Meeting Abstract

S6.8  Monday, Jan. 5  From Secondary Metabolites to Drugs: Rationale, Purification and Biological Screening TASDEMIR, Deniz; University of London, London deniz.tasdemir@pharmacy.ac.uk

Chemical compounds derived from plants, animals and microorganisms have formed the basis of most early medicines. Despite the significant advances in organic chemistry and the availability of large libraries of synthetic or combinatorial compounds, the secondary metabolites (SMs, natural products) are still the most prolific source for drugs because of their higher chemical diversity, biochemical specificity and other molecular properties, which make them superior to synthetic compounds as lead structures for drug discovery. This is believed to be due to the fact that SMs are structures, which have evolved through ecological pressures, such as competition and predation, for millions of years. So natural products can be viewed as privileged structures selected and optimized by evolutionary pressures to interact with a variety of proteins and other targets of the organisms predators, and thus possess a higher potential to interact with human proteins. The ability of a small molecule SM to bind or otherwise inhibit a certain macromolecule is the basic concept of drug discovery and explains the higher drug-like properties of SMs. In conclusion, the biological activity of SMs is of relevance for their ecological function, but is also the basis of their biomedical importance. Typical natural product drug discovery is a complex process. It includes the extraction and initial screening of natural material against a validated target, purification of its bioactive principle(s) by chromatography and structure elucidation of the active component(s) by spectroscopic methods. The selection of target protein/cell line and screening technique is crucial. This lecture will deal with high throughput screening, bioactivity-driven isolation and characterization of natural products from plants and marine invertebrates against established targets in cancer and malaria.