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1.
Cir Esp (Engl Ed) ; 102(4): 227, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-37956713
2.
Med Res Rev ; 43(6): 1878-1945, 2023 11.
Artigo em Inglês | MEDLINE | ID: mdl-37147865

RESUMO

One of the hallmarks of cancer is metastasis, a process that entails the spread of cancer cells to distant regions in the body, culminating in tumor formation in secondary organs. Importantly, the proinflammatory environment surrounding cancer cells further contributes to cancer cell transformation and extracellular matrix destruction. During metastasis, front-rear polarity and emergence of migratory and invasive features are manifestations of epithelial-mesenchymal transition (EMT). A variety of transcription factors (TFs) are implicated in the execution of EMT, the most prominent belonging to the Snail Family Transcriptional Repressor (SNAI) and Zinc Finger E-Box Binding Homeobox (ZEB) families of TFs. These TFs are regulated by interaction with specific microRNAs (miRNAs), as miR34 and miR200. Among the several secondary metabolites produced in plants, flavonoids constitute a major group of bioactive molecules, with several described effects including antioxidant, antiinflammatory, antidiabetic, antiobesogenic, and anticancer effects. This review scrutinizes the modulatory role of flavonoids on the activity of SNAI/ZEB TFs and on their regulatory miRNAs, miR-34, and miR-200. The modulatory role of flavonoids can attenuate mesenchymal features and stimulate epithelial features, thereby inhibiting and reversing EMT. Moreover, this modulation is concomitant with the attenuation of signaling pathways involved in diverse processes as cell proliferation, cell growth, cell cycle progression, apoptosis inhibition, morphogenesis, cell fate, cell migration, cell polarity, and wound healing. The antimetastatic potential of these versatile compounds is emerging and represents an opportunity for the synthesis of more specific and potent agents.


Assuntos
MicroRNAs , Neoplasias , Humanos , Transição Epitelial-Mesenquimal , Flavonoides/farmacologia , Homeobox 1 de Ligação a E-box em Dedo de Zinco/metabolismo , Neoplasias/tratamento farmacológico , Fatores de Transcrição , MicroRNAs/genética , MicroRNAs/metabolismo , Transdução de Sinais , Regulação Neoplásica da Expressão Gênica , Linhagem Celular Tumoral , Metástase Neoplásica
3.
Rev. bras. psicodrama ; 31: e0323, 2023.
Artigo em Português | LILACS-Express | LILACS, INDEXPSI | ID: biblio-1423659

RESUMO

RESUMO O presente artigo apresenta uma reflexão sobre o ancoramento científico da pesquisa e das práticas psicodramáticas, questionando a perspectiva colonial/moderna predominante no universo da ciência ocidental, e sugerindo uma aproximação com o pensamento decolonial que se desenvolve no século XXI, em que são retomadas epistemologias historicamente desconsideradas, como aquela em que se situam os princípios filosóficos morenianos. As questões discutidas acerca da pesquisa em Psicodrama podem ser transportadas para o campo das práticas, gerando questionamentos quanto ao lugar do psicodramatista na relação com o outro, a forma de elaboração dos problemas/hipóteses terapêuticas e o que se espera das intervenções, situando-as para além dos binarismos tradicionais modernos.


ABSTRACT This article reflects on the scientific anchoring of psychodramatic research and practice, questioning the colonial/modern perspective prevailing in the universe of Western science, and suggesting an approach to the decolonial thinking developed in the 21st century, in which historically disregarded epistemologies are resumed, such as the one in which the philosophical principles of Moreno's work are located. The questions discussed about research in Psychodrama can be transported to the field of practices, generating questions related to the place of the psychodramatist in the relationship with the other, the way of elaborating the therapeutic problems/hypotheses and what is expected of the interventions, placing them beyond traditional modern binarisms.


RESUMEN Este artículo reflexiona sobre el anclaje científico de la investigación y la práctica psicodramática, cuestionando la perspectiva colonial/moderna predominante en el universo de la ciencia occidental, y proponiendo una aproximación al pensamiento decolonial que se desarrolla en el siglo XXI, en el que se retoman epistemologías históricamente desconsideradas, como aquél en el que se ubican los principios filosóficos de la obra Moreniana. Las cuestiones discutidas sobre la investigación en Psicodrama pueden ser transportadas al campo de las prácticas, generando interrogantes sobre el lugar del psicodramatista en la relación con el otro, la forma de elaborar los problemas/hipótesis terapéuticas y lo que se espera de las intervenciones, ubicándolas más allá de los binarismos modernos tradicionales.

