Abstract

Historically, natural products have been used since ancient times and in folklore for the treatment of many diseases and illnesses. Classical natural product chemistry methodologies enabled a vast array of bioactive secondary metabolites from terrestrial and marine sources to be discovered. Many of these natural products have gone on to become current drug candidates. This brief review aims to highlight historically significant bioactive marine and terrestrial natural products, their use in folklore and dereplication techniques to rapidly facilitate their discovery. Furthermore a discussion of how natural product chemistry has resulted in the identification of many drug candidates; the application of advanced hyphenated spectroscopic techniques to aid in their discovery, the future of natural product chemistry and finally adopting metabolomic profiling and dereplication approaches for the comprehensive study of natural product extracts will be discussed.

Highlights

  • In recent years the advances in microcoil HPLC-nuclear magnetic resonance (NMR) and capillary NMR (CapNMR) has allowed for smaller quantities of samples to be analyzed in the order of 40–120 μL, this in combination with higher field magnets has greatly increased the sensitivity in profiling and dereplication natural product extracts [138,139,140]

  • We propose that a combination of metabolomics technologies with natural product discovery processes will be beneficial on multiple levels

  • By increasing the number of identifications in our metabolomics data we may provide novel structures to be tested for bioactivity for any disease under investigation

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Summary

A Historical Overview of Natural Products in Drug Discovery

Metabolomics Australia, School of Botany, The University of Melbourne, Parkville, Victoria 3010, Australia. Institute (HIRi) RMIT University, G.P.O. Box 2476V, Melbourne, Victoria 3001, Australia. Australian Centre for Plant Functional Genomics, School of Botany, The University of Melbourne, Parkville, 3010, Victoria, Australia. Received: 1 March 2012; in revised form: 31 March 2012 / Accepted: 31 March 2012 /

Natural Products in History
Medicinal Plants in Folklore
Medicinal Natural Products from Other Sources Used in Folklore
Historically Important Natural Products
Natural Products from Fungi
Natural Products from Plants
Natural Products from the Marine Environment
Natural Products from Marine Algae
Natural Products from Marine Sponges
Natural Products from other Marine Sources
Drug Discovery
Dereplication
Dereplication Methods
Database Searching
Findings
Conclusions
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