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1.
Arch Environ Contam Toxicol ; 87(1): 58-68, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38922419

RESUMO

Environmental stressors in aquatic organisms can be assessed using a bioenergetic approach based on the evaluation of changes in their physiological parameters. We evaluated the chronic effects of cadmium (Cd2+) on the energy balance as well as the survival, growth, metabolism, nitrogen excretion, hepatosomatic index, oxidized energy substrate, and osmoregulation of the shrimp Penaeus vannamei with the hypothesis that the high energy demand related to the homeostatic regulation of Cd2+could disrupt the energy balance and as a consequence, their physiological functions. The shrimp exposed to Cd2+ had higher mortality (30%), directed more energy into growth (33% of energy intake), ingested 10% more energy, and defecated less than control animals. Cd2+ exposure caused a tendency to decrease metabolism and ammonia excretion but did not alter the hepatosomatic index, type of energy substrate oxidized, and the hyperosmorregulatory pattern of the species. The Cd+2 exposure may have induced a trade-off response because there was a growth rate increase accompanied by increased mortality.


Assuntos
Cádmio , Metabolismo Energético , Penaeidae , Poluentes Químicos da Água , Animais , Cádmio/toxicidade , Penaeidae/efeitos dos fármacos , Penaeidae/fisiologia , Penaeidae/crescimento & desenvolvimento , Poluentes Químicos da Água/toxicidade , Metabolismo Energético/efeitos dos fármacos , Osmorregulação/efeitos dos fármacos
2.
Chem Biodivers ; 21(9): e202400686, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38923804

RESUMO

Pereskia aculeata has been widely investigated due to its anti-inflammatory potential. Among the metabolites found in this species are the phytosterols beta-sitosterol (ß-SIT) and stigmasterol (STIG). The objective of the study was to evaluate the anti-inflammatory and toxicity activities of the hexane partition of P. aculeata (PHEX), as well as ß-SIT and STIG. PHEX was prepared and the phytosterols were quantified. In terms of toxicity against L929 fibroblast cells, PHEX showed toxicity up to 200 µg/mL; STIG and ß-SIT showed toxicity up to 25 µg/mL. PHEX inhibited 66 % of nitric oxide radicals, while STIG and ß-SIT inhibited 33.73 % and 34.94 %, respectively. In an anti-inflammatory test against Zophobas morio larvae, all samples significantly reduced hemocyte levels. Additionally, the LD50 values were calculated: 229.6 mg/kg for PHEX, 101.5 mg/kg for STIG, and 103.8 mg/kg for ß-SIT. In conclusion, the study indicates that the phytosterols present in PHEX may contribute to its anti-inflammatory activity.


Assuntos
Anti-Inflamatórios , Larva , Óxido Nítrico , Estigmasterol , Animais , Larva/efeitos dos fármacos , Camundongos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Estigmasterol/farmacologia , Estigmasterol/química , Estigmasterol/isolamento & purificação , Óxido Nítrico/metabolismo , Óxido Nítrico/antagonistas & inibidores , Sitosteroides/farmacologia , Sitosteroides/química , Linhagem Celular , Fitosteróis/farmacologia , Fitosteróis/química , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/isolamento & purificação
3.
Nutrients ; 16(12)2024 Jun 18.
Artigo em Inglês | MEDLINE | ID: mdl-38931283

RESUMO

Carbohydrate counting is one of the dietary strategies used for the management of type 1 diabetes (T1DM), and counting proteins and fats allows individuals to achieve better glycemic and metabolic control, reducing glycemic variability and long-term complications. The aim of this paper is to analyze the factors associated with adherence to the protein- and fat-counting strategy in adults with T1DM. This cross-sectional study was conducted from November 2021 to June 2022 through an online questionnaire. We applied Pearson's Chi-square test with adjusted residual analysis and a binomial logistic regression test using SPSS software, version 24.0, considering p < 0.05 as indicative of statistical significance. There was an association between performing protein and lipid counting and having a higher education level, income exceeding three minimum wages, and having adequate glycated hemoglobin. Performing protein and lipid counting increased the chances of having adequate HbA1c by 4.3 times. Protein and lipid counting was a predictor of having adequate HbA1c. The results suggest that considering the practice of counting proteins and fats is important as a strategy to optimize glycemic control.


