Abstract

The marine environment is a rich source of chemically diverse, biologically active natural products, and serves as an invaluable resource in the ongoing search for novel antimicrobial compounds. Recent advances in extraction and isolation techniques, and in state-of-the-art technologies involved in organic synthesis and chemical structure elucidation, have accelerated the numbers of antimicrobial molecules originating from the ocean moving into clinical trials. The chemical diversity associated with these marine-derived molecules is immense, varying from simple linear peptides and fatty acids to complex alkaloids, terpenes and polyketides, etc. Such an array of structurally distinct molecules performs functionally diverse biological activities against many pathogenic bacteria and fungi, making marine-derived natural products valuable commodities, particularly in the current age of antimicrobial resistance. In this review, we have highlighted several marine-derived natural products (and their synthetic derivatives), which have gained recognition as effective antimicrobial agents over the past five years (2012–2017). These natural products have been categorized based on their chemical structures and the structure-activity mediated relationships of some of these bioactive molecules have been discussed. Finally, we have provided an insight into how genome mining efforts are likely to expedite the discovery of novel antimicrobial compounds.

Highlights

  • Infectious diseases caused by bacteria, fungi and viruses pose a major threat to public health despite the tremendous progress in human medicine

  • These brominated ethers exhibited in vitro antibacterial activity against MRSA, methicillin-sensitive Staphylococcus aureus (MSSA), E. coli O157:H7, and Salmonella

  • The addition of an extra cinnamyl derivative in compound 122 to the terminal amine of the spermine chain decreased the antibacterial selectivity between P. aeruginosa and S. aureus; the observed selectivity may be due to differential cell permeability between the Gram-negative and the Gram-positive bacteria [74]

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Summary

Introduction

Infectious diseases caused by bacteria, fungi and viruses pose a major threat to public health despite the tremendous progress in human medicine. Humans have turned to nature as a source of invaluable medicinal products, where terrestrial and marine organisms traditionally provide the most effective remedies [4,5]. It was only after the discovery of penicillin in 1928 that microbial sources were explored as sources of new therapeutic molecules. Many natural products were identified as promising candidates for drug development using bioassay-guided investigations, and chemical structure elucidation techniques [5,8] Too often this approach led to the re-isolation of known compounds. A number of other compounds boasting antibacterial, antidiabetic, antifungal, antiinflammatory and antiviral properties, properties, as well as potentially compoundsaffecting potentially affectingsystem, the nervous system,being are currently being as well as compounds the nervous are currently investigated for investigated use in and clinical andofthus form part of the preclinical use in clinicalfor settings thussettings form part the preclinical pipeline [27,28,29]. pipeline [27,28,29]

Chemical Entities in the Preclinical Antimicrobial Pipeline
Marine
Alkaloids
Antimicrobial
Lipids
Peptides
Halogenated Compounds
Polyketides
10. Isocoumarins
11. Nucleosides
Terretrione
13. Synthetic Interventions
14. Genome Mining of Marine Microorganisms—The Future of Antimicrobial Discovery
Findings
Concluding Remarks
Full Text
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