE = 0.2238 and F = 46.2739, with the tetra-parametric regression model. After analysis, three promising molecules were selected, Z-964, Z-627 and Z-814, with their predicted pIC50 values, Z-814 = 7.9484, Z-627 = 9.3458 and Z-964 = 9.5272. The inhibitors showed activity prediction (Pa > Pi) for cyclooxygenases, with Z-627 having higher antiarthritic activity compared to the adopted controls (Z-627 = 0.951, Rofecoxib = 0.828, Celecoxib = 0.663). Molecular docking showed a RMSD calculation of 0.86 Å for PDB 5KIR and 0.68 Å for PDB 3LN1, below the ideal adopted standard of 2 Å, with significant binding affinity (ΔG) values when compared to experimental results adopted in the literature. Of the 11 molecules selected in the second moment, two were more promising and were evaluated in vivo, presenting anti-inflammatory activity like commercial compounds and with relative side effects on the evaluated organs, however, the administered dosage must be evaluated. Conclusions: All inhibitors complied with Lipinski's rule of five, which provides for good oral availability, as well as statistical analysis consistent with predictability, allowing the validation of pharmacophoric models. On the other hand, the molecules evaluated against the Zebrafish model showed significant activity when compared to the reference drug, providing an alternative availability in front of it.
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CLEIDJANE GOMES FAUSTINO
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DEVELOPMENT OF FORMULATIONS FROM ESSENTIAL OIL FROM RESIN OF Protium heptaphyllum (Aubl. Marchand) FRONT OF THE VECTOR Aedes aegypti (Linnaeus, 1762)
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Data: 30/09/2022
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Brazil is a country with great biodiversity, being considered one of the largest in the world. Medicinal plants have been used since the dawn of humanity, being inserted in the treatment of various pathologies. Essential oils are made up of volatile substances from the secondary plant metabolism of aromatic plants. They are formed in special cells found in different parts of plants such as leaves, flowers, seeds, stems and roots. The objective of this work is to obtain and chemically characterize the essential oil of the Protium heptaphyllum resin and test the cream emulsions and nanoemulsions prepared with the essential oil and evaluate the biological activities: ovicidal, pupicidal, larvicidal, residual and repellent against Aedes aegypti. The essential oil was extracted by the steam drag technique in a Clevenger apparatus and characterized by Gas Chromatography coupled to a Mass Spectrometer. The nanoemulsion was prepared by a low energy titration method and characterized by photon correlation spectroscopy. The cream was prepared by the phase inversion temperature technique. The protein odor inhibition potential in Aedes aegypti and Anopheles gambiae was evaluated by molecular docking (MD) simulations. The extraction yielded 0.69 ± 0.085 (m/v) of essential oil. In the chromatographic analysis, the major constituents were p-cymeno (27.70 %), α-Pineno (22.31 %). The zeta potential demonstrated a kinetic stability and a monomodal distribution in the hydrophilic-lipophilic balance 14 with a particle diameter of 115.56 ± 1.68 nn and a zeta potential of -29.63 ± 3.46 mV. In the larvicidal trial, the group treated with the nanoemulsion at 20 µg.mL-1 reached 96% mortality in the first 24 hours, reaching 100% in 48 h. In the residual test, concentrations of 20 and 40 µg.mL-1 showed mortality up to 3 days, while doses of 60, 80 and 100 µg.mL-1 showed mortality up to 11 days, the control groups had no mortality. The nanoemulsion showed insecticidal action with LC50 0.404 µg·mL−1 for the ovicidal effect. In the pupicidal test, the concentration of 160 µg·mL−1 showed 100% mortality after 24 h of test. In adulticidal activity the diagnostic dose of 200 µg·mL−1 was determined in (120 min). In the repellency test, the concentration of 200 µg·mL−1 during the 180 min of the test showed a protection index of 77.67%. In molecular docking, the control showed significant stability and a proven repellent action. The α-Phellandrene and 2-Carene molecules showed a dual effect of action for the inhibition of AgamOBP1 (PDB ID 3N7H) and AaegOBP1 (PDB ID 3K1E. Therefore, the results presented here suggest that the essential oil emulsions of the Protium heptaphyllum resin have great potential in the prevention and control of Aedes aegypti.