Assuntos
Diabetes Mellitus Tipo 1 , Proteínas Alimentares , Hemoglobinas Glicadas , Humanos , Diabetes Mellitus Tipo 1/sangue , Masculino , Adulto , Feminino , Estudos Transversais , Proteínas Alimentares/administração & dosagem , Hemoglobinas Glicadas/metabolismo , Hemoglobinas Glicadas/análise , Cooperação do Paciente , Pessoa de Meia-Idade , Gorduras na Dieta/administração & dosagem , Controle Glicêmico/métodos , Adulto Jovem , Inquéritos e Questionários , Glicemia/metabolismo
4.
Front Endocrinol (Lausanne) ; 14: 1215792, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37766694

RESUMO

Background: The Carbohydrate Counting (CC) is directly associated with achieving glycemic control by people with Type 1 Diabetes Mellitus (T1DM). Therefore, this study aims to analyze characteristics of the CC practice associated with the adequacy of glycated hemoglobin (HbA1c) in adults with T1DM in Brazil. Methods: The study was cross-sectional, carried out using an online form with questions about knowledge of CC, clinical, anthropometric, sociodemographic data, follow-up with health professionals and understanding of the concepts of CC. Pearson's chi-square test and binomial logistic regression analysis (p<0.05) were applied. Results: 173 adults participated, of which 57.2% had increased HbA1c (≥7%). Having the diabetes duration <10 years (p=0.006), performing the CC at lunch (p=0.040) and dinner (p=0.018), using specific applications to perform the CC (p=0.001), having learned to perform CC with a nutritionist (p=0.037) and knowing how to correctly define the concepts of food bolus (p=0.001), correction bolus (p<0.001) and insulin/carbohydrate ratio (p<0.001) was associated with having adequate HbA1c (<7%). Participants who were undergoing CC practice were 3.273 times more likely to have adequate HbA1c and participants with diabetes duration <10 years were 2.686 times more likely to have adequate HbA1c. Conclusion: It was concluded that variables transversal to CC favor adequate HbA1c values in adults with T1DM and that practicing CC and having a diabetes duration of less than 10 years are predictive factors of having adequate HbA1c.


Assuntos
Diabetes Mellitus Tipo 1 , Terapia Nutricional , Adulto , Humanos , Hemoglobinas Glicadas , Brasil/epidemiologia , Estudos Transversais
5.
Cancers (Basel) ; 15(12)2023 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-37370684

RESUMO

Acute myeloid leukemia (AML) is the most common form of acute leukemia in adults, with a 5-year overall survival rate of approximately 30%. Despite recent advances in therapeutic options, relapse remains the leading cause of death and poor survival outcomes. New drugs benefit specific small subgroups of patients with actionable therapeutic targets. Thus, finding new targets with greater applicability should be pursued. Olfactory receptors (ORs) are seven transmembrane G-protein coupled receptors preferentially expressed in sensory neurons with a critical role in recognizing odorant molecules. Recent studies have revealed ectopic expression and putative function of ORs in nonolfactory tissues and pathologies, including AML. Here, we investigated OR expression in 151 AML samples, 6400 samples of 15 other cancer types, and 11,200 samples of 51 types of healthy tissues. First, we identified 19 ORs with a distinct and major expression pattern in AML, which were experimentally validated by RT-PCR in an independent set of 13 AML samples, 13 healthy donors, and 8 leukemia cell lines. We also identified an OR signature with prognostic potential for AML patients. Finally, we found cancer-related genes coexpressed with the ORs in the AML samples. In summary, we conducted an extensive study to identify ORs that can be used as novel biomarkers for the diagnosis of AML and as potential drug targets.

6.
Food Res Int ; 170: 113013, 2023 08.
Artigo em Inglês | MEDLINE | ID: mdl-37316080

RESUMO

Fruits have relevant usefulness in the elaboration of nutraceutical compositions and, as it is considered a "natural medicine", its market has been growing exponentially each year. Fruits, in general, contain a large source of phytochemicals, carbohydrates, vitamins, amino acids, peptides and antioxidants that are of interest to be prepared as nutraceuticals. The biological properties of its nutraceuticals can range from antioxidant, antidiabetic, antihypertensive, anti-Alzheimer, antiproliferative, antimicrobial, antibacterial, anti-inflammatory, among others. Furthermore, the need for innovative extraction methods and products reveals the importance of developing new nutraceutical compositions. This review was developed by searching patents of nutraceuticals from January 2015 until January 2022 in Espacenet, the search database of the European Patent Office (EPO). Of 215 patents related to nutraceuticals, 43% (92 patents) were including fruits, mainly berries. A great number of patents were focused on the treatment of metabolic diseases, representing 45% of the total patents. The principal patent applicant was the United States of America (US), with 52%. The patents were applied by researchers, industries, research centers and institutes. It is important to highlight that from 92 fruit nutraceutical patent applications reviewed, 13 already have their products available on the market.


