Review
Infectious Diseases
Mariam Rima, Mohamad Rima, Ziad Fajloun, Jean-Marc Sabatier, Burkhard Bechinger, Thierry Naas
Summary: Antimicrobial peptides are a promising alternative to antibiotics for treating bacterial infections, especially those caused by multidrug-resistant pathogens. They show various activity spectra and mechanisms of actions, and can be used synergistically against ESKAPE bacteria, particularly in biofilm treatments. Challenges and limitations in their therapeutic applications are highlighted, with potential solutions being evaluated to determine if antimicrobial peptides could potentially replace antibiotics in the future.
Article
Microbiology
Wenyu Xiang, Patrice Clemenza, Jessie Klousnitzer, Jespar Chen, Weiheng Qin, Stephanie Tristram-Nagle, Yohei Doi, Y. Peter Di, Berthony Deslouches
Summary: Antimicrobial peptides that directly disrupt bacterial membranes may overcome resistance to traditional antibiotics. A rational framework for systematically addressing this challenge was developed using novel peptides tested against antibiotic-resistant bacteria. The study selected peptides with broad-spectrum activity and low toxicity to mammalian cells, and the shortest peptide demonstrated effectiveness in killing antibiotic-resistant bacteria and protecting mice from infection.
FRONTIERS IN MICROBIOLOGY
(2022)
Review
Microbiology
Tanzeel Zohra, Muhammad Numan, Aamer Ikram, Muhammad Salman, Tariq Khan, Misbahud Din, Ayesha Farooq, Afreenish Amir, Muhammad Ali
Summary: Antimicrobial resistance is a growing silent pandemic, with multidrug-resistant strains threatening public health improvement and posing challenges in clinical practice. Understanding resistance mechanisms and developing new antimicrobial agents and alternative tools are crucial in combating this issue.
Review
Pharmacology & Pharmacy
Vasundhra Bhandari, Akash Suresh
Summary: This article discusses the emergence of resistance in bacterial species over time and the various protective mechanisms employed by bacterial cells. Additionally, it highlights the importance of new approaches and practices for tackling antimicrobial resistance and identifying new treatment options.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Infectious Diseases
Giancarlo Perez-Lazo, Susan Abarca-Salazar, Renata Lovon, Rocio Rojas, Jose Ballena-Lopez, Adriana Morales-Moreno, Wilfredo Flores-Paredes, Berenice Arenas-Ramirez, Luis Ricardo Illescas
Summary: A descriptive study conducted in a Peruvian hospital found a significant correlation between the use of ceftazidime and carbapenem-resistant Pseudomonas aeruginosa isolates, as well as a correlation between resistance to piperacillin/tazobactam and ciprofloxacin usage in Enterobacter spp. in the medical wards. Notably, there was a significant reduction in Pseudomonas aeruginosa resistance to piperacillin/tazobactam and amikacin in the ICU from 2015 to 2018. These findings highlight the importance of continuous support and assessment of antimicrobial stewardship strategies in hospitals.
Review
Biochemistry & Molecular Biology
Bruno S. Lopes, Alfizah Hanafiah, Ramesh Nachimuthu, Saravanan Muthupandian, Zarith Nameyrra Md Nesran, Sandip Patil
Summary: Antibiotic resistance caused by ESKAPE pathogens resulted in more than one million deaths globally in 2019. The use of antimicrobial peptides (AMPs) is crucial in combating this crisis, but their stability and potential toxic side effects need to be addressed. Developing new AMP analogues and using a one health approach, along with phage therapies and breakthroughs in antimicrobial peptide synthesis, can help tackle the problem of antimicrobial resistance (AMR).
Article
Multidisciplinary Sciences
Rong Sheng Li, Jiahui Liu, Cong Wen, Yaru Shi, Jian Ling, Qiue Cao, Lei Wang, Hu Shi, Cheng Zhi Huang, Na Li
Summary: This article introduces a transformable nano-antibiotics (TNA) that can target the bactericidal properties of Gram-negative bacteria by binding to BamA and LPSs. The TNA can kill Gram-negative bacteria through multiple modes of action and induce immune responses to protect against reinfections.
Article
Infectious Diseases
Manuela Arbune, Gabriela Gurau, Elena Niculet, Alina Viorica Iancu, Gabriela Lupasteanu, Silvia Fotea, Mihaela Camelia Vasile, Alin Laurentiu Tatu
Summary: This study aimed at identifying the main antimicrobial resistance of ESKAPE pathogens in a Romanian infectious diseases hospital. The results showed high rates of multidrug resistance among these pathogens, with ESBL, MRSA, and CR being the main resistance mechanisms.
