Evaluating Marine Cyanobacteria as a Source for CNS Receptor Ligands
| Autor: | Stacy‐Ann J. Parker, Andrea L Rague, Kevin Tidgewell |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
Cyanobacteria
Central Nervous System Aquatic Organisms Cannabinoid receptor natural products Pharmaceutical Science Biology Ligands 01 natural sciences Article Analytical Chemistry lcsh:QD241-441 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine lcsh:Organic chemistry Drug Discovery Radioligand Autophagy Humans Physical and Theoretical Chemistry Receptor Receptors Cannabinoid G protein-coupled receptor Cell Proliferation Biological Products Natural product 010405 organic chemistry Ligand Organic Chemistry marine cyanobacteria Transporter biology.organism_classification 0104 chemical sciences Receptors Adrenergic Biochemistry chemistry Chemistry (miscellaneous) Receptors Serotonin Vesicular Monoamine Transport Proteins G-protein coupled receptor Molecular Medicine 030217 neurology & neurosurgery |
| Zdroj: | Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry Molecules Volume 23 Issue 10 Molecules, Vol 23, Iss 10, p 2665 (2018) |
| ISSN: | 1420-3049 |
| Popis: | Natural products have a long history as a source of psychoactive agents and pharmacological tools for understanding the brain and its circuitry. In the last two decades, marine cyanobacteria have become a standard source of natural product ligands with cytotoxic properties. The study of cyanobacterial metabolites as CNS modulatory agents has remained largely untapped, despite the need for new molecules to treat and understand CNS disorders. We have generated a library of 301 fractions from 37 field collected cyanobacterial samples and screened these fractions against a panel of CNS receptors using radiolabeled ligand competitive-binding assays. Herein we present an analysis of the screening data collected to date, which show that cyanobacteria are prolific producers of compounds which bind to important CNS receptors, including those for 5-HT, DA, monoamine transporters, adrenergic, sigma, and cannabinoid receptors. In addition to the analysis of our screening efforts, we will also present the isolation of five compounds from the same cyanobacterial collection to illustrate how pre-fractionation followed by radioligand screening can lead to rapid identification of selective CNS agents. The systematic screening of natural products sources, specifically filamentous marine cyanobacteria, will yield a number of lead compounds for further development as pharmacological tools and therapeutics. |
| Databáze: | OpenAIRE |
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