Assuntos
Suplementos Nutricionais , Frutas , Antioxidantes , Vitaminas , Aminoácidos
8.
Future Microbiol ; 17: 1421-1432, 2022 11.
Artigo em Inglês | MEDLINE | ID: mdl-36169343

RESUMO

Drugs used to fight fungal infections may cause toxic or adverse drug interactions. For this reason, there is an increase in the development of natural, semisynthetic and synthetic antifungal peptides. This study aimed to perform a patent review to identify the advances in peptides to treat fungal infections. In a preliminary assessment, 597 patents were identified from the database. Then, duplicated patents (62) and those with titles in disagreement with the scope of this review (196) were excluded. Then, six patents were not in English or Spanish. Following the screening, 288 patents were outside the focus of this review, according to their abstract and description. The final selection covered 45 patents.


Currently, medications used to treat fungal infections may interact negatively with other drugs or be hazardous to the host. Scientists have been looking for novel, safe and efficient antifungal drugs since the enhancement of fungal resistance. Antimicrobial peptides, as opposed to traditional antibiotics, offer a variety of antibacterial activity against bacteria, fungi, parasites, viruses and cancer cells. The production of isolated natural, semisynthetic and synthetic antifungal peptides has increased. As a result, patents are a reliable and up-to-date source of innovation. As a result, their content analysis provides crucial information for identifying trends in new medications and targeted treatment plans.


Assuntos
Antifúngicos , Micoses , Humanos , Antifúngicos/farmacologia , Antifúngicos/uso terapêutico , Micoses/tratamento farmacológico , Micoses/microbiologia , Peptídeos/farmacologia , Peptídeos/uso terapêutico
9.
Eur J Pharm Sci ; 175: 106222, 2022 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-35649471

RESUMO

The drug delivery systems are an important strategy of pharmaceutical technology to modulate undesirable properties, increasing efficacy, and reducing the side effects of active pharmaceutical ingredients (API). The sustained release is a type of controlled-release system that provides a suitable drug level in the blood through a slow release rate. An interesting alternative to achieve a controlled release is the application of carrier materials such as polymers, cyclodextrins, and clays. Sodium montmorillonite (Na-MMT) is a biocompatible natural clay that allows the insertion of organic compounds in interlamellar space, owing to its high cation exchange capacity and large internal surface area. Bromopride (BPD) is an aminated compound with antiemetic properties classified as class II (low solubility, high permeability) of the Biopharmaceutical Classification System (BCS). Herein, the aim of the study was the development and investigation of a drug delivery system formed by intercalation of BPD with Na-MMT. The results indicate the successful intercalation of this API with the lamellar silicate, meanwhile, there was no evidence of BPD intercalation in organic montmorillonite. The Na-MMT/BPD molecular complex exhibits a sustained release in performed assays. Molecular dynamics simulations suggested that BPD molecules interact with the montmorillonite layer through ion-dipole interactions and also between BPD molecules, forming hydrogen bonds web into montmorillonite interlayer space. The new drug delivery system showed an alternative to achieve the BPD sustained release, which may improve its pharmacological performance in therapeutic applications.


Assuntos
Bentonita , Metoclopramida , Bentonita/química , Argila , Preparações de Ação Retardada , Metoclopramida/análogos & derivados
10.
Aesthetic Plast Surg ; 46(1): 287-296, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-34750657