4.
Molecules ; 27(5)2022 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-35268802

RESUMO

Tomato producing and processing industries present undoubted potential for industrial discarded products valorization whether due to the overproduction of fresh tomatoes or to the loss during processing. Although tomato by-products are not yet considered a raw material, several studies have suggested innovative and profitable applications. It is often referred to as "tomato pomace" and is quite rich in a variety of bioactive compounds. Lycopene, vitamin C, ß-carotene, phenolic compounds, and tocopherol are some of the bioactives herein discussed. Tomato by-products are also rich in minerals. Many of these compounds are powerful antioxidants with anti-inflammatory properties besides modulating the immune system. Several researchers have focused on the possible application of natural ingredients, especially those extracted from foods, and their physiological and pharmacological effects. Herein, the effects of processing and further applications of the bioactive compounds present in tomato by-products were carefully reviewed, especially regarding the anti-inflammatory and anti-cancer effects. The aim of this review was thus to highlight the existing opportunities to create profitable and innovative applications for tomato by-products in health context.


Assuntos
Solanum lycopersicum
5.
Crit Rev Food Sci Nutr ; 62(15): 4095-4151, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33554619

RESUMO

Type 2 diabetes (T2D) is an expanding global health problem, resulting from defects in insulin secretion and/or insulin resistance. In the past few years, both protein tyrosine phosphatase 1B (PTP1B) and dipeptidyl peptidase-4 (DPP-4), as well as their role in T2D, have attracted the attention of the scientific community. PTP1B plays an important role in insulin resistance and is currently one of the most promising targets for the treatment of T2D, since no available PTP1B inhibitors were still approved. DPP-4 inhibitors are among the most recent agents used in the treatment of T2D (although its use has been associated with possible cardiovascular adverse events). The antidiabetic properties of flavonoids are well-recognized, and include inhibitory effects on the above enzymes, although hitherto not therapeutically explored. In the present study, a comprehensive review of the literature of both synthetic and natural isolated flavonoids as inhibitors of PTP1B and DPP-4 activities is made, including their type of inhibition and experimental conditions, and structure-activity relationship, covering a total of 351 compounds. We intend to provide the most favorable chemical features of flavonoids for the inhibition of PTP1B and DPP-4, gathering information for the future development of compounds with improved potential as T2D therapeutic agents.


Assuntos
Diabetes Mellitus Tipo 2 , Dipeptidil Peptidase 4/metabolismo , Inibidores da Dipeptidil Peptidase IV , Resistência à Insulina , Diabetes Mellitus Tipo 2/tratamento farmacológico , Inibidores da Dipeptidil Peptidase IV/química , Inibidores da Dipeptidil Peptidase IV/farmacologia , Inibidores da Dipeptidil Peptidase IV/uso terapêutico , Inibidores Enzimáticos/química , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Humanos , Hipoglicemiantes/química , Monoéster Fosfórico Hidrolases/uso terapêutico , Relação Estrutura-Atividade
6.
J Photochem Photobiol B ; 223: 112301, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34492530