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SÔNIA DO SOCORRO DO CARMO OLIVEIRA
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Extraction, characterization and evaluation of antioxidant, antimicrobial and anti-inflammatory activity of extracts from seeds of Bixa orellana L.
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Data: 23/09/2022
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Introduction: Bixa orellana L. (Bixaceae), known as “urucum”, “annatto”, whose seeds have antioxidant, antibacterial and anti-inflammatory properties, has bixin as the major compound present in 80% of the extracts. Annatto seed extracts are raw materials for pharmaceutical development. Objectives: To morphologically analyze Bixa orellana L. phenotypes and evaluate in vitro the antioxidant and antimicrobial activities of the fractions and extracts, as well as the anti-inflammatory activity of the nanoformulation in vivo, obtained from annatto seed oily extract (ASE). Methodology: The total phenolic content was determined, and in vitro antioxidant and antibacterial activities (MIC) of the seeds of the three annatto phenotypes (red, yellow and green) were evaluated, using different solvents (hexane, ethyl acetate, methanol and hydroethanolic). Nanomaterials were developed from annatto seed oily extract (ASE), myristic acid (tetradecanoic acid) and its fatty acid esters. The obtained nanoformulation (ASE + BNO-NLC) was used in an acute toxicity assay and the antiinflammatory activity was evaluated through the inhibition of edema formation in adult zebrafish induced by intraperitoneal injection of carrageenan. Results and discussion: The highest concentration of total phenolics (30.10 ± 0.05 mg EAG.g -1 extrato, p < 00.5) and the highest antioxidant capacity by the DPPH method (IC50 97.81 ± 1.86 µg.mL-1 , EC50 2.44 ± 0.04 and ARP 40.90 ± 0.77) was found in the methanolic fraction of the green fruit. The total antioxidant activity (phosphomolybdenum assays) showed the highest percentage inhibition rate to the hexane fraction of green fruit (68.04 ± 0.09) and metanolic fraction of red fruit (67.98 ± 0.33), without significant difference between both (p> 0.05). The three hydroethanolic seeds extracts from three phenotypes showed high antibacterial properties against Gram-positive S. aureus Newman, with MIC values ranging from 4.9 µg.mL-1 to 6.6 µg.mL-1 . The lipid nanoparticles obtained using myristic acid and ASE + BNO or only BNO and lipid nanoemulsions produced from methyl tetradecanoate and ASE + BNO showed better results. The nanoformulation showed no toxicity at the dose tested (dose of 1000 µg/kg, v.o.). In the anti-inflammatory activity test, the experimental groups (ASE + BNO-NLC) at doses of 50, 150, 500 and 650 mg/kg demonstrated a significant antiinflammatory effect (p<0.05), up to the dose limit of 500 mg/kg. Conclusions: The findings confirmed the antioxidant activity of B. orellana extracts, high antibacterial activity of the hydroethanolic extracts against S. aureus Newman and the antiinflammatory effect of the obtained nanoformulation.