RESUMO

BACKGROUND: Obesity is considered a condition of systemic chronic inflammation. Under this condition, adipose tissue macrophages switch from an M2 (anti-inflammatory) activation pattern to an M1 (proinflammatory) activation pattern. OBJECTIVE: The study aimed to verify the profile of skin macrophage activation after bariatric surgery as well as the role of MMP-1 in extracellular tissue remodeling. METHODS: This is a prospective, controlled and comparative study with 20 individuals split into two groups according to their skin condition: post-bariatric and eutrophic patients. Histological and morphometric analyses based on hematoxylin-eosin, picrosirius red (collagen), orcein (elastic fiber systems), and alcian blue (mast cells)-stained sections and immunohistochemical analysis (CD68, iNOS, and mannose receptor) for macrophages and metalloproteinase-1 were performed. RESULTS: Post-bariatric skin showed an increase in inflammation, angiogenesis, CD68, M1 macrophages (P< 0.001), and mast cells (P< 0.01); a decrease in M2 macrophages (P< 0.01); and a significant decrease in the collagen fiber network (P< 0.001). MMP-1 was increased in the papillary dermis of post-bariatric skin and decreased in the epidermis compared to eutrophic skin (P< 0.05). CONCLUSION: This study shows that post-bariatric skin maintains inflammatory characteristics for two years. Mast cells and M1 macrophages maintain and enhance the remodeling of the dermal extracellular matrix initiated during obesity in part due to the presence of MMP-1 in the papillary dermis. EBM LEVEL IV: This journal requires that authors assign a level of evidence to each article. For a full description of these Evidence-Based Medicine ratings, please refer to the Table of Contents or the online Instructions to Authors www.springer.com/00266 .


Assuntos
Cirurgia Bariátrica , Bariatria , Cirurgia Bariátrica/efeitos adversos , Humanos , Macrófagos , Estudos Prospectivos , Pele
11.
NPJ Sci Food ; 5(1): 28, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34725351

RESUMO

Recently, many consumers have been adding plant-based beverages to their diets, due to different reasons. The addition of plant proteins to enrich these products in order to make them more nutritionally balanced has become a trend, mainly because of their lower prices and reduced environmental damage. Thus, the aims of the present patent review are to discuss the potential of, and challenges posed by, plant proteins to the beverage industry, as well as to check market trends, focused on raw materials and beverage types. Based on the results, pea, rapeseed, bean, peanut, chickpea, lentil, hempseed, sunflower seed, and cottonseed were among the most often addressed raw materials. Furthermore, this enrichment process is not limited to create products that mimic dairy, therefore expansion in plant proteins used to enrich carbonated beverages, sports drinks, or even juices is expected to happen. Thus, plant-derived proteins have been promising to high-quality beverage production, as well as to ensure food security, animal welfare, and low environmental impacts.

12.
J Pharm Pharmacol ; 72(12): 1933-1945, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32846458

RESUMO

OBJECTIVES: A previous study reported that the hexane fraction (HF) obtained from Pereskia aculeata leaves showed promising topical anti-inflammatory activity. Intending its future use in clinical practice, a herbal medicine cream named INFLATIV was developed. Its anti-inflammatory and antipsoriatic potential were investigated. INFLATIV was subjected to preliminary accelerated stability tests and to a degradation profile assessment. METHODS: INFLATIV was prepared at 6% and 12%. The anti-inflammatory activity was assessed by croton oil single and multiple application challenge in mice. Mouse tail test was used for antipsoriatic potential investigation. Cutaneous atrophy test was performed. Preliminary accelerated stability tests were performed together with a degradation profile by GC-MS analysis. KEY FINDINGS: The anti-inflammatory activity shown by INFLATIV was comparable to dexamethasone. However, the skin atrophy caused by that drug was not observed. INFLATIV modified skin parakeratotic differentiation into orthokeratosis, which revealed its antipsoriatic potential. The ingredients used were suitable to carry the bioactives as they were well permeated by the skin. The preliminary accelerated stability tests indicated that INFLATIV 6% is more stable than 12%. CONCLUSIONS: The results demonstrated the relevant therapeutic and marketing potentials of INFLATIV, which is likely to be further evaluated in clinical trials for drug registration process with regulatory agencies.