RESUMO

Prostate cancer (PCa) is the second most frequent cancer diagnosed in men worldwide. Among the common treatment options, photodynamic therapy (PDT) is being considered a promising local therapy to treat this cancer. Although PDT is an established treatment modality approved for several types of cancer, the low solubility, the reduced tumor selectivity, the absorption in the therapeutic window and the poor clearance from the body of the currently approved photosensitizers (PS) hampers its wide clinical application. In this regard, herein we synthesized three fluorinated porphyrinoid derivatives and entrapped them into polyvinylpyrrolidone (PVP) to prevent their aggregation and preserve their desirable photophysical properties under the physiological environment. In vitro studies revealed the negligible dark cytotoxicity of all PVP formulations (PS1@PVP, PS2@PVP and PS3@PVP) at the tested concentrations (5.0 to 20 µM), but also confirmed the significant photodynamic effect of PS2@PVP and PS3@PVP towards the PCa cell line PC-3, upon red light irradiation at an irradiance of 17.6 mW.cm-2. To provide insight into the underlying mechanisms of cell death under PDT treatment induced by PS2@PVP and PS3@PVP, their intracellular localization in PC-3 cells was firstly investigated by confocal microscopy. Since both PS2@PVP and PS3@PVP nanoparticles were mainly localized in mitochondria, the involvement of this organelle in PDT-induced apoptosis mediated by both formulations was further explored. Western blot analysis revealed that PDT treatment of PC-3 cells with either PS2@PVP or PS3@PVP resulted in the reduction of the expression level of the anti-apoptotic protein Bcl-2. As the photodamage to Bcl-2 after PDT with PS2@PVP and PS3@PVP was accompanied by the further activation of pro-caspase-3, we assumed that upon irradiation the photogenerated reactive oxygen species (ROS) were able to activate a caspase-dependent apoptotic response as a consequence of a post-mitochondrial event. Taken together, these findings demonstrate that among the tested fluorinated porphyrinoids, PS2@PVP and, particularly, PS3@PVP, are significantly more effective in overall PC-3 cell killing than PS1@PVP, thus highlighting their great potential as therapeutic agents for PCa.


Assuntos
Apoptose/efeitos dos fármacos , Fármacos Fotossensibilizantes/farmacologia , Porfirinas/farmacologia , Caspase 3/metabolismo , Linhagem Celular Tumoral , Regulação para Baixo/efeitos dos fármacos , Composição de Medicamentos , Humanos , Masculino , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Nanopartículas/química , Fotoquimioterapia , Fármacos Fotossensibilizantes/química , Fármacos Fotossensibilizantes/uso terapêutico , Porfirinas/química , Porfirinas/uso terapêutico , Povidona/química , Neoplasias da Próstata/tratamento farmacológico , Neoplasias da Próstata/patologia , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Espécies Reativas de Oxigênio/metabolismo
7.
Pharmacol Res ; 169: 105604, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-33845125

RESUMO

Diabetes mellitus is one of the biggest health emergencies of the 21st century worldwide, characterized by deficiency in insulin secretion and/or action, leading to hyperglycemia. Despite the currently available antidiabetic therapeutic options, 4.2 million people died in 2019 due to diabetes. Thus, new effective interventions are required. Polyphenols are plant secondary metabolites and have been recognized for their vast number of biological activities, including potential antidiabetic effects. However, the poor bioavailability and high metabolization of polyphenols restrict their biological effects in vivo. Nanotechnology is a promising area of research to improve the therapeutic effect of several compounds. Therefore, this review provides an overview of the literature about the utility of nano-based drug delivery systems as vehicles of polyphenols in diabetes treatment. It was possible to conclude that, in general, nano-based drug delivery systems can potentiate the beneficial antidiabetic properties of polyphenols, when compared with the free compounds, opening a new field of research in diabetology.


Assuntos
Diabetes Mellitus Tipo 1/tratamento farmacológico , Hipoglicemiantes/administração & dosagem , Sistemas de Liberação de Fármacos por Nanopartículas , Animais , Humanos , Hipoglicemiantes/uso terapêutico , Sistemas de Liberação de Fármacos por Nanopartículas/administração & dosagem
8.
Oxid Med Cell Longev ; 2021: 2804521, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34987699

RESUMO

Styrylchromones (SC) are a group of oxygen-containing heterocyclic compounds, which are characterized by the attachment of a styryl group to the chromone core. SC can be found in nature or can be chemically synthesized in the laboratory. As their presence in nature is scarce, the synthetic origin is the most common. Two types of SC are known: 2-styrylchromones and 3-styrylchromones. However, 2-styrylchromones are the most common, being more commonly found in nature and which chemical synthesis is more commonly described. A wide variety of SC has been described in the literature, with different substituents in different positions, the majority of which are distributed on the A- and/or B-rings. Over the years, several biological activities have been attributed to SC. This work presents a comprehensive review of the biological activities attributed to SC and their structure-activity relationship, based on a published literature search, since 1989. The following biological activities are thoroughly revised and discussed in this review: antioxidant, antiallergic, antiviral, antibacterial, antifungal, anti-inflammatory, and antitumoral, affinity and selectivity for A3 adenosine receptors, neuroprotective, and α-glucosidase inhibition. In general, SC are composed by a promising scaffold with great potential for the development of new drugs.


