Review
Biochemistry & Molecular Biology
V. Conti, G. Corbi, V. Manzo, C. Sellitto, F. Iannello, S. Esposito, E. De Bellis, T. Iannaccone, A. Filippelli
Summary: Pharmacogenetics plays a crucial role in predicting the response to pharmacological treatments based on individual genetic background, especially in anticoagulant and antiplatelet therapy. Despite accumulating evidence of its effectiveness, there are still barriers to the implementation of pharmacogenetics in clinical practice.
CURRENT MEDICINAL CHEMISTRY
(2021)
Review
Hematology
Mark Goldin, Ioannis Koulas, Jeffrey Weitz, Alex C. Spyropoulos
Summary: Venous thromboembolism (VTE) and arterial thromboembolism (ATE) are connected by the common mechanism of thrombin generation, suggesting a possible dual-pathway inhibition strategy. Existing data supports the effectiveness of this strategy in reducing major and fatal thrombotic outcomes, with acceptable bleeding risk. More research is needed to identify the patient populations that can benefit the most from this approach.
THROMBOSIS AND HAEMOSTASIS
(2022)
Article
Hematology
Nicole R. Bonetti, Annukka S. Jouppila, Seyed Soheil Saeedi Saravi, Brian C. Cooley, Lisa Pasterk, Luca L. Liberale, Sara Gobbato, Thomas F. Luscher, Giovanni G. Camici, Riitta P. Lassila, Jurg H. Beer
Summary: This study investigated the effects of a semi-synthetic dual antiplatelet and anticoagulant (APAC) on arterial thrombosis. The results showed that APAC can target vascular injury sites after administration, exerting local dual antiplatelet and anticoagulant actions, and reducing thrombosis caused by carotid injuries in mice. This study suggests that APAC may be a novel antithrombotic that can help reduce the risk of cardiovascular complications.
THROMBOSIS RESEARCH
(2023)
Review
Pharmacology & Pharmacy
Mario Enrico Canonico, Giuseppe Damiano Sanna, Roberta Siciliano, Fernando Scudiero, Giovanni Esposito, Guido Parodi
Summary: HCV infection increases cardiovascular and bleeding risks, requiring concomitant use of antithrombotic therapies. However, there may be drug-drug interactions between antithrombotic drugs and HCV antiviral drugs.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Dentistry, Oral Surgery & Medicine
Anita Aminoshariae, Mark Donaldson, Michael Horan, James C. Kulild, Dale Baur
Summary: For patients undergoing endodontic microsurgery while taking anticoagulant or antiplatelet agents, assessment of bleeding risk is crucial, especially for surgeries exceeding 45 minutes. Individualized risk assessment and consultation with the patient's physician are recommended to balance the effects of medications and potential risks effectively.
JOURNAL OF ENDODONTICS
(2021)
Article
Medicine, General & Internal
Wen-Yi Huang, Bruce Ovbiagele, Meng Lee
Summary: A meta-analysis showed that compared with antiplatelet therapies, oral anticoagulants (OACs) were associated with a lower risk of recurrent ischemic stroke in patients with cryptogenic stroke and potential cardiac emboli. OACs might be a viable non-procedural alternative in these patients.
EUROPEAN JOURNAL OF INTERNAL MEDICINE
(2022)
Article
Hematology
Francesco Paciullo, Emanuele Valeriani, Angelo Porfidia, Marcello Di Nisio, Marco P. Donadini, Rossella Marcucci, Domenico Prisco, Carlo Cagini, Paolo Gresele, Walter Ageno
Summary: Retinal vein occlusion is a common cause of visual impairment and blindness, which may have both local and systemic risk factors. The association with thrombophilia is still controversial and there is limited and inconsistent data on antithrombotic therapy for RVO. The Italian Society on Thrombosis and Haemostasis provides a position statement to guide the management of patients with RVO based on available evidence and expert opinion.
Article
Ophthalmology
Chi-Juei Jeng, Yi-Ting Hsieh, Cheng-Li Lin, I-Jong Wang
Summary: Antiplatelet/anticoagulant therapy has a protective effect against the development of non-proliferative diabetic retinopathy in patients with type 2 diabetes mellitus. Single use of aspirin or dipyridamole is beneficial for the prevention of non-proliferative diabetic retinopathy.