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INANA FAURO DE ARAÚJO
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Larvicidal potential of crude extracts of endophytic fungi Aspergillus sp. and Trichoderma asperellum isolated from Bertholletia excelsa Humb. & Bonpl against Aedes aegypti: innovation and understanding of the mechanism of action
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Data: 08/09/2022
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Introduction: Endophytic fungi represent a rich source of bioactive natural products still unexplored. Its secondary metabolites are particularly attractive due to the metabolic interactions with their hosts. Arboviruses, mainly those transmitted by Aedes aegypti, are considered a public health problem, especially because vaccines are not yet available, and vector control is the most efficient way to contain outbreaks caused by these viruses. In this regard, vector control through effective and selective substances with low human and environmental toxicity is essential. Objective: This work aimed to obtain extracts of endophytic fungi isolated from Bertholletia excelsa and evaluate their larvicidal potential against Aedes aegypti, as well as elucidate a possible mechanism of action of the substance in the insect's nervous system. Methodology: Endophytic fungi were isolated from Bertholletia excelsa nuts. Different extracts and growing medium were prepared (liquid and semi-solid). Then the extracts were dried, characterized, and evaluated against the 3rd instar larvae of Aedes aegypti under controlled laboratory conditions, at different concentrations and medium. Possible mechanisms of action and inhibition of acetylcholinesterase and juvenile hormone were evaluated through computational methods such as molecular docking for 187 molecules cataloged in the literature as metabolites of the fungus Aspergillus sp. Result: The isolated fungi were molecularly identified as Aspergillus sp and Trichoderma asperellum. The extracts tested on Aedes aegypti showed, in general, high to moderate bioactivity. The hydroethanolic extract of Aspergillus sp revealed LC50 values of 26.86 μg/mL in 24 hours and 18.75 μg/mL in 48 hours. Through molecular docking, the compound Aspergillol B, present in this extract, was identified as a potent larvicidal candidate for inhibiting the enzyme acetylcholinesterase. From the 187 substances produced by the fungus Aspergillus spp, the validation results of the molecular docking protocol indicated that N-βacetyltryptamine presents itself as a potential insecticidal agent that inhibits the action of juvenile hormone. The crude extract of the fungus Trichoderma asperellum, when evaluated on Aedes aegypti, revealed promising results for vector control when associated with silk protein as a vehicle, in addition to the absence of significant toxicity to non-target organism Danio rerio. Conclusion: This study allowed the isolation, identification, and production of extracts of endophytic fungi, Aspergillus sp and Trichoderma asperellum from Brazil nuts and their larvicidal evaluation in Aedes aegypti. Moreover, it elucidated possible mechanisms of action of substances produced by them. New substances have been identified as potential insecticide candidates, such as Aspergillol B, which may represent significant advances in the control of vectors with toxicological safety.
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LECILDO LIRA BATISTA
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STUDY OF EFFICACY AND CLINICAL SAFETY OF PHARMACEUTICAL FORMULATION CONTAINING EXTRACT OF Acmella oleracea (L.) R.K. Jansen (Asteraceae) IN PATIENTS WITH PREMATURE EJACULATION
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Data: 12/08/2022
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Introduction: Premature ejaculation (PE) is described as the inability to delay ejaculation in all or almost all vaginal penetrations. The agents available to treat PE are associated with relevant side effects. A formulation incorporated into natural products such as Acmella oleracea (L.) R.K. Jansen (A. oleracea) becomes promising for the treatment of sexual dysfunctions, due to sensory properties, such as the tingling sensation. Objective: to evaluate the clinical efficacy of a pharmaceutical formulation containing standardized extract of Acmella oleracea (L.) R.K. Jansen (Asteraceae) in patients with premature ejaculation. Material and Methods: After ethanolic extraction of A. oleracea inflorescences, a nanoformulation was developed, presented in spray. With base formulation (polysorbate surfactant (5% to 10%) and deionized water (90% to 95%) and incorporation of the extract into the base formulation (5% to 10% of the extract: 90% to 95% of the base formulation). Spilanthol analysis was performed using gas chromatography coupled to a mass spectrometer. The spray was prescribed for 12 weeks, being used 5 minutes before sexual intercourse. A clinical trial was carried out on participants, with physical examination, anamnesis, laboratory tests, before and after application of the topical formulation, in addition to recording the scores of Intravaginal Ejaculation Latency Time (IELT), International Index of Erectile Function, Hamilton Rating Scale. The sample number was obtained by free demand, from patients from the Urology and Andrology outpatient clinic, with the inclusion profile for the study, who signed a Free and Informed Consent Term. Ordinal variables were represented by descriptive statistics. The variable used to assess therapeutic efficacy was the mean IELT. Results were expressed as mean-standard deviation. Differences were considered significant if the p value was < 0.05. Results and Discussion: Spilanthol-based nanoformulation of A. oleracea increased the IELT value during spray use by participants compared to baseline. This fact is presumed due to the unique property of alkylamides to activate mechanosensitive neurons to anesthetics. Conclusions: The nanoformulation containing ethanolic extract standardized in spilanthol from A. oleracea can be an efficient alternative to improve sexual satisfaction. More studies are needed, especially a multicenter study, with a larger number of participants, due to the inclusion criteria required for the study.
