High-throughput fractionation of natural products for drug discovery.

Abstract 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.