INFECTION AND DRUG RESISTANCE
(2021)
Article
Infectious Diseases
Emanuela Roscetto, Rosa Bellavita, Rossella Paolillo, Francesco Merlino, Nicola Molfetta, Paolo Grieco, Elisabetta Buommino, Maria Rosaria Catania
Summary: This study confirmed the antimicrobial activity of two analogues of Temporin L against carbapenemase-producing K. pneumoniae, with peptide C showing stronger antimicrobial properties and bactericidal activity. The results highlight the great potential of antimicrobial peptides as a new treatment option for difficult-to-treat infections and as a new strategy for drug-resistance control.
Article
Immunology
Chinyere Aloke, Ikechukwu Achilonu
Summary: ESKAPE pathogens are the major cause of nosocomial infections worldwide. This review explores emerging alternative therapeutic strategies for treating these pathogens, including combination antibiotics, antimicrobial peptides (AMPs), bacteriophage, and photodynamic therapies. The findings highlight the resistance mechanisms of ESKAPE pathogens and the limitations and future prospects of these therapeutic approaches.
MICROBIAL PATHOGENESIS
(2023)
Article
Food Science & Technology
Jose J. L. Silva, Maria R. A. de Miranda, Pedro F. N. Souza
Summary: Fungal contamination is a major cause of food spoilage, posing serious risks to human health and economic losses. This review discusses the recent advances in using synthetic peptides as agents to address foodborne fungal resistance and their applications in food preservation.
CURRENT OPINION IN FOOD SCIENCE
(2023)
Review
Chemistry, Medicinal
Nishigandha S. Mone, Sahil Syed, Palanisamy Ravichandiran, Surekha K. Satpute, A. Rhan Kim, Dong Jin Yoo
Summary: Antimicrobial resistance is a major global health threat. Naphthoquinones, derived from plants and chemicals, are effective against multidrug-resistant pathogens. This review emphasizes the structure-function relationships of naphthoquinones against multidrug-resistant pathogens and highlights their potential in combating antimicrobial resistance.
Review
Biochemistry & Molecular Biology
Giulia E. Valenti, Silvana Alfei, Debora Caviglia, Cinzia Domenicotti, Barbara Marengo
Summary: With the increasing antibiotic and anticancer drug resistance, finding therapeutic strategies to combat multi-drug resistance has become crucial. This review provides a critical overview of innovative tools available to fight multi-drug resistance and discusses the potential use of nanoparticles and peptide mimetics.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Pharmacology & Pharmacy
Rachel Yoon Kyung Chang, Sue C. Nang, Hak-Kim Chan, Jian Li
Summary: The rise of antibiotic resistance has made antibiotic therapy ineffective against bacterial infections. ESKAPE pathogens, which exhibit high levels of resistance, pose a major global health threat. Novel antimicrobial therapeutic strategies, including bacteriophages, enzymes, immunomodulators, and monoclonal antibodies, are urgently needed to address this issue.
ADVANCED DRUG DELIVERY REVIEWS
(2022)
Article
Biochemistry & Molecular Biology
Karyne Rangel, Fellipe O. Cabral, Guilherme C. Lechuga, Joao P. R. S. Carvalho, Maria H. S. Villas-Boas, Victor Midlej, Salvatore G. De-Simone
Summary: This study evaluated the bactericidal effect of high levels of ozone gas on reference and ESKAPE bacteria. The results showed that exposure to high concentrations of ozone inhibited the growth of all bacterial strains tested, significantly reducing colony counts. Cell viability of MRSA and XDR was considerably reduced, and SEM showed damage to bacteria after ozone treatment.
Article
Cell Biology
Teresa Zelante, Tsokyi Choera, Anne Beauvais, Francesca Fallarino, Giuseppe Paolicelli, Giuseppe Pieraccini, Marco Pieroni, Claudia Galosi, Claudia Beato, Antonella De Luca, Francesca Boscaro, Riccardo Romoli, Xin Liu, Adilia Warris, Paul E. Verweij, Eloise Ballard, Monica Borghi, Marilena Pariano, Gabriele Costantino, Mario Calvitti, Carmine Vacca, Vasilis Oikonomou, Marco Gargaro, Alicia Yoke Wei Wong, Louis Boon, Marcel den Hartog, Zdenek Spacil, Paolo Puccetti, Jean-Paul Latge, Nancy P. Keller, Luigina Romani
Summary: Research shows that Aspergillus fumigatus expresses different ido genes under varying environmental conditions, and loss of these genes results in increased pathogenicity and inflammation. Fungal tryptophan metabolic pathways cooperate with the host xenobiotic response to shape host-microbe interactions.
