RESUMO
The marine kingdom is an important source of a huge variety of scaffolds inspiring the design of new drugs. The complex molecules found in the oceans present a great challenge to organic and medicinal chemists. However, the wide variety of biological activities they can display is worth the effort. In this article, we present an overview of different seaweeds as potential sources of bioactive pigments with activity against neurodegenerative diseases, especially due to their neuroprotective effects. Along with a broad introduction to seaweed as a source of bioactive pigments, this review is especially focused on astaxanthin and fucoxanthin as potential neuroprotective and/or anti-neurodegenerative agents. PubMed and SciFinder were used as the main sources to search and select the most relevant scientific articles within the field.
Assuntos
Doenças Neurodegenerativas , Fármacos Neuroprotetores , Alga Marinha , Xantofilas , Xantofilas/farmacologia , Xantofilas/química , Xantofilas/isolamento & purificação , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/química , Alga Marinha/química , Humanos , Doenças Neurodegenerativas/tratamento farmacológico , Animais , Pigmentos Biológicos/farmacologia , Pigmentos Biológicos/química , Pigmentos Biológicos/isolamento & purificaçãoRESUMO
As we celebrate International Women's Day 2024 with the theme "Inspire Inclusion", the women of the ACS Medicinal Chemistry Division (MEDI) want to foster a sense of belonging, relevance, and empowerment by sharing uplifting stories of what inspired them to become medicinal chemists. In this editorial, we are featuring female medicinal chemistry scientists to provide role models, encouragement, and inspiration to others. We asked women medicinal chemists to contribute a brief paragraph about what inspired them to become medicinal chemists or what inspires them today as medicinal chemists. The responses and contributions highlight their passions and motivations, such as their love of the sciences and their drive to improve human health by contributing to basic research and creating lifesaving drugs.
RESUMO
As we celebrate International Women's Day 2024 with the theme "Inspire Inclusion", the women of the ACS Medicinal Chemistry Division (MEDI) want to foster a sense of belonging, relevance, and empowerment by sharing uplifting stories of what inspired them to become medicinal chemists. In this editorial, we are featuring female medicinal chemistry scientists to provide role models, encouragement, and inspiration to others. We asked women medicinal chemists to contribute a brief paragraph about what inspired them to become medicinal chemists or what inspires them today as medicinal chemists. The responses and contributions highlight their passions and motivations, such as their love of the sciences and their drive to improve human health by contributing to basic research and creating lifesaving drugs.
Assuntos
Química Farmacêutica , Poder Psicológico , Humanos , FemininoRESUMO
Hydroxycoumarins are an important source of biologically active compounds. Previous studies have shown that the number and position of the hydroxyl substituents in the scaffold play an important role for the observed biological activity. In the present study, 3-(3-hydroxyphenyl)-7-hydroxycoumarin was synthesized, and potential cytogenotoxic effects determined in human HepG2/C3A cells displaying phase 1 and phase 2 enzymes (metabolizing cell ability) and compared to human peripheral blood mononuclear cells (PBMC) without xenobiotics metabolizing capacity. Cell viability was determined with concentrations between 0.01 and 10 µg/ml of 3-(3-hydroxyphenyl)-7-hydroxycoumarin using MTT (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) and trypan blue tests. Genotoxicity was determined utilizing the comet assay, and the clastogenic/aneugenic potential employing the micronucleus (MN) test. The results of the in vitro cytotoxicity assays showed a significant decrease in cell viability of PBMC following exposure to 10 µg/ml concentration of the studied compound after 48 and 72 hr. Comet assay observations noted significant DNA damage in PBMC after 4 hr treatment. No marked cytogenotoxic effects were found in HepG2/C3A cells. No chromosomal mutations were observed in both cell lines. It is important to note that 3-(3-hydroxyphenyl)-7-hydroxycoumarin may exert beneficial pharmacological actions at the low micromolar range and with half-life less than 24 hr. Therefore, the results obtained encourage the continuation of studies on this new molecule for medicinal purposes, but its potential toxicity at higher concentrations and longer exposure times needs to be investigated in further studies.
