High-Throughput Fractionation of Natural Products for Drug Discovery

An automated high-throughput method applied to the production and analysis of libraries of natural �products for high-throughput biological screening is described. The production of the library includes solid-phase extraction of crude extracts to remove polyphenols, followed by automated preparative high-performance liquid chromatography (HPLC) fractionation. Libraries of fractions are analyzed by an ultra-performance liquid chromatography–UV diode-array detection–evaporative light scattering detection–mass spectrometry system (UPLC/PDA/ELSD/MS) to provide information that facilitates characterization of compounds in active fractions. This system fractionates 2,600 unique natural product samples per year, providing fractions in 0.5–10 mg scale for creation of libraries that could be used for the screening of multiple targets to identify hits for various applications including drug discovery.