Abstract
Cryptococcosis is a fungal disease of global significance for which new effective treatments are needed. The conjugation of the synthetic antimicrobial peptide fragment UBI 31-38 to a coumarin derivative showed to be an effective approach for the design of a novel anticryptococcal agent. In addition to antifungal activity, the conjugate exhibited intense fluorescence, which could be valuable for mechanistic investigations of this molecule. In this work, we studied the photophysical properties of the conjugate and confocal scanning laser microscopy was used to inspect the distribution of the peptide-coumarin conjugate in Cryptococcus cell. The synergism of this compound with amphotericin B or fluconazole against C. gattii and C. neoformans strains was also investigated. The results indicated that the fluorescent conjugate alone as well as its combination with amphotericin B are promising tools against cryptococcosis.
Keywords: UBI 31-38, peptide-coumarin conjugate, fluorescent, anticryptococcal activity, interaction studies, confocal scanning laser microscopy.
Current Topics in Medicinal Chemistry
Title:A UBI 31-38 Peptide-coumarin Conjugate: Photophysical Features, Imaging Tracking and Synergism with Amphotericin B Against Cryptococcus
Volume: 18 Issue: 2
Author(s): Soraya M.Z.M.D. Ferreira, Hellem C. Carneiro, Rosemeire B. Alves, Ana Carolina S. Batista, Eufranio N. da Silva Junior, Gleiston G. Dias, Jarbas M. Resende, Daniel A. Santos, Debora L. Oliveira, Marcio L. Rodrigues and Rossimiriam P. Freitas*
Affiliation:
- Departamento de Quimica, Instituto de Ciencias Exatas, Universidade Federal de Minas Gerais, Belo Horizonte,Brazil
Keywords: UBI 31-38, peptide-coumarin conjugate, fluorescent, anticryptococcal activity, interaction studies, confocal scanning laser microscopy.
Abstract: Cryptococcosis is a fungal disease of global significance for which new effective treatments are needed. The conjugation of the synthetic antimicrobial peptide fragment UBI 31-38 to a coumarin derivative showed to be an effective approach for the design of a novel anticryptococcal agent. In addition to antifungal activity, the conjugate exhibited intense fluorescence, which could be valuable for mechanistic investigations of this molecule. In this work, we studied the photophysical properties of the conjugate and confocal scanning laser microscopy was used to inspect the distribution of the peptide-coumarin conjugate in Cryptococcus cell. The synergism of this compound with amphotericin B or fluconazole against C. gattii and C. neoformans strains was also investigated. The results indicated that the fluorescent conjugate alone as well as its combination with amphotericin B are promising tools against cryptococcosis.
Export Options
About this article
Cite this article as:
Ferreira M.Z.M.D. Soraya , Carneiro C. Hellem , Alves B. Rosemeire, Batista Carolina S. Ana , da Silva Junior N. Eufranio , Dias G. Gleiston , Resende M. Jarbas , Santos A. Daniel , Oliveira L. Debora , Rodrigues L. Marcio and Freitas P. Rossimiriam*, A UBI 31-38 Peptide-coumarin Conjugate: Photophysical Features, Imaging Tracking and Synergism with Amphotericin B Against Cryptococcus, Current Topics in Medicinal Chemistry 2018; 18 (2) . https://dx.doi.org/10.2174/1568026618666180221113137
DOI https://dx.doi.org/10.2174/1568026618666180221113137 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Adaptogens—History and Future Perspectives
Adaptogens are pharmacologically active compounds or plant extracts that are associated with the ability to enhance the body’s stability against stress. The intake of adaptogens is associated not only with a better ability to adapt to stress and maintain or normalise metabolic functions but also with better mental and physical ...read more
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chronic Kidney Disease
The scope of the special thematic issue includes but not limited to the mechanism of chronic kidney disease (CKD), the treatment of renal fibrosis and early diagnosis of CKD and so on. We also welcome manuscripts from other scientific research area with respect to internal medicine. Cell death has been ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Current Status on 1,4-Dihydropyridine Derivatives against Human
Pathogenic Parasites
Current Medicinal Chemistry The Effects of Soluble Aβ Oligomers on Neurodegeneration in Alzheimer's Disease
Current Pharmaceutical Design Targeting Mitochondrial Bioenergetics for Alzheimers Prevention and Treatment
Current Pharmaceutical Design Withdrawal Notice: Evaluation of Clinical Profile, Diagnostic Tests, And Prognosis of Crypto-coccal Meningitis in HIV Infected Patients in Western India
Infectious Disorders - Drug Targets New Developments of Clinical Trial in Immunotherapy for Alzheimer's Disease
Current Pharmaceutical Biotechnology Genetic Modifications of Icosahedral Plant Virus-based Nanoparticles for Vaccine and Immunotherapy Applications
Current Protein & Peptide Science Potential Relevance of Melatonin Against Some Infectious Agents: A Review and Assessment of Recent Research
Current Medicinal Chemistry Preclinical Study of the Pharmacokinetics of p75ECD-Fc, a Novel Human Recombinant Protein for Treatment of Alzheimer’s Disease, in Sprague Dawley Rats
Current Drug Metabolism Neurotuberculosis: An Overview
Central Nervous System Agents in Medicinal Chemistry Human Parvovirus B19: An Infectious Agent with the Potential to Induce and Trigger Rheumatic Disease
Current Rheumatology Reviews Determination of Spatial and Temporal Distribution of Microglia by 230nm-High-Resolution, High-Throughput Automated Analysis Reveals Different Amyloid Plaque Populations in an APP/PS1 Mouse Model of Alzheimers Disease
Current Alzheimer Research <i>Larrea tridentata</i> and its Biological Activities
Current Topics in Medicinal Chemistry Immunotherapy for Alzheimers Disease: Potential Problems and Possible Solutions
Current Immunology Reviews (Discontinued) Discovery, SAR and Medicinal Chemistry of Herpesvirus Helicase Primase Inhibitors
Current Medicinal Chemistry - Anti-Infective Agents Neuroinflammation and Complexes of 17β -Hydroxysteroid Dehydrogenase type 10 - Amyloid β in Alzheimer's Disease
Current Alzheimer Research Challenges with Mosquito-borne Viral Diseases: Outbreak of the Monsters
Current Topics in Medicinal Chemistry Role of Formyl Peptide Receptors (FPR) in Abnormal Inflammation Responses Involved in Neurodegenerative Diseases
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry A Case of Cerebral Toxoplasmosis and Cryptococcosis Preferred Therapy Associated Adverse Drug Reactions in a Patient Newly Co-diagnosed with Acquired Immune Deficiency Syndrome
Current Drug Safety Therapeutic Modulation of Cytokines in Chronic Infectious Diseases
Current Pharmaceutical Design PFGE: Importance in Food Quality
Recent Patents on Food, Nutrition & Agriculture