Alpinia zerumbet is a plant popularly used to treat hypertension and anxiety. Studies with Alpinia zerumbet demonstrate antihypertensive and vasodilator effects, among others. The objective of this study was to analyze the effect of essential oil of Alpinia zerumbet (EOAz) on cardiovascular and autonomic function in rats with isoproterenol-induced myocardial infarction. Male Wistar rats (n=32) were equally allocated into four groups: Control, ISO (150mg/kg, subcutaneous), EOAz (100mg/kg by gavage), ISO+EOAz. The rats were evaluated for cardiovascular and, autonomic parameters, electrocardiogram, and infarct size. EOAz was not able to reduce the electrocardiographic variations induced by ISO. Heart rate variability showed a decrease in sympathetic modulation on the heart in the groups treated with EOAz. The cardiopulmonary reflex induced by serotonin invoked a superior blood pressure variation at the 2 µg/kg dose in the EOAz treated groups, while the heart rate variation was significantly higher at the 16 µg/kg dose, when compared to other doses, in all groups, except EOAz+ISO. The sympathetic vagal index was higher in ISO group than in control. EOAz did not reduce the infarct size. We conclude that pretreatment with EOAz does not reverse the hemodynamic and electrocardiographic damage caused by isoproterenol but does reduce sympathetic modulation.
1 October 2025 in Mini-Reviews in Medicinal Chemistry
Ruthenium complexes stand out as an excellent alternative in the field of organometallic chemistry with applications in various areas. Recently, in cardiovascular pharmacology, there has been a growing interest in investigating complexes that modulate the Nitric Oxide (NO) pathway without necessarily and directly donating NO. NO has a proven vasodilatory and cardioprotective effect, and it is known that reduced levels are associated with an increased risk of CardioVascular Diseases (CVD). Studies suggest that ruthenium complexes significantly contribute to the treatment of CVD pathophysiology through different pharmacological mechanisms, including the precise delivery of carbon monoxide (CO) to the molecular target, the release of nitric oxide species under visible and invisible (UV) light, the ability to stimulate the activation of soluble Guanylate Cyclase (sGC) enzyme, participation in the opening of potassium channels, and reduction of cytoplasmic calcium levels. This study aims to conduct a narrative review of the cardiovascular effects of ruthenium complexes, focusing on hypertension and myocardial injury, and demonstrate that metal complexes acting on the NO pathway may have promising targets for the development of therapeutic strategies in CVD treatment.
α-Lipoic acid (LA) is an antioxidant of endogenous production, also obtained exogenously. Oxidative stress is closely associated with hypertension, which causes kidney injury and endothelial dysfunction. Here, we evaluated the cardiovascular and renal effects of LA in the two-kidney-one-clip (2K1C) hypertension model. The rats were divided into four groups: Sham surgery (Sham), the two-kidneys-one-clip (2K1C) group, and groups treated with LA for 14 days (Sham-LA and 2K1C-LA). No changes were observed in the pattern of food, water intake, and urinary volume. The left/right kidney weight LKw/RKw ratio was significantly higher in 2K1C animals. LA treatment did not reverse the increase in cardiac mass. In relation to vascular reactivity, there was an increase in the potency of phenylephrine (PHE) curve in the hypertensive animals treated with LA compared to the 2K1C group and also compared to the Sham group. Vasorelaxation induced by acetylcholine (Ach) and sodium nitroprusside (SNP) were not improved by treatment with LA. Urea and creatinine levels were not altered by the LA treatment. In conclusion, the morphological changes in the aorta and heart were not reversed; however, the treatment with LA mitigated the contraction increase induced by the 2K1C hypertension.
22 September 2023 in Revista Multidisciplinar em Saúde
INTRODUÇÃO: Doenças cardiovasculares (DCVs) são as causas mais comuns de morbidade no mundo. Entender os fatores de riscos das DCVs, como obesidade e sedentarismo, são de grande importância para conhecer melhor os fatores iniciadores destas doenças. No Brasil, a hipertensão arterial sistêmica (HAS) apresenta-se como um dos principais fatores de riscos para DCVs. Óxido nítrico (NO) é uma molécula gasosa de grande valor para estudos sobre distúrbios cardiovasculares, pois podem regular o fluxo sanguíneo e mantem o tônus vascular. Os metalocomplexos de rutênio são substâncias promissoras para clínica médica, pois são bons doadores de NO, no qual, estes são utilizados para o tratamento de distúrbios cardiovasculares. OBJETIVO: Avaliar a toxicidade aguda do complexo de rutênio cis-[Ru(bpy)2(2-MIM)Cl]+ (FOR011A) em modelo animal, por meio da determinação da DL50 pela adaptação do protocolo Teste “Up and Down. MÉTODOS: Foi utilizado o protocolo Teste “Up and Down” proposto pela Organização para a Cooperação e Desenvolvimento Econômico (OECD) adaptado. Utilizou-se camundongos swiss fêmeas entre 17 e 22 gramas, sob autorização do Comitê de Ética em Pesquisa Animal do NPDM, com a numeração 13010819-0. Além disso, para o desenvolvimento das doses administradas, foi utilizado o software Acute Oral Toxicity 425, obtendo-se as doses de 10, 28, 70 e 175mg/kg. RESULTADOS e DISCUSSÃO: O FOR011A apresentou a dose 70mg/kg como dose limite. DL50 foi estimada em 45,72 mg/kg. Apresentou letargia independente da dose, vasodilatação e tremores na dose de 28mg/kg e morte dos animais estudados na dose de 70mg/kg em até 15 minutos após administração, bem como também apresentou alterações histopatológicas renais e hepáticas. CONCLUSÃO: Com a realização do protocolo Teste “Up and Down” e, posteriormente, a realização de análises histopatológicas foi constatada uma relativa toxicidade do metalocomplexo utilizado. Desta forma, é necessário a continuação de estudos pré-clínicos para um melhor entendimento de seus efeitos fisiológicos.
Background: The World Health Organization (WHO) declared a pandemic due to Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), the etiologic agent responsible for Coronavirus Disease 2019 (COVID-19). Although case numbers declined after the initial outbreak, Brazil experienced slight increases in COVID-19 cases in 2024 and 2025, underscoring the persistent need for effective therapeutic interventions. Recently, proxalutamide—an androgen receptor antagonist—has been proposed as a potential therapeutic agent against COVID-19, as supported by several clinical studies. Methods: In the present work, we aimed to elucidate the molecular interactions between proxalutamide and key proteins involved in the viral fusion and replication processes of SARS-CoV-2. Computational techniques, including molecular docking and molecular dynamics simulations, were employed. Results: Our analyses indicated a high success rate, with stable conformations and favorable binding affinity values for ACE2 (−8.90 kcal/mol) and TMPRSS2 (−9.28 kcal/mol), resulting in strong docking scores. Moreover, molecular dynamics simulations confirmed the stability of these complexes, as evidenced by consistent mean square deviation values, low structural flexibility, a stable radius of gyration, and maintained surface rigidity over a 100 ns simulation period. Conclusions: These combined docking and dynamics results suggest that proxalutamide interacts firmly with the active sites, indicating high binding affinity that may interfere with SARS-CoV-2 entry. Nevertheless, experimental validation and rigorous safety assessments are warranted to confirm this potential.