Assuntos
Dano ao DNA , Leucócitos Mononucleares , Humanos , Ensaio Cometa/métodos , Testes para Micronúcleos/métodos , Morte Celular , Umbeliferonas/farmacologiaRESUMO
Plasmodium berghei ANKA (PbA) infection in mice resembles several aspects of severe malaria in humans, such as cerebral malaria and acute respiratory distress syndrome. Herein, the effects of N-(coumarin-3-yl)cinnamamide (M220) against severe experimental malaria have been investigated. Treatment with M220 proved to protect cognitive abilities and lung function in PbA-infected mice, observed by an object recognition test and spirometry, respectively. In addition, treated mice demonstrated decreased levels of brain and lung inflammation. The production and accumulation of microglia, and immune cells that produce the inflammatory cytokines TNF and IFN-γ, decreased, while the production of the anti-inflammatory cytokine IL-10 by innate and adaptive immune cells was enhanced. Treatment with M220 promotes immunomodulatory, neuroprotective, and lung function-preserving effects during experimental severe malaria. Therefore, it may be an interesting therapeutic candidate to treat severe malaria effects.
RESUMO
A abrangência da Enfermagem de Reabilitação não se limita apenas às instituições hospitalares e/ou de outra tipologia e vai até ao local onde o cidadão vive, trabalha e se relaciona, o que exige um profissional capaz de mobilizar conhecimentos e competências, com vista a um cuidado holístico, como é o caso da comunidade. As lesões músculo-esqueléticas são um problema de saúde multifatorial que se constituem como uma prioridade de atuação da Enfermagem de Reabilitação, a diferentes níveis, sendo que a promoção da saúde será fundamental para trazer ganhos em saúde a toda a população. Nesta ótica foi realizado um Estágio de Natureza Profissional com os objetivos gerais de desenvolver competências especializadas na prática de cuidados de Enfermagem de Reabilitação e de contribuir para a mudança de cuidados na prevenção das lesões músculo-esqueléticas na comunidade, nomeadamente, pela capacitação dos cuidadores informais de doentes dependentes no domicílio e da comunidade escolar. Para melhor dar resposta aos objetivos descritos previamente utilizou-se por base a Metodologia de Projeto e desenvolveram-se três atividades major: "Prática de Cuidados de Enfermagem de Reabilitação na Comunidade"; "Prevenção de Lesões Músculoesqueléticas nos Cuidadores Informais de Doentes Dependentes no Domicílio" e "Na Escola Eu Aprendo Às Lesões Músculo-esqueléticas Não me Rendo!". As intervenções desenvolvidas permitiram ir de encontro à capacitação dos cuidadores informais de doentes dependentes no domicílio, pois a amostra abrangida evidenciou melhoria em relação a quinze das vinte medidas preventivas de lesões músculoesqueléticas ensinadas/instruídas e treinadas e no caso da comunidade escolar os comportamentos transmitidos como ideais/corretos nas sessões sobre "Educação Postural" foram os mais expressados pelos alunos. Contudo, verificou-se uma baixa taxa de adesão e valorização dos exercícios preventivos das lesões músculo-esqueléticas, tanto nos cuidadores informais, como nos estudantes. Considera-se, assim, que os objetivos planeados foram cumpridos na sua generalidade, dando realce à alteração do paradigma primordial da Enfermagem de Reabilitação, que é a prevenção terciária, em benefício da prevenção primária e secundária. Realça-se a importância de continuar a investir nesta área específica, incluindo novos estudos, validando instrumentos de medida adequados e até levando intervenções deste cariz a outras populações, no âmbito do campo de atuação da Enfermagem de Reabilitação.