Assuntos
Cromonas/química , Humanos , Relação Estrutura-Atividade
9.
Einstein (Säo Paulo) ; 19: eAO6451, 2021. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1350702

RESUMO

ABSTRACT Objective: To characterize the situation of breastfeeding and the adequacy of prescription of infant formulas to infants assisted by a secondary care program of the Public Health System. Methods: This is a cross-sectional study with analysis of medical records of 350 infants from zero to 6 months, followed up between February to April 2019. Results: The possibility of breastfeeding was present in 97.0% of mothers and no infant presented an acceptable medical condition for proscription of breastfeeding. Despite this, only 47.2% of cases were on exclusive breastfeeding before being referred to the program. Regarding the reasons for the introduction of infant formulas, complementation to breast milk was the most present (75.8%), followed by mothers returning to the job market (20.1%). The general rates of inadequacy of those prescribed were 65% before arriving at the program, increasing to 69% (standard formulas) and 80% (formulas for special purposes) during follow-up. Conclusion: The low rate of exclusive breastfeeding and the indiscriminate prescription of infant formulas are a concern for damage to maternal-child healthcare and sound finances of the Public Health System.


RESUMO Objetivo: Caracterizar a situação de aleitamento materno e da adequação de prescrição de fórmulas infantis a lactentes assistidos por um programa de Atenção Secundária do Sistema Único de Saúde. Métodos: Trata-se de estudo transversal pela análise de prontuários de 350 lactentes de zero a 6 meses, acompanhados entre fevereiro a abril de 2019. Resultados: A possibilidade de aleitamento materno esteve presente em 97,0% das mães, e nenhum lactente apresentou condição médica aceitável para a proscrição do aleitamento materno. Apesar disso, apenas 47,2% dos casos estavam em aleitamento materno exclusivo antes do encaminhamento ao programa. Em relação aos motivos da introdução das fórmulas infantis, a complementação ao leite materno foi o mais presente (75,8%), seguido da volta da mãe ao mercado de trabalho (20,1%). As taxas gerais de inadequação dentre os prescritos foram de 65% antes da chegada ao programa, passando para 69% (fórmulas padrão) e 80% (fórmulas para fins especiais) durante o acompanhamento. Conclusão: A baixa taxa de aleitamento materno exclusivo e a prescrição indiscriminada de fórmulas infantis são preocupantes por causar prejuízos à saúde maternoinfantil e financeira do Sistema Único de Saúde.


Assuntos
Humanos , Feminino , Lactente , Aleitamento Materno , Fórmulas Infantis , Saúde Pública , Estudos Transversais , Mães
10.
Cancers (Basel) ; 12(11)2020 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-33121137

RESUMO

Reprogramming of lipid metabolism directly contributes to malignant transformation and progression. The increased uptake of circulating lipids, the transfer of fatty acids from stromal adipocytes to cancer cells, the de novo fatty acid synthesis, and the fatty acid oxidation support the central role of lipids in many cancers, including prostate cancer (PCa). Fatty acid ß-oxidation is the dominant bioenergetic pathway in PCa and recent evidence suggests that PCa takes advantage of the peroxisome transport machinery to target monocarboxylate transporter 2 (MCT2) to peroxisomes in order to increase ß-oxidation rates and maintain the redox balance. Here we show evidence suggesting that PCa streamlines peroxisome metabolism by upregulating distinct pathways involved in lipid metabolism. Moreover, we show that MCT2 is required for PCa cell proliferation and, importantly, that its specific localization at the peroxisomal membranes is essential for this role. Our results highlight the importance of peroxisomes in PCa development and uncover different cellular mechanisms that may be further explored as possible targets for PCa therapy.

