Label-free cell phenotypic profiling identifies pharmacologically active compounds in two traditional Chinese medicinal plants

摘要: Traditional Chinese Medicines (TCMs) are widely used in clinical practice and natural products have been a rich resource for drug discovery. Identification of pharmacologically active chemical constituents is essential to the future TCMs product-based Here we report label-free cell phenotypic profiling strategy identify fractions compounds two TCM plants including Paederia scandens (Lour.) Merri. (Jishiteng Chinese) Millettia pachyloba Drake (Duyuteng Chinese), determine their mechanisms action. The extracts both were first fractionated 160 fractions. Label-free afforded by resonant waveguide grating biosensor microplate then acting at three different lines A431, A549 HT29. Mass spectroscopy-directed purification was purify compounds. NMR mass spectroscopy structures compounds, pharmacological assays elucidate Using this strategy, discovered that medicinal contain moderately high amount niacin, an agonist hydroxyl carboxylic acid receptor-2. Literature mining further suggests presence niacin may be responsible its antidyslipidemic effect found clinic studies. This study demonstrates potential identifying as well elucidating