Assuntos
Anti-Inflamatórios/administração & dosagem , Cactaceae , Edema/prevenção & controle , Extratos Vegetais/administração & dosagem , Psoríase/tratamento farmacológico , Pele/efeitos dos fármacos , Administração Cutânea , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/metabolismo , Cactaceae/química , Óleo de Cróton , Modelos Animais de Doenças , Edema/induzido quimicamente , Edema/metabolismo , Edema/patologia , Masculino , Camundongos , Permeabilidade , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/metabolismo , Folhas de Planta , Psoríase/metabolismo , Psoríase/patologia , Pele/metabolismo , Pele/patologia , Absorção Cutânea , Creme para a Pele
13.
J Nat Prod ; 83(6): 1980-1989, 2020 06 26.
Artigo em Inglês | MEDLINE | ID: mdl-32453565

RESUMO

Our previous study showed that kaempferitrin, the main flavonoid from Bauhinia forficata Link leaves, induces diuresis and saluresis when orally given to rats. Since afzelin (AFZ) and kaempferol (KFL) are active compounds from the biometabolism of kaempferitrin, the diuretic and renal protective properties of these two compounds were evaluated. While the acute treatment with AFZ evoked a diuretic action associated with an increase in Cl- excretion and a Ca2+-sparing effect, KFL did not present any activity. The pretreatment with a muscarinic receptor blocker or with an inhibitor of the cyclooxygenase fully avoided AFZ-induced diuresis. AFZ also induced a prolonged (7-day treatment) diuretic effect in normotensive (NTR) and hypertensive rats (SHR), with an increase of urinary Na+ and Cl- excretion, while it decreased the elimination of Ca2+. AFZ was able to decrease ROS and nitrite generation on kidney homogenates in comparison with the SHR group treated with the vehicle, as well as mitigated the changes in the renal corpuscle region (glomerulus and Bowman's capsule). Moreover, AFZ significantly reduced calcium oxalate crystal formation in urine, with inhibition rates of 41% for the NTR and 92% for the SHR group. Taken together, this study shows that AFZ exerts acute and prolonged diuretic effects plus protective renal properties.


Assuntos
Diuréticos/farmacologia , Hipertensão/tratamento farmacológico , Quempferóis/farmacologia , Nefropatias/prevenção & controle , Manosídeos/farmacologia , Proantocianidinas/farmacologia , Substâncias Protetoras/farmacologia , Animais , Antioxidantes/farmacologia , Bauhinia/química , Cálcio/metabolismo , Cloretos/metabolismo , Inibidores de Ciclo-Oxigenase/farmacologia , Nefropatias/patologia , Estrutura Molecular , Antagonistas Muscarínicos/farmacologia , Folhas de Planta/química , Ratos , Ratos Endogâmicos SHR , Ratos Wistar , Espécies Reativas de Oxigênio/metabolismo
14.
Anat Rec (Hoboken) ; 303(11): 2857-2864, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-32134212

RESUMO

Therapeutic immobilization is a common treatment for the locomotor system; however, it causes loss of muscle due to disuse, leading to protein degradation and generating atrophy of muscle cells, ultimately changing functionality. In this sense, it is important for remobilization to be initiated early and performed with appropriate therapeutic strategies that enable tissue and functional recovery. One method of remobilization is physical exercise, among which whole body vibration (WBV) has been highlighted and mainly applied in people with reduced mobility. However, there are gaps on the morphological effects WBV has on muscle tissue, so in this study we analyzed the histomorphometry of the tibialis anterior muscle (TA) of Wistar rats remobilized using WBV. For the experiment, 32 male Wistar rats were used and divided into four groups (n = 8/group). Groups consisted of: control (CG), immobilized (IG), immobilized and remobilized freely (FG), and immobilized and remobilized with WBV (WG). After the experimental period, the TA was collected and processed for analysis in light microscopy. When compared to the control group, significant morphological changes were observed, which characterize muscle atrophy and reduction of all histomorphometric parameters of the TA of the immobilized animals. Remobilized animals showed improvement in all parameters, and the WBV was not different from the free remobilization, except for the reduction of central nuclei, which can be related to acceleration of the process of tissue regeneration. Thus, we can conclude that the WBV can have an impact on the acceleration of the muscle regenerative process, and may be beneficial in people with reduced mobility.


Assuntos
Imobilização/efeitos adversos , Músculo Esquelético/fisiopatologia , Atrofia Muscular/terapia , Recuperação de Função Fisiológica/fisiologia , Vibração/uso terapêutico , Animais , Eletromiografia , Masculino , Atrofia Muscular/etiologia , Atrofia Muscular/fisiopatologia , Ratos , Ratos Wistar
15.
Surg. cosmet. dermatol. (Impr.) ; 12(4 S2): 156-158, fev.-nov. 2020.
Artigo em Português | LILACS-Express | LILACS | ID: biblio-1367836

RESUMO

O carcinoma basocelular (CBC), quando acomete a região periorbicular, localiza-se mais comumente em região palpebral inferior. Ocorre predominantemente nos homens, entre 50-70 anos, apresenta alta taxa de recidiva, pode ocorrer invasão orbitária e raramente metastatiza-se. O objetivo deste trabalho é apresentar um caso de CBC pigmentado de localização incomum. A localização do CBC em região de pálpebra superior é rara, e a dermatoscopia é fundamental para identificá-lo e diferenciá-lo em relação a seus principais diagnósticos diferenciais.