Article
Cardiac & Cardiovascular Systems
Masashi Amano, Makoto Miyake, Takeshi Kitai, Yuki Obayashi, Misa Takegami, Kunihiro Nishimura, Yutaka Furukawa, Chisato Izumi
Summary: Additional single-antiplatelet therapy (SAPT) on top of anticoagulant therapy may reduce the risk of stroke/systemic embolism in patients with atrial fibrillation (AF) after bioprosthetic valve replacement, while the incidence of bleeding remains similar. These findings suggest the potential safety and effectiveness of adding SAPT to anticoagulant therapy in real-world clinical settings.
CIRCULATION JOURNAL
(2022)
Article
Cardiac & Cardiovascular Systems
Mattia Galli, Davide Capodanno, Stefano Benenati, Domenico D'Amario, Filippo Crea, Felicita Andreotti, Dominick J. Angiolillo
Summary: This systematic review and meta-analysis found that low-dose direct oral anticoagulants (DOACs) in adjunct to antiplatelet therapy can reduce ischaemic events in patients with cardiovascular disease (CVD). However, it comes at the cost of increased major and all bleeding. The use of very low-dose DOAC (specifically rivaroxaban 2.5 mg twice daily) appeared to have advantages in reducing bleeding risk without compromising efficacy.
EUROPEAN HEART JOURNAL-CARDIOVASCULAR PHARMACOTHERAPY
(2022)
Article
Dentistry, Oral Surgery & Medicine
Bogumil Lewandowski, Aleksander Myszka, Malgorzata Migut, Ewelina Czenczek-Lewandowska, Robert Brodowski
Summary: This study retrospectively examined 153 patients using antiplatelet therapy and found that the application of TachoSil patches effectively stopped bleeding and prevented secondary bleeding after tooth extraction, providing a helpful treatment option for patients.
Article
Cardiac & Cardiovascular Systems
Joris J. Komen, Tomas Forslund, Aukje K. Mantel-Teeuwisse, Olaf H. Klungel, Mia von Euler, Frieder Braunschweig, Hakan Wallen, Paul Hjemdahl
Summary: This study analyzed 90-day mortality in atrial fibrillation (AF) patients after a stroke or a severe bleed, and found that NOAC treatment was associated with lower mortality rates, while warfarin may lead to higher mortality rates after intracranial hemorrhage.
EUROPEAN HEART JOURNAL-CARDIOVASCULAR PHARMACOTHERAPY
(2021)
Review
Medicine, General & Internal
Jing Jin, Xiaojun Zhuo, Mou Xiao, Zhiming Jiang, Linlin Chen, Yashvina Devi Shamloll
Summary: This research analysis indicates that adding apixaban to the DAPT regimen significantly increases the risk of bleeding events in patients with ACS, without showing a significant difference in fatal bleeding. Further larger studies are needed to confirm these findings due to the limited data available.
Article
Endocrinology & Metabolism
Nousjka P. A. Vranken, Saman Rasoul, Jasper J. P. Luijkx, Tobias F. S. Pustjens, Sonja Postma, Evelien J. Kolkman, Elvin Kedhi, Sodiqur Rifqi, Michael K. Y. Lee, Henning Ebelt, Bela Merkely, Monica Verdoia, Wojtek Wojakowski, Arnoud A. W. J. van 't Hof, Harry Suryapranata, Giuseppe De Luca
Summary: This study found that in diabetic patients undergoing PCI for ACS, there were similar clinical outcomes between 3 months and 12 months DAPT, suggesting that short-term DAPT may be a safe option. Additional larger studies are needed for more precise evaluation of short-term DAPT in high-risk patients.
DIABETES-METABOLISM RESEARCH AND REVIEWS
(2022)
Article
Cardiac & Cardiovascular Systems
Dong Geum Shin, Sunhwa Kim, Yoo Ri Kim
Summary: In patients with non-valvular atrial fibrillation, combination therapy of non-vitamin K antagonist oral anticoagulants (NOACs) and antiplatelet agents (APT) is associated with a higher incidence of bleeding events compared to monotherapy with NOACs. However, there is no difference in stroke/systemic embolic events and major adverse cardiac events. The bleeding risk in AF patients taking the combination of NOACs and APT should be carefully evaluated.