11.
Cien Saude Colet ; 25(4): 1361-1374, 2020 Mar.
Artigo em Português, Inglês | MEDLINE | ID: mdl-32267438

RESUMO

This paper aims to present a debate on the new Brazilian Primary Health Care (PHC) funding policy. We consulted the national and international literature, and we involved municipal, state, and federal PHC managers to develop the payment method. The proposed final model is based on weighted capitation, payment-for-performance, and incentive for strategic actions. Capitation is weighted by the socioeconomic vulnerability, demographic aspects, and municipal adjustment, the payment-for-performance consists of an entire set of 21 indicators, and incentives for strategic actions were facilitated from the maintenance of some specific programs. The results of the simulations pointed to low registration (90 million Brazilians) for the currently estimated coverage (148,674,300 Brazilians). Moreover, they showed an immediate increase in financial resources for 4,200 Brazilian municipalities. We observed that the funding proposal brings Brazilian PHC into the 21st century, points to the strengthening of PHC attributes, and materializes the principles of universality and equity of the Unified Health System.


O objetivo desse artigo é apresentar um debate sobre a nova política de financiamento para Atenção Primária à Saúde (APS) no Brasil. Para desenvolvimento do método de pagamento foi realizado consulta da literatura nacional e internacional, além do envolvimento de gestores municipais, estaduais e federais da APS. O modelo final proposto é baseado em Capitação ponderada; Pagamento por desempenho; Incentivo para Ações Estratégicas. A capitação é ponderada por vulnerabilidade socioeconômica, aspectos demográficos e ajuste municipal, o pagamento por desempenho composto por um conjunto total de 21 indicadores e incentivos a ações estratégicas foi possível a partir da manutenção de alguns programas específicos. Os resultados das simulações apontaram para um baixo cadastro (90 milhões de brasileiros) para a cobertura estimada atual (148.674.300 milhões de brasileiros). Além disso, demonstraram um incremento imediato de recursos financeiros para 4.200 municípios brasileiros. Observa-se que a proposta do financiamento traz a APS brasileira para o século XXI, aponta para o fortalecimento dos atributos da APS e torna concreto os princípios de universalidade e equidade do Sistema Único de Saúde.


Assuntos
Capitação , Financiamento Governamental , Programas Nacionais de Saúde/economia , Atenção Primária à Saúde/economia , Reembolso de Incentivo , Brasil , Financiamento Governamental/legislação & jurisprudência , Humanos , Programas Nacionais de Saúde/legislação & jurisprudência
12.
Turk Arch Otorhinolaryngol ; 58(1): 48-51, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32313895

RESUMO

Cat-scratch disease (CSD) is one of the most common causes of infectious cervicofacial lymphadenopathies in children, adolescents, and young adults. With this case report, we highlight the wide spectrum of atypical manifestations of CSD in an elderly patient who presented not only with cervicofacial lymphadenopathies but also parotid enlargement, and Parinaud's oculoglandular syndrome which comprises granulomatous nonsuppurative conjunctivitis with adjacent ipsilateral preauricular lymphadenopathy. A high index of suspicion is needed to correctly diagnose and treat this clinical entity.

13.
Ciênc. Saúde Colet. (Impr.) ; 25(4): 1361-1374, abr. 2020. tab, graf
Artigo em Português | LILACS | ID: biblio-1089507

RESUMO

Resumo O objetivo desse artigo é apresentar um debate sobre a nova política de financiamento para Atenção Primária à Saúde (APS) no Brasil. Para desenvolvimento do método de pagamento foi realizado consulta da literatura nacional e internacional, além do envolvimento de gestores municipais, estaduais e federais da APS. O modelo final proposto é baseado em Capitação ponderada; Pagamento por desempenho; Incentivo para Ações Estratégicas. A capitação é ponderada por vulnerabilidade socioeconômica, aspectos demográficos e ajuste municipal, o pagamento por desempenho composto por um conjunto total de 21 indicadores e incentivos a ações estratégicas foi possível a partir da manutenção de alguns programas específicos. Os resultados das simulações apontaram para um baixo cadastro (90 milhões de brasileiros) para a cobertura estimada atual (148.674.300 milhões de brasileiros). Além disso, demonstraram um incremento imediato de recursos financeiros para 4.200 municípios brasileiros. Observa-se que a proposta do financiamento traz a APS brasileira para o século XXI, aponta para o fortalecimento dos atributos da APS e torna concreto os princípios de universalidade e equidade do Sistema Único de Saúde.


