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What do all of these have in common?

What do all of these have in common?. They all contain natural products…. Natural Products Drug Discovery. Searching for Cures in the Plant Kingdom. Primary Metabolites. Molecules that are necessary for survival of organism lipids, nucleic acids, proteins, polysaccharides.

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What do all of these have in common?

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  1. What do all of these have in common?

  2. They all contain natural products… Natural Products Drug Discovery Searching for Cures in the Plant Kingdom

  3. Primary Metabolites • Molecules that are necessary for survival of organism • lipids, nucleic acids, proteins, polysaccharides

  4. Secondary Metabolites • Not essential to the survival of the organism • May give the organism a selective advantage • Limited distribution in nature • Also called Natural Products • Show bioactivity– the ability to inhibit the growth of microbes taxol

  5. Most natural products have been found in plants, fungi and bacteria

  6. Step 1: Extraction • Extracts contain all of the compounds in the cell • HOW? Add a solvent to the plant sample. • Solvents can be either polar or nonpolar

  7. Choices, choices… which solvent to use? • The solvent is chosen based on the properties of the molecule you want to extract • Most bioactive compounds are POLAR.

  8. How a solvent works • Solvent breaks the cell membrane open. • “Like dissolves like” – the polar solvent draws out the polar compounds into solution • The smaller the pieces, the greater the surface area available for the solvent to work on the cells.

  9. Step 2: Microbial Bioassay • Are the compounds in the extract bioactive? • Bioactive = able to inhibit the growth of microbes • Test the extract on E. coli (prokaryote) & S. cerevisiae (eukaryote) – see if extract can inhibit growth

  10. Prokaryotes vs. Eukaryotes

  11. Microbial Assay • Microbe is plated onto agar plate • Sterile Discs are dipped into extract

  12. Microbial Assay • Discs are placed on the plate

  13. Microbial Assay: Controls • Positive Control = Iodine • Negative Control = Solvent only

  14. Extract Disc 1 Positive Control Negative Control Extract Disc 2

  15. Zones of Inhibition • If an extract is bioactive, it causes a halo to form around the disc (prevents growth) • The size of the halo (the zone of inhibition) indicates how effective an extract is as an antimicrobial agent.

  16. Original source of natural product Extracts prepared Biological testing (Bioassay) Fractionation and Purification of active compound(s) Determination of the Chemical Structure Pre-clinical testing (pre-human testing) Human clinical trials FDA Approval How are Natural Products discovered?10-15 yrs.$83 million

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