Abstract

Throughout the centuries, traditional Chinese medicine has been a rich resource in the development of new drugs. Modern drug discovery, which relies increasingly on automated high throughput screening and quick hit-to-lead development, however, is confronted with the challenges of the chemical complexity associated with natural products. New technologies for biological screening as well as library building are in great demand in order to meet the requirements. Here we review the developments in these techniques under the perspective of their applicability in natural product drug discovery. Methods in library construction, component characterization, biological evaluation, and other screening approaches including NMR and X-ray diffraction are discussed.

Keywords: Traditional Chinese medicine, natural products, high throughput screening, drug discovery, TCM, Saliva Miltiorrhiza, structure-activity relationship, SAR, HTS, Bioassay-Guided Isolation, nuisance compounds, promiscuous inhibitors, frequent hitters, Isatis tinctoria, Target-Based Bioassays, Schizandra chinensis, Fluorescence resonance energy transfer, FRET, Homogeneous time-resolved fluorescence, HTRF, Chemiluminescence, Cell-Based Bioassays, luciferase, chloramphenicol acetyltransferase, CAT, galactosidase, green fluorescence protein, Tripterygium wilfordii, Drosophila melanogaster, matrix-assisted laser desorption/ionization, MALDI, Affinity size-exclusion chromatography, Capillary Electrophoresis-Based Assay, Affinity capillary electrophoresis, ACE, immobilized liposome chromatography, IAMC, cell membrane chromatography, CMC, X-ray crystallography, Protein crystallography