Abstract This paper aims to present a debate on the new Brazilian Primary Health Care (PHC) funding policy. We consulted the national and international literature, and we involved municipal, state, and federal PHC managers to develop the payment method. The proposed final model is based on weighted capitation, payment-for-performance, and incentive for strategic actions. Capitation is weighted by the socioeconomic vulnerability, demographic aspects, and municipal adjustment, the payment-for-performance consists of an entire set of 21 indicators, and incentives for strategic actions were facilitated from the maintenance of some specific programs. The results of the simulations pointed to low registration (90 million Brazilians) for the currently estimated coverage (148,674,300 Brazilians). Moreover, they showed an immediate increase in financial resources for 4,200 Brazilian municipalities. We observed that the funding proposal brings Brazilian PHC into the 21st century, points to the strengthening of PHC attributes, and materializes the principles of universality and equity of the Unified Health System.


Assuntos
Humanos , Atenção Primária à Saúde/economia , Reembolso de Incentivo , Capitação , Financiamento Governamental/legislação & jurisprudência , Programas Nacionais de Saúde/economia , Brasil , Programas Nacionais de Saúde/legislação & jurisprudência
14.
Cancers (Basel) ; 12(3)2020 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-32164347

RESUMO

Human papillomaviruses (HPV) are the causative agents of the most common sexually transmitted infection worldwide. While infection is generally asymptomatic and can be cleared by the host immune system, when persistence occurs, HPV can become a risk factor for malignant transformation. Progression to cancer is actually an unintended consequence of the complex HPV life cycle. Different antiviral defence mechanisms recognize HPV early in infection, leading to the activation of the innate immune response. However, the virus has evolved several specific strategies to efficiently evade the antiviral immune signalling. Here, we review and discuss the interplay between HPV and the host cell innate immunity. We further highlight the evasion strategies developed by different HPV to escape this cellular response and focus on the correlation with HPV-induced persistence and tumorigenesis.

15.
Eur Arch Otorhinolaryngol ; 277(3): 955-956, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31897719

RESUMO

We appreciate the opportunity to comment the observations on our paper entitled "Score risk scale as a prognostic factor after sudden sensorineural hearing loss", by Capuano et al. This letter highlights several important points, including the role of hyperbaric oxygen therapy and the possible association between patent foramen ovale and sudden sensorineural hearing loss (SSHL). Further research is needed to strengthen the association between cardiovascular risk and SSHL. We thank the authors for their insights into our paper and for adding their experience and observations on the potential role of cardiovascular risk in the etiology of SSHL.


Assuntos
Perda Auditiva Neurossensorial , Perda Auditiva Súbita , Oxigenoterapia Hiperbárica , Perda Auditiva Neurossensorial/diagnóstico , Perda Auditiva Neurossensorial/etiologia , Perda Auditiva Súbita/diagnóstico , Perda Auditiva Súbita/etiologia , Perda Auditiva Súbita/terapia , Humanos , Prognóstico
16.
Curr Med Chem ; 27(14): 2257-2321, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-30277140

RESUMO

The use of anti-diabetic drugs has been increasing worldwide and the evolution of therapeutics has been enormous. Still, the currently available anti-diabetic drugs do not present the desired efficacy and are generally associated with serious adverse effects. Thus, entirely new interventions, addressing the underlying etiopathogenesis of type 2 diabetes mellitus, are required. Chalcones, secondary metabolites of terrestrial plants and precursors of the flavonoids biosynthesis, have been used for a long time in traditional medicine due to their wide-range of biological activities, from which the anti-diabetic activity stands out. This review systematizes the information found in literature about the anti-diabetic properties of chalcones, in vitro and in vivo. Chalcones are able to exert these properties by acting in different therapeutic targets: Dipeptidyl Peptidase 4 (DPP-4); Glucose Transporter Type 4 (GLUT4), Sodium Glucose Cotransporter 2 (SGLT2), α-amylase, α-glucosidase, Aldose Reductase (ALR), Protein Tyrosine Phosphatase 1B (PTP1B), Peroxisome Proliferator-activated Receptor-gamma (PPARγ) and Adenosine Monophosphate (AMP)-activated Protein Kinase (AMPK). Chalcones are, undoubtedly, promising anti-diabetic agents, and some crucial structural features have already been established. From the Structure-Activity Relationships analysis, it can generally be stated that the presence of hydroxyl, prenyl and geranyl groups in their skeleton improves their activity for the evaluated anti-diabetic targets.


