Objective: To develop a fluorescence imaging-based novel system for quick screening of antitumor compounds in vitro.
Methods: The antitumor activity of 26 components from Lindera aggregate were determined by relative number of viable cell labelled with fluorescein diacetate (FDA) in multiwell plates after exposure to these 26 different components. Then, the linearity and precision of this method were validated. The structures of active compounds in components with strong antitumor activity were deduced by LC/MS.
Results: The linearity of this method for cells stained with FDA was validated (r² = 0.9858) in the range of 0-10⁴ cells per well, and the in-plate precision was 9.41 %. Two of 26 components from Lindera aggregate showed significant inhibition effect on proliferation of HepG2 cells (inhibition rate >90%).
Conclusion: This proposed rapid and reliable approach can be used for screening compounds with antitumor activity from Traditional Chinese Medicine in vitro. The major active compound of Lindera aggregate was putatively identified as norboldine by LC/MS analysis.