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Journal of Biomolecular Screening
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Natural Products in High Throughput Screening: Automated High-Quality Sample Preparation

Ingrid Schmid

Hans-Knoll-Institute for Natural Products Research, Beutenbergstrale 11, D-07745 Jena, Germany

Isabel Sattler

Hans-Knoll-Institute for Natural Products Research, Beutenbergstrale 11, D-07745 Jena, Germany

Susanne Grabley

Hans-Knoll-Institute for Natural Products Research, Beutenbergstrale 11, D-07745 Jena, Germany

Ralf Thiericke

Hans-Knoll-Institute for Natural Products Research, Beutenbergstrale 11, D-07745 Jena, Germany

At present, compound libraries from combinatorial chemistry are the major source for high throughput screening (HTS) programs in drug discovery. On the other hand, nature has been proven to be an outstanding source for new and innovative drugs. Secondary metabolites from plants, animals, and microorganisms show a striking structural diversity that supplements chemically synthesized compounds or libraries in drug discovery programs. Unfortunately, extracts from natural sources are usually complex mixtures of compounds, often generated in time-consuming and, for the most part, manual processes. Because quality and quantity of the provided samples play a pivotal role in the success of HTS programs, this poses serious problems. In order to make samples of natural origin competitive with synthetic compound libraries, we devised a novel, automated sample preparation procedure based on solid-phase extraction (SPE). By making use of modified Zymark (Hopkinton, MA) RapidTrace® SPE workstations, we developed an easy-to-handle and effective fractionation method that generates high-quality samples from natural origin, fulfilling the requirements for an integration in high throughput drug discovery programs.

Journal of Biomolecular Screening, Vol. 4, No. 1, 15-25 (1999)
DOI: 10.1177/108705719900400104
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[Abstract] [Full Text]