Assuntos
Diabetes Mellitus Tipo 2 , Chalconas , Diabetes Mellitus Tipo 2/tratamento farmacológico , Humanos , Hipoglicemiantes , alfa-Glucosidases
17.
Food Funct ; 10(9): 5718-5731, 2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31441917

RESUMO

Dipeptidyl peptidase-4 (DPP-4) inhibitors present a unique approach for the management of type 2 diabetes (T2D). In the present study, the inhibition of DPP-4 was evaluated for a large panel of flavonoids, important components of the human diet, using in vitro and ex vivo models. The activity of the isolated enzyme was assayed in vitro. Subsequently, the most active flavonoids were tested ex vivo in human whole blood and plasma. In this study, contrary to the in vitro fluorometric tests, flavonoids did not show inhibitory activity against DPP-4. Due to the discrepancy in the results between the in vitro and ex vivo approaches, plasma protein binding values were determined, presenting values from 43.9 to 100.0%. This work provides a new insight into the inhibitory activity for DPP-4, based on the flavonoid scaffold. Additionally, the obtained results showed that the inhibitory effect of flavonoids against DPP-4 was hindered in protein rich environments, like that occurring in blood, and indicated the need for experimental refinement in drug discovery for blood targets.


Assuntos
Proteínas Sanguíneas/química , Dipeptidil Peptidase 4/química , Inibidores da Dipeptidil Peptidase IV/química , Flavonoides/química , Diabetes Mellitus Tipo 2/enzimologia , Humanos , Hipoglicemiantes , Cinética , Ligação Proteica
18.
Braz J Cardiovasc Surg ; 34(3): 305-310, 2019 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-31310469

RESUMO

OBJECTIVE: The aim of the present study was to investigate the acute response to aerobic exercise on autonomic cardiac control of patients undergoing coronary artery bypass grafting (CABG). METHODS: The study sample consisted of eight patients (age: 58.6±7.7 years; body mass index: 26.7±3.5 kg.m2) who underwent a successful CABG (no complications during surgery and/or in the following weeks). To assess heart rate variability (HRV), participants remained in a supine position with a 30-degree head elevation for 20 minutes. Electrocardiographic signal (protocol with three derivations) was collected from 600 Hz sample rate to obtain beat-to-beat intervals (R-R interval). This assessment was performed before, after one hour and after 24 hours of the exercise session. All patients underwent a 35 minutes aerobic exercise session (AES) (low-moderate intensity) on the cycle ergometer. RESULTS: Significant differences were found in the time domain, with positive changes in root mean square of successive RR interval differences (rMSSD) (ms) (parasympathetic component) (one [P=0.017] and 24 hours [P=0.007] post-session). In the frequency domain, we found a significant difference in high frequency (HF) (ms2) (parasympathetic component) (one hour [P=0.048] post-session). The low frequency (LF)/HF ratio (sympathetic and parasympathetic components with a predominance of the sympathetic component) reached statistical significance only 24 hours (P=0.018) post-session. Additionally, the largest effect size was observed only for the LF/HF ratio at one (d=-0.8) and 24 hours (d=-1.3) after one AES. CONCLUSION: The practice of (acute) aerobic exercise improved autonomic cardiac control in patients undergoing CABG.


Assuntos
Sistema Nervoso Autônomo/fisiopatologia , Reabilitação Cardíaca/métodos , Ponte de Artéria Coronária/reabilitação , Terapia por Exercício/métodos , Exercício Físico/fisiologia , Frequência Cardíaca/fisiologia , Idoso , Análise de Variância , Índice de Massa Corporal , Eletrocardiografia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Valores de Referência , Reprodutibilidade dos Testes , Estatísticas não Paramétricas , Decúbito Dorsal/fisiologia , Fatores de Tempo , Resultado do Tratamento
19.
Eur Arch Otorhinolaryngol ; 276(10): 2739-2745, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31222585