Basal cell carcinoma (BCC) is more common in the lower eyelid region when it affects the periorbital region. It occurs predominantly in men between 50-70 years and has a high recurrence rate. Although it rarely metastasizes, orbital invasion can occur. This study aims to present a case of pigmented BCC of unusual location. The location of BCC in the upper eyelid region is rare, and dermoscopy is essential to distinguish it from its primary differential diagnoses.

16.
Surg. cosmet. dermatol. (Impr.) ; 12(4 S2): 159-162, fev.-nov. 2020.
Artigo em Português | LILACS-Express | LILACS | ID: biblio-1367837

RESUMO

O dermatofibroma (DF) aneurismático é um tumor benigno raro, de origem na derme, considerado uma variante de dermatofibroma. É prevalente nos membros inferiores de mulheres acima de 30 anos. Sua etiologia é desconhecida, e o exame histopatológico confirma o diagnóstico. Este trabalho apresenta dois casos de DF aneurismático, em pacientes jovens, do sexo masculino, e com lesões semelhantes: nódulo hipercrômico único, de aproximadamente 1,5cm e crescimento progressivo. O objetivo deste relato é demonstrar uma variante pouco frequente de dermatofibroma e ressaltar o possível diagnóstico diferencial com outros tumores por meio do exame dermatoscópico.


Aneurysmal dermatofibroma (DF) is a rare benign tumor originating in the dermis, considered a variant of dermatofibroma. It is more prevalent in women over 30 years of age, in the lower limbs. Its etiology is unknown and histopathological examination confirms the diagnosis. This study reports two cases of aneurysmal DF in young patients, both men, presenting similar lesions: single hyperchromic nodule, with approximately 1.5 cm and progressive growth. This report aims to demonstrate an uncommon variant of dermatofibroma and to highlight the possible differential diagnosis with other tumors through dermoscopic examination

17.
Med Chem ; 16(6): 774-783, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31244442

RESUMO

BACKGROUND: Although several research efforts have been made worldwide to discover novel drug candidates for the treatment of Chagas disease, the nitroimidazole drug benznidazol remains the only therapeutic alternative in the control of this disease. However, this drug presents reduced efficacy in the chronic form of the disease and limited safety after long periods of administration, making it necessary to search for new, more potent and safe prototypes. OBJECTIVE: We described herein the synthesis and the trypanocidalaction of new functionalized carbohydrazonamides (2-10) against trypomastigote forms of Trypanosoma cruzi. METHODS: These compounds were designed through the application of molecular hybridization concept between two potent anti-T. cruzi prototypes, the nitroimidazole derivative megazol (1) and the cinnamyl N-acylhydrazone derivative (14) which have been shown to be twice as potent in vitro as benznidazole. RESULTS: The most active compounds were the (Z)-N'-((E)-3-(4-nitrophenyl)-acryloyl)-1-methyl-5- nitro-1H-imidazol-2-carbohydrazonamide (6) (IC50=9.50 µM) and the (Z)-N'-((E)-3-(4- hydroxyphe-nyl)-acryloyl)-1-methyl-5-nitro-1H-imidazol-2-carbohydrazonamide (8) (IC50=12.85 µM), which were almost equipotent to benznidazole (IC50=10.26 µM) used as standard drug. The removal of the amine group attached to the imine subunit in the corresponding N-acylhydrazone derivatives (11-13) resulted in less potent or inactive compounds. The para-hydroxyphenyl derivative (8) presented also a good selectivity index (SI = 32.94) when tested against mammalian cells from Swiss mice. CONCLUSION: The promising trypanocidal profile of new carbohydrazonamide derivatives (6) and (8) was characterized. These compounds have proved to be a good starting point for the design of more effective trypanocidal drug candidates.