Article
Chemistry, Medicinal
Giannamaria Annunziato, Costanza Spadini, Nina Franko, Paola Storici, Nicola Demitri, Marco Pieroni, Sara Flisi, Lucrezia Rosati, Mattia Iannarelli, Marialaura Marchetti, Joana Magalhaes, Stefano Bettati, Andrea Mozzarelli, Clotilde Silvia Cabassi, Barbara Campanini, Gabriele Costantino
Summary: This study demonstrates the use of an OASS inhibitor as a colistin adjuvant to treat infections caused by Gram-positive and Gram-negative pathogens, showing promising synergistic or additive activities. The compound binds OASS, engages the intracellular target, has good safety profile, and its 3D structure complexed with OASS is determined by crystallography, providing insights for further research on developing a new class of adjuvants.
ACS INFECTIOUS DISEASES
(2021)
Article
Chemistry, Medicinal
Joana Magalhaes, Nina Franko, Samanta Raboni, Giannamaria Annunziato, Paivi Tammela, Agostino Bruno, Stefano Bettati, Stefano Armao, Costanza Spadini, Clotilde Silvia Cabassi, Andrea Mozzarelli, Marco Pieroni, Barbara Campanini, Gabriele Costantino
Summary: Many bacteria and actinomycetales use L-cysteine biosynthesis to increase their tolerance to antibacterial treatment, leading to the onset of antimicrobial resistance, which is a serious threat to public health worldwide. In this study, a series of inhibitors targeting Salmonella thyphimurium serine acetyltransferase (SAT) were developed, showing promising potential, although the most potent compound failed to inhibit bacterial growth in experiments, indicating the need for further research.
Article
Pharmacology & Pharmacy
Michele Biagioli, Silvia Marchiano, Rosalinda Roselli, Cristina Di Giorgio, Rachele Bellini, Martina Bordoni, Anna Gidari, Samuele Sabbatini, Daniela Francisci, Bianca Fiorillo, Bruno Catalanotti, Eleonora Distrutti, Adriana Carino, Angela Zampella, Gabriele Costantino, Stefano Fiorucci
Summary: The study found that pelargonidin can reverse intestinal inflammation by activating the Aryl hydrocarbon Receptor, reducing ACE2 induction. This has potential implications for combating SARS-CoV-2.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Simone Giovannuzzi, Chad S. Hewitt, Alessio Nocentini, Clemente Capasso, Gabriele Costantino, Daniel P. Flaherty, Claudiu T. Supuran
Summary: The inhibition of alpha-class carbonic anhydrases (CAs) from bacterial pathogens by phenols and phenolic acids was investigated. Small changes in the phenol scaffold led to drastic effects on the inhibitory activity of bacterial CA. This underinvestigated class of bacterial CA inhibitors may have potential in fighting drug resistant bacteria.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Andrea Angeli, Emanuela Berrino, Simone Carradori, Claudiu T. Supuran, Marzia Cirri, Fabrizio Carta, Gabriele Costantino
Summary: After being neglected in the past, carbonic anhydrase activators (CAAs) have been proven to be useful in pharmaceutical and industrial applications, with amino acid and amine derivatives being the most explored compounds.
Article
Biochemistry & Molecular Biology
Damiano Tanini, Antonella Capperucci, Maria Locuoco, Marta Ferraroni, Gabriele Costantino, Andrea Angeli, Claudiu T. Supuran
Summary: A series of benzoselenoates were prepared and investigated for their inhibitory properties against various human Carbonic Anhydrases isoforms. The study revealed that benzoselenoates may serve as potential new inhibitors with higher selectivity and efficacy for different hCAs.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Andrea Angeli, Marta Ferraroni, Antonella Capperucci, Damiano Tanini, Gabriele Costantino, Claudiu T. Supuran
Summary: This study presents the activity of selenocarbamates as novel carbonic anhydrase (CA) inhibitors. Through CA-mediated hydrolysis, selenocarbamates release selenolates that effectively inhibit CA by binding to zinc. Different human CA isoforms were evaluated against a series of selenocarbamates with high molecular diversity and complexity. X-ray studies provided insights into the binding mode of this novel class of CA inhibitors.
