Coupling biological detection to liquid chromatography: a new tool in drug discovery
| Autor: | Ricardo Borges, Jesica Diaz, José J. Fernández, Mónica S. Montesinos, R. González-Brito, M. A. Campuzano-Bublitz, José G. Hernández-Jiménez |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Drug media_common.quotation_subject Pharmacology toxicology High-performance liquid chromatography Rats Sprague-Dawley 03 medical and health sciences 0302 clinical medicine Organ Culture Techniques Medium pressure Drug Discovery Animals Stevia Tissue Distribution media_common Pharmacology Chromatography Chemistry Drug discovery Plant Extracts General Medicine Rats Coupling (electronics) Stevia rebaudiana 030104 developmental biology 030217 neurology & neurosurgery Chromatography Liquid |
| Zdroj: | Naunyn-Schmiedeberg's archives of pharmacology. 391(1) |
| ISSN: | 1432-1912 |
| Popis: | Procedures to characterize drugs that can be obtained from plant extracts or combinatorial chemistry are tedious, and they consume considerable resources (e.g., animals) and time. Thus, we have looked for a way to streamline this process. We describe here a novel system for the pre-characterization of drugs based on liquid chromatography coupled to biological detection using perifused or perfused organs. This novel system allows the on-line detection of pharmacologically active substances in hydrosoluble mixtures from vegetal extracts or combinatorial chemistry libraries. Depending on the volume of drug solution and concentration of the samples, the procedure can work through either medium pressure liquid chromatography or HPLC, and it enables the fingerprints of drugs to be assessed based on their contractile activity on combinations of different isolated tissues. As an example, we show how the system can identify active fractions from an extract of Stevia rebaudiana Bertoni, an activity that was later associated with rebaudioside N. Coupling liquid chromatography to biological detection offers a rapid way to focus attention on active products in complex samples, mostly from hydrosoluble species, helping to considerably reduce the time and cost of the pre-characterization of drugs. |
| Databáze: | OpenAIRE |
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