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JOSIANE VIANA CRUZ
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Planning of new cyclooxygenase 2 inhibitors with potential anti-inflammatory activity from celecoxib: a bioinformatics approach
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Data: 24/06/2022
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Introduction: Cyclooxygenase 2 (COX-2) selective non-steroidal anti-inflammatory drugs were designed to avoid or even decrease the incidence of side effects of cyclooxygenase 1 (COX-1) inhibition. Cyclooxygenase 2 (COX-2) is an enzyme that acts as a target for the design of anti-inflammatory intermediates. Celecoxib was selected as a reference molecule to perform ligand-based virtual screening, in the search for structures with similar shape and electrostatic potential. Objective: The aim of this study was to design new cyclooxygenase 2 inhibitors with potential antiinflammatory activity from celecoxib through a bioinformatics approach. Material and methods: Virtual screening strategies were performed based on the ligand celecoxib, by searching for structures by similarity in the form of the Rapid Overlay of Chemical Structures (ROCS) “Top2000/base” and electrostatic potential of the Electrostatic Similarity calculations (EON) “ Top500/base” in eight commercially available databases, as well as ChemBridge (DIVERSet TM_ EXP), DIVERSet CORE Library (DIVERSet™-CL), ZINC drug database, ZINC natural stock, Drug@FDA BindingDB, IBS Natural subdivision, IBS Synthetic subdivision and Princeton. Afterwards, the pharmacokinetic predictions were screened using the QikProp program and the toxicological predictions filtered through the Derek and ProTox software. There was molecular coupling and refined based on affinity value and binding energy as standard template ligand celecoxib and rofecoxib. Afterwards, predictions were made on the Molinspiration server and in silico analysis of endocrine disruption. Then, the selected molecules follow the metabolism predictions and molecular dynamics simulations. Results and discussions: The search for structures based on the stereo-electronic space resulted in 4000 molecules that followed the pharmacokinetic screening, where a total of 2,702 and toxicological 947 structures were obtained, so that, after molecular docking, it happened in 2 structures. Conclusions: In molecular docking, there was higher binding affinity compared to rofecoxib on the COX-2 target for theoretical data. In predicting bioactivity, ZINC408709 and ZINC2090319 were considered biologically active. In the endocrine disruption analysis, it was established that the molecule ZINC2090319 strongly binds to the target related to cardiovascular risk in a desirable manner as a non-steroidal antagonist and ZINC408709 is associated with the treatment of inflammatory diseases similar to celecoxib. The metabolite generated in this theoretical study is less likely to have adverse effects. Despite the differences, the ZINC408709 molecule showed better stability for COX-2 during molecular dynamics simulation.
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LIZANDRA LIMA SANTOS
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DESENVOLVIMENTO DE FORMULAÇÃO BIOINSETICIDA A BASE DO ÓLEO ESSENCIAL DE Pogostemon cabine BENTH
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Data: 10/06/2022
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Introduction: The Pogostemon cablin (Blanco) Benth, popularly known as Oriza and Patchouli is a plant of the Lamiaceae family, which has several biologicals including antimicrobial, antioxidant, analgesic, anti-inflammatory, antithrombotic, antidepressant, cytotoxic and recognized entomotoxic potential that serves as a alternative strategy for the chemical control of Aedes aegypti. Objective: Thus, this work aims to develop a bioinsecticide formulation using the essential oil of the leaves of Pogostemon cablin Benth effective against the Aedypti vector. Material and Methods: The activity was essential for the phytochemical composition of the oil through Aspect Gas Chromatography and Nuclear Magnetic Resonance and the prediction of the insecticide was made in silica. The essential oil tested in ovicidal, pupicidal, larvicidal and repellent activities against A. aegypti according to the WHO methodology. The bioinsecticide formulation was formulated and elaborated with organoleptic properties; of the cream, a repellency test was carried out on A. aegypti. Identified Results and discussion: Of the identified groups, patchouli alcohol, αguayene, and aa-guayene, presented in greater abundance. The essential oil showed ovicidal and larvicidal activity < 20 ppm and the pupicidal activity > 300 ppm. An adulticidal analysis indicated that Aedes aegypti females were susceptible to a diagnostic dose of 20 μg.ml-1. The formulation did not show significant in the analysis of organs and the pH showed variability5,9, a result within the tolerability range. The cream formulation in a viable concentration at 200ppm of 100% protection in a period of 100% protection in a period of 180 min. Conclusions: P. species with projected concentration, and its specially designed cream combination an alternative for the vector control of A.egypti.