REVIEWS IN CARDIOVASCULAR MEDICINE
(2022)
Review
Pharmacology & Pharmacy
Rita Roque-Bravo, Rafaela Sofia Silva, Rui F. Malheiro, Helena Carmo, Felix Carvalho, Diana Dias da Silva, Joao Pedro Silva
Summary: Synthetic cannabinoids, a chemically diverse group of new psychoactive substances that target the endocannabinoid system, have more intense effects than cannabis and are increasingly being used recreationally. However, the rise in intoxications and deaths associated with synthetic cannabinoids poses a major public health concern and challenge for policy makers.
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY
(2023)
Article
Toxicology
Ana Reis-Mendes, Felix Carvalho, Fernando Remiao, Emilia Sousa, Maria de Lourdes Bastos, Vera Marisa Costa
Summary: This study compares the cardiotoxicity of MTX and its metabolite NAPHT in an in vitro cardiac model and explores the role of metabolism in the cardiotoxic effects. The results show that MTX causes concentration-dependent cytotoxicity, affecting mitochondrial function and lysosome uptake, while NAPHT only exhibits concentration-dependent cytotoxicity. Inhibition or induction of metabolism has minimal impact on MTX-induced cytotoxicity, suggesting that metabolism is not a major contributor to MTX toxicity. However, autophagy is involved in MTX-induced cytotoxicity, potentially through the involvement of p62/LC3-II.
ARCHIVES OF TOXICOLOGY
(2023)
Article
Chemistry, Medicinal
Mariana C. Almeida, Paulo M. da Costa, Emilia Sousa, Diana I. S. P. Resende
Summary: With the increasing drug resistance, it is crucial to develop effective antimicrobial therapies. One promising approach is the conjugation of antibiotics with relevant molecules to enhance their activity through target-directed delivery. By hijacking microorganisms' iron transport systems, siderophore-antibiotic Trojan horses can carry antibiotics into cells. This Perspective examines the potential of these Trojan horses for infection treatment and the role of siderophores in diagnostic techniques. It also discusses other conjugated compounds, such as those involving vitamin B12, carbohydrates, amino acids, protein degradation, and beta-lactamase activated prodrugs.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Rotchana Klaram, Tida Dethoup, Fatima P. Machado, Luis Gales, Decha Kumla, Salar Hafez Ghoran, Emilia Sousa, Sharad Mistry, Artur M. S. Silva, Anake Kijjoa
Summary: Five undescribed pentaketide derivatives and a p-hydroxyphenyl-2-pyridone derivative were isolated from the ethyl acetate extract of a marine sponge-derived fungus, and their structures were determined using NMR and mass spectral analyses. The growth inhibitory activity of these compounds against various plant pathogenic fungi was also evaluated.
Article
Biochemistry & Molecular Biology
Ana Jesus, Ana I. Sebastiao, Goncalo Brites, Marta Correia-da-Silva, Honorina Cidade, Maria T. Cruz, Emilia Sousa, Isabel F. Almeida
Summary: A synthetic hydrophilic sulfated glycosylated derivative called RSV-GS, inspired by marine natural products, has been found to have lower cytotoxicity and comparable bioactivity to Resveratrol (RSV). In vitro experiments showed that RSV-GS does not have skin sensitization potential, and it can mitigate skin sensitization and allergic contact dermatitis induced by allergens. These findings highlight the potential use of RSV-GS as a safe and anti-allergic active ingredient in cosmetics.
Article
Infectious Diseases
Mariana C. Almeida, Nikoletta Szemeredi, Fernando Duraes, Solida Long, Diana I. S. P. Resende, Paulo Martins da Costa, Madalena Pinto, Gabriella Spengler, Emilia Sousa
Summary: Drug resistance is becoming a major global health threat, with overexpression of efflux pumps and formation of biofilms being common mechanisms. Therefore, it is crucial to develop antimicrobial agents that can counteract resistance. Pyrazino[2,1-b]quinazoline-3,6-diones have recently been discovered to have relevant antimicrobial properties.
Article
Chemistry, Multidisciplinary
Catia A. Bonito, Ricardo J. Ferreira, Maria-Jose. U. Ferreira, Fernando Duraes, Emilia Sousa, Jean-Pierre Gillet, M. Natalia D. S. Cordeiro, Daniel J. V. A. dos Santos
Summary: A medicinal chemistry study combined in silico and in vitro methodologies to identify and characterize putative allosteric drug-binding sites (aDBSs) at the interface of the transmembrane-and nucleotide-binding domains (TMD-NBD) of P-glycoprotein. Two aDBSs were identified using in silico fragment-based molecular dynamics and were characterized in terms of size, polarity, and lining residues. Several compounds from a small library of thioxanthone and flavanone derivatives were found to decrease verapamil-stimulated ATPase activity, indicating allosteric efflux modulation in P-glycoprotein. Molecular docking and dynamics simulations provided insights into the binding mode of flavanone derivatives as allosteric inhibitors.