RESUMO

INTRODUCTION: Sudden sensorineural hearing loss (SSHL) is an otologic urgency whose treatment is still controversial. Its etiology remains largely unknown in most cases and predicting its prognosis is still a challenge. Cardiovascular risk factors (CVRF) have been implicated in the etiopathogenesis of this entity. OBJECTIVES: Application of the SCORE (Systematic Coronary Risk Evaluation) risk scale in patients with SSHL and evaluation of its potential prognostic value in recovery in patients with CVRF. MATERIALS AND METHODS: Prospective analysis of patients with SSHL admitted for protocol treatment including intravenous corticosteroid therapy associated to weekly intratympanic injection in the event of therapeutic failure or severe hearing loss at admission. Demographic, audiometric, clinical and imaging data were assessed. The SCORE risk scale was applied and the audiometric recovery was compared among different risk groups. RESULTS: Our overall complete and partial recovery rates were 35.9% and 26%, respectively. More than a half of our patients had at least one CVRF. Of these, overweight/obesity, hyperlipidemia and hypertension were the most common. In our sample, patients with CVRF and higher SCORE risk presented higher PTA at admission and also worse hearing outcome, although these results were not statically significant. CONCLUSION: This preliminary study could not confirm the validity for SCORE scale for cardiovascular risk assessment in predicting audiometric recovery in patients with SSHL with multiple comorbidities. Further research with larger samples are needed to elucidate the etiology of SSHL and the exact role of cardiovascular risk factors in the pathophysiology of SSHL. LEVEL OF EVIDENCE: 4.


Assuntos
Perda Auditiva Neurossensorial/epidemiologia , Perda Auditiva Súbita/epidemiologia , Prognóstico , Medição de Risco , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Audiometria de Tons Puros , Doenças Cardiovasculares/epidemiologia , Dexametasona/uso terapêutico , Diabetes Mellitus/epidemiologia , Feminino , Glucocorticoides/uso terapêutico , Perda Auditiva Neurossensorial/tratamento farmacológico , Perda Auditiva Súbita/tratamento farmacológico , Humanos , Injeção Intratimpânica , Masculino , Pessoa de Meia-Idade , Obesidade/epidemiologia , Estudos Prospectivos , Recuperação de Função Fisiológica , Fumar/epidemiologia , Acidente Vascular Cerebral/epidemiologia , Adulto Jovem
20.
Rev. bras. cir. cardiovasc ; 34(3): 305-310, Jun. 2019. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1013457

RESUMO

Abstract Objective: The aim of the present study was to investigate the acute response to aerobic exercise on autonomic cardiac control of patients undergoing coronary artery bypass grafting (CABG). Methods: The study sample consisted of eight patients (age: 58.6±7.7 years; body mass index: 26.7±3.5 kg.m2) who underwent a successful CABG (no complications during surgery and/or in the following weeks). To assess heart rate variability (HRV), participants remained in a supine position with a 30-degree head elevation for 20 minutes. Electrocardiographic signal (protocol with three derivations) was collected from 600 Hz sample rate to obtain beat-to-beat intervals (R-R interval). This assessment was performed before, after one hour and after 24 hours of the exercise session. All patients underwent a 35 minutes aerobic exercise session (AES) (low-moderate intensity) on the cycle ergometer. Results: Significant differences were found in the time domain, with positive changes in root mean square of successive RR interval differences (rMSSD) (ms) (parasympathetic component) (one [P=0.017] and 24 hours [P=0.007] post-session). In the frequency domain, we found a significant difference in high frequency (HF) (ms2) (parasympathetic component) (one hour [P=0.048] post-session). The low frequency (LF)/HF ratio (sympathetic and parasympathetic components with a predominance of the sympathetic component) reached statistical significance only 24 hours (P=0.018) post-session. Additionally, the largest effect size was observed only for the LF/HF ratio at one (d=-0.8) and 24 hours (d=-1.3) after one AES. Conclusion: The practice of (acute) aerobic exercise improved autonomic cardiac control in patients undergoing CABG.


Assuntos
Humanos , Masculino , Feminino , Pessoa de Meia-Idade , Idoso , Sistema Nervoso Autônomo/fisiopatologia , Exercício Físico/fisiologia , Ponte de Artéria Coronária/reabilitação , Terapia por Exercício/métodos , Reabilitação Cardíaca/métodos , Frequência Cardíaca/fisiologia , Valores de Referência , Fatores de Tempo , Índice de Massa Corporal , Reprodutibilidade dos Testes , Análise de Variância , Resultado do Tratamento , Decúbito Dorsal/fisiologia , Estatísticas não Paramétricas , Eletrocardiografia
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