Article
Biochemistry & Molecular Biology
Andrea Angeli, Marta Ferraroni, Fabrizio Carta, Cecile Haeberli, Jennifer Keiser, Gabriele Costantino, Claudiu T. Supuran
Summary: The limited options for treating schistosomiasis necessitate the discovery of alternative drugs. This study successfully inhibited the growth of Schistosoma mansoni using new PZQ derivatives, but further optimization is still needed.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Silvia Grottelli, Giannamaria Annunziato, Gioena Pampalone, Marco Pieroni, Mirco Dindo, Francesca Ferlenghi, Gabriele Costantino, Barbara Cellini
Summary: This study aimed to find pharmacological chaperones for the treatment of primary hyperoxaluria type I (PH1). The researchers screened and chemically optimized compounds, identifying a promising hit compound and drawing conclusions about the requirements for optimal pharmacological chaperone activity.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Filippo Pigazzani, Davide Gorni, Kenneth A. Dyar, Matteo Pedrelli, Gwen Kennedy, Gabriele Costantino, Agostino Bruno, Isla Mackenzie, Thomas M. MacDonald, Uwe J. F. Tietge, Jacob George
Summary: Oxidative stress plays a role in the development and exacerbation of cardiovascular diseases. Derivatives-reactive oxygen metabolites (d-ROMs) are a new biomarker of oxidative stress that can be quantified within minutes. High levels of d-ROMs are an independent predictor of cardiovascular events and mortality, while low levels of d-ROMs are a good negative predictor for cardiovascular events in patients with coronary artery disease and heart failure. Combining d-ROMs with other commonly used biomarkers may help in more accurate cardiovascular risk assessment.
Article
Chemistry, Medicinal
Giannamaria Annunziato, Costanza Spadini, Marialaura Marchetti, Nina Franko, Marialaura Pavone, Mattia Iannarelli, Agostino Bruno, Marco Pieroni, Stefano Bettati, Clotilde Silvia Cabassi, Barbara Campanini, Gabriele Costantino
Summary: Antibacterial adjuvants are important for reducing therapeutic dose and antibacterial resistance. OASS inhibitors were found to be potential colistin adjuvants for treating infections caused by critical pathogens. Derivatives of OASS inhibitors showed good activity and low toxicity in vitro, and exhibited additive or synergistic effects against pathogenic bacteria in vitro. The engagement of OASS inside bacteria cells was confirmed.
Article
Chemistry, Medicinal
Gustavo Provensi, Alessia Costa, Barbara Rani, Maria Vittoria Becagli, Fabio Vaiano, Maria Beatrice Passani, Damiano Tanini, Antonella Capperucci, Simone Carradori, Jacobus P. Petzer, Anel Petzer, Daniela Vullo, Gabriele Costantino, Patrizio Blandina, Andrea Angeli, Claudiu T. Supuran
Summary: This study reported the synthesis of β-arylchalcogeno amines with structural similarity to amphetamine, which showed good activation properties for certain enzymes in the brain. In vivo evaluation demonstrated the procognitive effects of these compounds without causing unwanted side effects. These findings suggest the potential utility of these compounds for improving cognitive decline associated with neurodegenerative and psychiatric diseases.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Miriam Girardini, Francesca Ferlenghi, Giannamaria Annunziato, Giulia Degiacomi, Bianca Papotti, Cinzia Marchi, Jose Camilla Sammartino, Sari S. Rasheed, Anna Contini, Maria Rosalia Pasca, Federica Vacondio, Joanna C. Evans, Thomas Dick, Rolf Mueller, Gabriele Costantino, Marco Pieroni
Summary: Tuberculosis is a deadly infectious disease and the increase in drug-resistant strains is concerning. Previous studies have identified compounds with inhibitory activity against Mycobacterium tuberculosis strains. In this study, researchers aimed to determine the metabolic fate of these compounds and explore structural modifications to improve activity and avoid rapid clearance. Novel antitubercular chemotypes were also investigated. The findings led to the design of improved compounds with good activity against drug-susceptible and drug-resistant strains.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Marialaura Pavone, Samanta Raboni, Marialaura Marchetti, Giannamaria Annunziato, Stefano Bettati, Bianca Papotti, Cinzia Marchi, Emanuele Carosati, Marco Pieroni, Barbara Campanini, Gabriele Costantino
Summary: The development of antibiotic adjuvants as inhibitors of non-essential targets is an innovative approach to combat antimicrobial resistance. This study focuses on compounds targeting serine acetyltransferase (SAT), a key enzyme involved in cysteine biosynthesis. A new compound with promising SAT inhibitory activity has been discovered, and further investigation into its potential and structure-activity relationships has been conducted.
RESULTS IN CHEMISTRY
(2022)