The scope of rehabilitation nursing does not end in the hospitals and/or similar institutions but it continues up to the place where the citizen lives, works and socializes, which requires a professional who is capable of mobilizing knowledge and skills, in order to provide a holistic care, as it is the case of the community. The musculoskeletal injuries, which are a multifactorial health problem, constitute a priority in the Rehabilitation Nursing practice at different levels, being the health promotion something pivotal in bringing health gains to the entire population. Bearing this in mind, a Professional Internship took place, with the general objectives of developing specialised skills in the practice of Rehabilitation Nursing care, and of contributing for a change of care services in the prevention of musculoskeletal injuries in the community, namely, by the training of informal caregivers of dependent patients at home and in the school community. In order to give a better response to the aims that were previously mentioned, the Project Methodology was used as a basis, and three major activities were developed: "Practice of Rehabilitation Nursing Care in the Community"; "Prevention of Musculoskeletal Injuries in Informal Caregivers of Dependent Patients at Home" and "At school I learn... To the MuskuloskeletaI Injuries I Don't Surrender!" The interventions carried out, allowed us to meet the training of the informal caregivers of dependent patients at home, since the sample covered showed improvement in relation to fifteen of the twenty preventive measures of musculoskeletal injuries taught/instructed and trained and in the case of the school community the behaviors transmitted as ideal/correct in the sessions of "Postural Education" were the most expressed by the students. However, there was a low rate of adherence and valorization of the preventive exercises of musculoskeletal injuries, both in informal caregivers and in students. It is considered, therefore, that the planned objectives were fulfilled in their generality, emphasizing the alteration of the primordial paradigm of Rehabilitation Nursing, which is the tertiary prevention, for the benefit of primary and secondary prevention. It should be emphasised the importance of continuing to invest in this specific area, by including new studies, validating adequate measuring instruments or even bringing similar interventions to other populations, as far as the action in the field of Rehabilitation Nursing is concerned.
Assuntos
Serviços de Saúde Escolar , Doenças Musculoesqueléticas , Enfermagem em Reabilitação , Prevenção de DoençasRESUMO
Amiodarone (AM)-induced thyrotoxicosis (AIT) is a condition with uncertainties from the diagnostic and therapeutic standpoints. A 54-year old male was referred to the hospital due to thyrotoxicosis. He had history of atrial fibrillation medicated with AM. No history of pre-existing thyroid disease was present, thyroid palpation revealed no goiter, and there were no signs of Graves' ophthalmopathy. Thyroid autoantibodies and thyroid-stimulating hormone receptor antibodies (TRABs) were negative. Thyroid and Doppler ultrasounds were normal. 99mTc-sestaMIBI thyroid scan (STS) showed uptake with rapid washout. AM therapy was discontinued, and combined therapy was started. After a long course of glucocorticoid and thionamides, the patient became euthyroid. It is necessary to distinguish between the types of AIT to decide whether or not continue AM treatment; after that, the appropriate therapy should be selected. STS was very important in the diagnosis of the type of AIT.
A tireotoxicose induzida por amiodarona (AIT) é uma condição incerta do ponto de vista de diagnóstico e tratamento. Um homem de 54 anos de idade foi encaminhado ao hospital devido à tireotoxicose. Ele apresentou um histórico de fibrilação atrial medicada com amiodarona (AM). Não havia histórico de doença da tiroide preexistente, a palpação da tiroide não revelou bócio e não havia sinais de oftalmopatia de Graves. Os autoanticorpos contra a tireoide e anticorpos para os receptores de hormônio estimulante da tireoide (TRABs) foram negativos. Os resultados do ultrassom da tiroide e do exame de Doppler foram normais. A cintigrafia da tiroide com 99mTc-sestaMIBI mostrou captação com rápida eliminação. O tratamento com AM foi descontinuado, e se iniciou a terapia combinada. Após um longo tratamento com glicocorticoides e tionaminas, o paciente se tornou eutiroide. É necessário distinguir entre os tipos de AIT para se determinar a continuação ou interrupção do tratamento com AM. Depois disso, o tratamento apropriado deve ser selecionado. A STS é muito importante no diagnóstico do tipo de AIT.