title: How to translate a bioassay into a screening assay for natural products: general considerations and implementation of antimicrobial screens.
abstract: Natural product sources have been a valuable provider of molecular diversity in many drug discovery programs and several therapeutically important drugs have been isolated from these. However, the screening of such materials can be very complicated due to the fact that they contain a complex mixture of secondary metabolites, but also the purified natural compounds exert a challenge for bioactivity screening. Success in identifying new therapeutics using in vitro bioassays is largely dependent upon the proper design, validation, and implementation of the screening assay. In this review, we discuss some aspects which are of significant concern when screening natural products in a microtiter plate-based format, being partly applicable to other assay formats as well, such as validation parameters, layouts for assay protocols, and common interferences caused by natural products samples, as well as various troubleshooting strategies. Examples from the field of natural product drug discovery of antibacterial compounds are discussed, and contributions from the realm of academic screenings are highlighted.
authors.affiliation: Division of Pharmaceutical Biosciences, Centre for Drug Research, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.
authors.forename: Adyary
authors.initials: A
authors.lastname: Fallarero
authors.affiliation: Division of Pharmaceutical Biosciences, Centre for Drug Research, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.
authors.forename: Leena
authors.initials: L
authors.lastname: Hanski
authors.affiliation: Division of Pharmaceutical Biosciences, Centre for Drug Research, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.
authors.forename: Pia
authors.initials: P
authors.lastname: Vuorela
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000302:isolation & purification / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D001681:Biological Assay / Q000379:methods*; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology*; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D054852:Small Molecule Libraries
chemical_list: D000900:Anti-Bacterial Agents; D001688:Biological Products; D010936:Plant Extracts; D054852:Small Molecule Libraries