Abstract
Cyanobacteria possess the ability to produce compounds with remarkable biological activity, and have thus attracted the attention of the pharmaceutical industry. Cyanopeptides acting as protease inhibitors have shown potential in the field of pharmacotherapy through regulation of abnormal physiological processes in the human body. Despite the already described cyanopeptide protease inhibitors, the search for new congeners is of considerable interest which may pave the way for more efficient molecules. In this study, the presence of the protease inhibitors aeruginosin and cyanopeptolin with non-, mono- and dichlorination and also genes coding for their synthetases was investigated in 90 cyanobacterial strains. Mass spectrometry analyses highlighted production of 91, 19 and 3 non-, mono- and dichlorinated congeners, respectively. The purified extract of Microcystis botrys SPC759 inhibited 61% of pepsin protease. PCR amplifications of aeruginosin and cyanopeptolin synthetase gene regions were observed in 41 and 28% of evaluated strains, respectively. The sequences obtained for the aerA-aerB (aeruginosin) and mcnC-mcnE (cyanopeptolin) gene regions grouped together with their homologues found in other cyanobacterial strains in the phylogenetic analyses with high bootstrap support. Antimicrobial activity assays performed using all intracellular extracts inhibited 31 and 26% of Gram-negative and Gram-positive pathogenic bacterial growth, respectively. The results of this study showed the production of aeruginosin and cyanopeptolin and the presence of their genes in several cyanobacterial genera for the first time besides the discovery of novel congeners.
Keywords: Antimicrobial, aeruginosin, bioactive peptides, chlorination, cyanobacteria, cyanopeptolin, mass spectrometry, natural products, pepsin, protease inhibitors
Current Medicinal Chemistry
Title:Non-Ribosomal Halogenated Protease Inhibitors from Cyanobacterial Isolates as Attractive Drug Targets
Volume: 19 Issue: 30
Author(s): M.E. Silva-Stenico, J. Rigonato, M.G. Leal, M.G.M.V. Vaz, A.P.D. Andreote and M.F. Fiore
Affiliation:
Keywords: Antimicrobial, aeruginosin, bioactive peptides, chlorination, cyanobacteria, cyanopeptolin, mass spectrometry, natural products, pepsin, protease inhibitors
Abstract: Cyanobacteria possess the ability to produce compounds with remarkable biological activity, and have thus attracted the attention of the pharmaceutical industry. Cyanopeptides acting as protease inhibitors have shown potential in the field of pharmacotherapy through regulation of abnormal physiological processes in the human body. Despite the already described cyanopeptide protease inhibitors, the search for new congeners is of considerable interest which may pave the way for more efficient molecules. In this study, the presence of the protease inhibitors aeruginosin and cyanopeptolin with non-, mono- and dichlorination and also genes coding for their synthetases was investigated in 90 cyanobacterial strains. Mass spectrometry analyses highlighted production of 91, 19 and 3 non-, mono- and dichlorinated congeners, respectively. The purified extract of Microcystis botrys SPC759 inhibited 61% of pepsin protease. PCR amplifications of aeruginosin and cyanopeptolin synthetase gene regions were observed in 41 and 28% of evaluated strains, respectively. The sequences obtained for the aerA-aerB (aeruginosin) and mcnC-mcnE (cyanopeptolin) gene regions grouped together with their homologues found in other cyanobacterial strains in the phylogenetic analyses with high bootstrap support. Antimicrobial activity assays performed using all intracellular extracts inhibited 31 and 26% of Gram-negative and Gram-positive pathogenic bacterial growth, respectively. The results of this study showed the production of aeruginosin and cyanopeptolin and the presence of their genes in several cyanobacterial genera for the first time besides the discovery of novel congeners.
Export Options
About this article
Cite this article as:
Silva-Stenico M.E., Rigonato J., Leal M.G., Vaz M.G.M.V., Andreote A.P.D. and Fiore M.F., Non-Ribosomal Halogenated Protease Inhibitors from Cyanobacterial Isolates as Attractive Drug Targets, Current Medicinal Chemistry 2012; 19 (30) . https://dx.doi.org/10.2174/092986712803530539
DOI https://dx.doi.org/10.2174/092986712803530539 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
![](/images/wayfinder.jpg)
- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
-
Mouse Models of Autoimmune Diseases - Autoimmune Myocarditis
Current Pharmaceutical Design Targeting Molecular Imaging Approach for Detection of Infection and Inflammation by Diagnostic Nuclear Medicine Techniques
Current Medical Imaging Editorial [Hot Topic: Nitric Oxide and Lipoxins: Role in Inflammation and Defence (Guest Editor: Stefano Fiorucci)]
Inflammation & Allergy - Drug Targets (Discontinued) Amyloid-Degrading Enzymes as Therapeutic Targets in Alzheimers Disease
Current Alzheimer Research Channel-Like Functions of the 18-kDa Translocator Protein (TSPO): Regulation of Apoptosis and Steroidogenesis as Part of the Host-Defense Response
Current Pharmaceutical Design Diabetes Mellitus and Renal Function: Current Medical Research and Opinion
Current Diabetes Reviews Hypersensitivity to Antineoplastic Agents
Current Pharmaceutical Design Novel Therapeutic Approaches in Limiting Oxidative Stress and Inflammation
Current Pharmaceutical Biotechnology Impact of COVID-19 Pandemic on Cardiology Resident Training and Education
New Emirates Medical Journal Pharmacological Inhibition of Protein Tyrosine Phosphatase 1B: A Promising Strategy for the Treatment of Obesity and Type 2 Diabetes Mellitus
Current Medicinal Chemistry Recent Advancement and Technological Aspects of Pulsatile Drug Delivery System - A Laconic Review
Current Drug Targets Secondary Prevention of Ischemic Stroke
Current Drug Targets Patented Small Molecules Used for Reprogramming
Recent Patents on Regenerative Medicine Bridge Between Neuroimmunity and Traumatic Brain Injury
Current Pharmaceutical Design Severe Influenza: Clinical Features and Treatment Options
Current Respiratory Medicine Reviews Synthesis of Medicinally Privileged Heterocycles through Dielectric Heating
Current Medicinal Chemistry Vasopressin in Liver Disease – Should We Turn On or Off?
Current Clinical Pharmacology Role of Heat Shock Proteins in Atherosclerosis and Atrial Fibrillation
Current Immunology Reviews (Discontinued) Nutraceuticals, Nutritional Therapy, Phytonutrients, and Phytotherapy for Improvement of Human Health: A Perspective on Plant Biotechnology Application
Recent Patents on Biotechnology Neonatal Fever in the Term Infant: Evaluation and Management Strategies
Current Pediatric Reviews