Assuntos
Doença de Chagas/tratamento farmacológico , Tripanossomicidas/síntese química , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Animais , Células Cultivadas , Desenho de Fármacos , Macrófagos Peritoneais/efeitos dos fármacos , Camundongos , Modelos Moleculares , Estrutura Molecular , Relação Estrutura-Atividade , Tripanossomicidas/química
18.
Int J Nurs Knowl ; 31(2): 109-123, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31339006

RESUMO

PURPOSE: To elucidate six diagnostic concepts related to urinary incontinence (UI). METHODS: Eight out of nine steps of the simultaneous concept analysis (SCA) method were used to elucidate six diagnostic concepts related to UI proposed by NANDA International. FINDINGS: Individual concepts of each diagnosis were elucidated, including antecedents, outcomes, associated conditions, and risk populations, and the interrelations among these concepts were identified, comparing them to those already present in the current NANDA-I taxonomy. The overflow UI was excluded, and were included mixed and transient UI diagnoses. CONCLUSIONS: SCA enabled identifying similar characteristics and factors exclusive to the revised nursing diagnoses. IMPLICATIONS FOR NURSING PRACTICE: To support for clinical reasoning to identify properly the types of UI. OBJETIVO: Elucidar seis conceitos diagnósticos relacionados à incontinência urinária. MÉTODOS: Oito das nove etapas do método de análise simultânea de conceitos foram utilizadas para elucidar seis conceitos diagnósticos relacionados à incontinência urinária propostos pela NANDA International. RESULTADOS: Conceitos individuais de cada diagnóstico foram elucidados, incluindo antecedentes, consequentes, condições associadas e populações em risco, e as inter-relações entre esses conceitos foram identificadas, comparando-as com aquelas já presentes na atual taxonomia da NANDA-I. A incontinência urinária por transbordamento foi excluída e foram incluídos os diagnósticos de incontinência urinária mista e incontinência urinária transitória. CONCLUSÕES: A análise simultânea de conceitos permitiu identificar características e fatores semelhantes exclusivos aos diagnósticos de enfermagem revisados. IMPLICAÇÕES PARA A PRÁTICA DE ENFERMAGEM: Apoiar o raciocínio clínico para identificar adequadamente os tipos de incontinência urinária.


Assuntos
Incontinência Urinária/diagnóstico , Formação de Conceito , Humanos , Terminologia Padronizada em Enfermagem
19.
Med Chem ; 16(4): 487-494, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31309899

RESUMO

BACKGROUND: Approximately, 5-7 million people are infected with T. cruzi in the world, and approximately 10,000 people per year die of complications linked to this disease. METHODS: This work describes the construction of a new family of hidrazonoyl substituted derivatives, structurally designed exploring the molecular hybridization between megazol and nitrofurazone. RESULTS AND DISCUSSION: The compounds were evaluated for their in vitro activity against bloodstream trypomastigotes of Trypanosoma cruzi, etiological agent of Chagas disease, and for their potential toxicity to mammalian cells. CONCLUSION: Among these hydrazonoyl derivatives, we identified the derivative (4) that showed trypanocidal activity (IC50/24 h = 15.0 µM) similar to Bz, the standard drug, and low toxicity to mammalian cells, reaching an SI value of 18.7.


Assuntos
Hidrazonas/síntese química , Hidrazonas/farmacologia , Tripanossomicidas/síntese química , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Animais , Linhagem Celular , Técnicas de Química Sintética , Hidrazonas/química , Relação Estrutura-Atividade , Tripanossomicidas/química
20.
An Bras Dermatol ; 94(5): 590-593, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31777362

RESUMO

The correct identification of pigmented nodular lesions of the scalp is often challenging. Despite the importance of clinical patterns and dermoscopy, important adjuvant tools that are usually helpful, their interpretation sometimes is not clear-cut. Here, the authors discuss a case of sebaceoma mimicking a malignant pigmented neoplasia, with conclusive histopathology.


Assuntos
Carcinoma/patologia , Couro Cabeludo/patologia , Neoplasias das Glândulas Sebáceas/patologia , Neoplasias Cutâneas/patologia , Idoso de 80 Anos ou mais , Biópsia , Carcinoma/diagnóstico , Dermoscopia , Diagnóstico Diferencial , Feminino , Humanos , Imuno-Histoquímica , Neoplasias das Glândulas Sebáceas/diagnóstico , Neoplasias Cutâneas/diagnóstico
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