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LETHICIA BARRETO BRANDÃO
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TECHNOLOGICAL DEVELOPMENT OF FORMULATION BASED ON ESSENTIAL OIL FROM BASIL LEAVES (Ocimum basilicum inn.) FRONT OF Aedes aegypti
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Data: 10/06/2022
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Brazil is a country with great biodiversity, being considered one of the largest in the world. The objective of this work is to prepare a cream containing the essential oil of Ocimum basilicum, evaluating its accelerated stability and evaluation of the repellency test against the Aedes aegypti mosquito. Ovicide, larvicide, pupicidal and adulticide tests were performed. The main chemical constituents were Linalool (36.90%), Eucalyptol (9.95%), Estragole (7.57%), α-Bergamotene (6.67%) and τ-Cadinol (6.18%). The essential oil showed insecticidal action with LC50 73.5 μg.mL-1 for ovicidal activity, LC50 89.5 μg.mL-1 for larvicidal activity and LC50 816.5μg.mL-1 when evaluating the pupae. With regard to adulticidal activity, all concentrations tested showed activity. As for the residual evaluation, the oil showed that the concentrations of 100, 200 and 300 μg.mL-1 showed longer lasting responses than the other concentrations tested. The larvae, exposed to the oil of the species, showed changes in their morphology when compared to the control. Stability was evaluated in the following physicochemical parameters: temperature (environment, refrigerator and oven), centrifuge, pH and organoleptic characteristics. During the study, the organoleptic characteristics remained constant. The pH did not change. At room temperature and refrigerator there was no change. In the centrifuge and oven analysis, there was no phase separation and the organoleptic characteristics remained the same. The repellency test of the cream and essential oil showed a protection index of 97% and 95.67% in the 30 minutes after its application and in the time of 180 minutes it protected approximately 85% and 81%. The findings corroborate the potentiality of the species against the A. aegypti vector. In conclusion, O. basilicum cream can be considered a promising agent for the control of infectious disease vectors.
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SUSY ÉRIKA DE LIMA BARROS
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Study of the anti-inflammatory and anti-allergic activity of kefir and its postbiotic, kefiran: an alternative therapy in childhood food allergy
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Data: 21/01/2022
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Introduction: Food allergy is a public health problem, affecting the nutritional status and quality of life of people of all ages, especially children. Kefir demonstrates beneficial health effects, but studies are still needed on its main component: kefiran. Objectives: To evaluate the anti-inflammatory and anti-allergic activity of kefir and kefiran in silico and in vivo. Material and Methods: Chromatography of milk kefir grain extract was performed. In the in silico study, prediction of pharmacokinetic and toxicological properties, prediction of biological activity and simulation of molecular docking between kefiran and selected biological targets were performed. In the in vivo study in zebrafish, the acute toxicity of kefiran was evaluated through the limit test with histological analysis of gills, kidneys, liver and intestines. The anti-inflammatory and anti-allergic activity was evaluated through the intraperitoneal induction of dextran and histamine, with analysis of edema formation, behavior, white blood cell count and histology of the gills and intestine. Results and discussion: In chromatography, kefiran was identified as the main component. The in silico results showed low human and intestinal oral absorption; low logP value, low permeability in MDCK and Caco-2 cells, and inability to cross the blood-brain barrier. Kefiran did not present any alert for toxicity and showed potential for activities: anti-allergic, anti-inflammatory, antioxidant and immunostimulant. In docking, the highest affinity was with the VEGF target. In the in vivo study, kefiran did not cause changes in toxicity and showed an antiedematogenic effect via histamine, inhibiting the antiallergic and anti-inflammatory process. Conclusions: Therefore, kefiran is safe and can be used to develop medicines or functional foods for the prevention or treatment of allergic or inflammatory diseases, such as children's food allergies.
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