Review
Chemistry, Medicinal
Salar Hafez Ghoran, Fatemeh Taktaz, Emilia Sousa, Carla Fernandes, Anake Kijjoa
Summary: Marine-derived fungi are unique sources of bioactive secondary metabolites, particularly peptides, with diverse structures and biological activities. This review summarizes the literature on marine fungal peptides from January 1991 to June 2023, covering their chemical characteristics, sources, and biological and pharmacological activities. Among 30 genera, Aspergillus was found to produce the highest number of peptides, followed by Penicillium, Acremonium, Eurotium, Trichoderma, Simplicillium, and Beauveria. The predominant activity of the reported marine peptides was cytotoxicity against human cancer cell lines, followed by antibacterial, antifungal, antiviral, anti-inflammatory, and enzyme inhibition activities.
Article
Biochemistry & Molecular Biology
Francisca Carvalhal, Ana Cristina Magalhaes, Rita Rebelo, Andreia Palmeira, Diana I. S. P. Resende, Fernando Duraes, Miguel Maia, Cristina P. R. Xavier, Luisa Pereira, Emilia Sousa, Marta Correia-da-Silva, M. Helena Vasconcelos
Summary: This study focuses on the interaction between the spike protein of SARS-CoV-2 and the ACE2 receptor. Through virtual screening and in vitro assays, five synthetic compounds were identified as potential inhibitors of SARS-CoV-2 infection, with xanthene 1 being the most promising. It exhibited antiviral activity without cytotoxicity to human lung cells.
Article
Environmental Sciences
Catia Vilas-Boas, Elisabete R. Silva, Diana Resende, Beatriz Pereira, Goncalo Sousa, Madalena Pinto, Joana R. Almeida, Marta Correia-da-Silva, Emilia Sousa
Summary: Marine biofouling pollution has negative impacts on ecosystems and the global economy. However, traditional antifouling marine coatings release toxic biocides that accumulate in sediments and aquatic organisms. This study evaluated the environmental fate and efficacy of xanthones 1 and 2, which can inhibit mussel settlement without acting as biocides. The results showed that xanthone 2 had a shorter half-life and suitable leaching behavior compared to xanthone 1. Additionally, the xanthone-based coatings successfully reduced the attachment of Mytilus galloprovincialis larvae.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2023)
Article
Pharmacology & Pharmacy
Vera Marisa Costa, Joao Paulo Capela, Maria Lourdes Bastos, Fernando Remiao, Kurt James Varner, Jose Alberto Duarte, Felix Carvalho
Summary: Prolonged overexposure to catecholamines causes toxicity due to continuous adrenoceptor stimulation, autoxidation, and reactive pro-oxidant species formation. This study investigated the contribution of oxidative stress in adrenaline-induced neurotoxicity using non-differentiated SH-SY5Y cells. Results showed that Adrenaline caused concentration- and time-dependent cytotoxicity in the cells, and N-acetyl-cysteine prevented the toxicity while the antioxidant Tiron was non-protective. Further analysis is needed to understand the involvement of these processes in catecholamine-induced peripheral neuropathy.
BRAZILIAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Article
Chemistry, Medicinal
Sofia Reis Brandao, Ana Reis-Mendes, Maria Joao Neuparth, Felix Carvalho, Rita Ferreira, Vera Marisa Costa
Summary: The cardiotoxicity of doxorubicin (DOX) may manifest at the beginning/during treatment or years after, compromising patients' quality of life. This study reveals that the molecular mechanisms elicited by DOX are modulated at different extents over time, supporting the differences in clinical cardiotoxic manifestations with time.
Review
Toxicology
Ana Dias-Carvalho, Susana Isabel Sa, Felix Carvalho, Eduarda Fernandes, Vera Marisa Costa
Summary: As life expectancy increases, the burden of neurologic disorders in the elderly has become a major challenge. Inflammation plays a crucial role in the development of aging and neurologic disorders, such as Alzheimer's, Parkinson's, and multiple sclerosis. Understanding the role of inflammation is essential for developing effective treatments and interventions to alleviate the social and economic burden of these diseases.
ARCHIVES OF TOXICOLOGY
(2023)
