Skip to main content

Table 2 Summary of HSC for drug discovery from TCM

From: High content screening for drug discovery from traditional Chinese medicine





Identified compound


eIF4E immunostaining in MEF cells.

mTOR signaling pathway affects cellular localization of eIF4E

Array-Scan® VTI HCS Reader (Thermo Scientific, USA)

Discover novel mTOR signaling pathway inhibitors

1,4-O-diferuloylsecoisola-riciresinol and PierreioneB


Nuclear translocation of NFATc1 in EGFP-NFATc1 U2OS cells

NFATc1 nuclear translocation affects osteoclast genesis and bone erosion

A confocal microscopy (Zeiss 710)

Screen for drug candidate for relevant diseases caused by osteoclast genesis

6-[10(Z)-heptadecenyl] salicylic acid from Syzygium tetragonum Wall


GFP-LC3-expressing HeLa cells

Autophagy induce the number of GFP-LC3 puncta rapidly increases

Opera HCS System, Columbus2.3 Software (Perkin-Elmer)

Screen for novel apoptosis and autophagy regulators

Neobractatin isobractatin from Garcinia bracteata


African green monkey kidney cell line BSC-1

Microtubules are essential for proper chromosome congression and separation

Automated microscope Axiovert 200 M (Carl Zeiss, Germany) data was analyzed using MetaMorph (Visitron, Germany)

Search for inhibitor of mitosis

Podoverine A from the plant Podophyllum versipelle Hance


Primary cortical neuron and dorsal root ganglion

Morphological change of synapse and the neurite outgrowth reflect neuron viability

ImageXpress Micro automated wide-field fluorescent microscope (Molecular Devices)

Discover potential neuroprotective drugs for paclitaxel-induced neurotoxicity

5-Hydroxydecanoate (5-HD)


Cell cycle or cytoskeletal stain on HeLa cells

Cell cycle and cytoskeleton is the markers for cell growth and stress

ImageXpress Micro inflorescent microscope (Molecular Devices)

Develop new tool to identify novel compound from large candidate libraries



β-catenin staining in the human MG-63 OS cell line

β-catenin is the reporter of WNT signaling

(TFM-680; Shanghai Tuming Optical Instrument Co., Ltd.)

Identify WNT signaling inhibitor for the treatment of osteosarcoma



The human prostate cancer cell line DU145

The position of lysosomes to the nucleus is a readout for lysosome anterograde trafficking

Cellomics Arrayscan (Thermo Fisher Scientific, Inc, Waltham, MA)

Screen for drugs that inhibit lysosome trafficking



Non-small cell lung cancer (NSCLC) cell lines NCI-H157 and NCI-H460

Cell death can be monitored by Anexin V/PI and DAPI staining

Kinetic Scan Reader (ThermoFisher Scientific, USA)

Identify the compounds to induce cell death

Ophiopogonin B from Radix Ophiopogon Japonicus


p-ERK and c-myc staining in MKP-1 overexpression cells

p-ERK and c-myc reflect MKP-1 activity

ArrayScan II (Cellomics, Pittsburgh, PA) S-Plus statistical Software package (Insightful, Inc., Seattle, WA)

Identify the inhibitor of MKP-1



Apoptotic markers staining

Apoptotic markers reflect cells death

KineticScan Reader (Cellomics Inc, Pittsburg, PA, USA)

To identify hepatoprotective compounds

Salvianolic acid B from Radix Salviae miltiorrhizae


Neurite imaging of SH-SY5Y cells

Neurite outgrowth is a marker for ROCK2 inhibition

In Cell Analyzer 2000 (GE, Healthcare) IN Cell Investigator

Discover ROCK2 inhibitors



LX-2 hepatic stellate cell proliferation

Hepatic stellate cell proliferation is a marker of liver fibrosis

Cellomics Arra yScan VTI HCS Reader Cellomics Cell Health Profiling BioApplication

Identify the active components of Danshen for anti-liver fibrosis

Salvianolic acid B, caffeic acid and rosmarinic acid


HepG2 cell

Apoptotic markers reflect cells death

Assay Scan VTI HCS Reader

Investigate the anti-proliferative and apoptotic effects of TMP



A549 cells

Nuclei morphology reflects cell growth and mitosis status

BeckmanCoulter/Q3DM EIDAQ100, Activity Base and XLfit software

Identify compound that induces mitotic arrest

A novel quinazolinone


Apoptotic markers staining on MCF7 cancer cells

Apoptotic markers reflect cells death

Eclipse TE2000-S microscope (Nikon, Tokyo, Japan)

Identify anti-cancer compounds



The NF-κB translocation staining in HT-29 cells

Nuclear translocation of NF-κB reflects inflammation

Cellomic ArrayScan HCS Reader (Thermo Scientific, USA)

Determine the anti-cancer and anti-inflammatory effects of PAB

Pseudolaric acid B (PAB)


The NF-κB translocation staining in A549 lung cancer cells

Nuclear translocation of NF-κB reflects inflammation

ArrayScan HCS system (Cellomics), ArrayScan II Data Acquisition and Data Viewer version 3.0 (Cellomics)

Identify the NF-κB inhibitor

Panduratin A


Rhodamine 123 staining of mitochondrial membrane potential in H9c2 cardiac muscle Cells

Mitochondrial membrane permeability change affect Rhodamine 123 signal

Leica DMI 6000 B (Leica Microsystems, Wetzlar, Germany) Cell Detection 1.0 Software

Identify compound to rescue mitochondrial membrane potential decrease

Salvianolic acid B, protocatechuic aldehyde, and tanshinone II A


HeLa cells stably expressing EGFP-LC3

GFP-LC3 is the marker for Autophagosome

In Cell 2000 system (GE Healthcare)

Find therapeutic method in chemotherapy of cancer by inhibiting autophagy

Dauricine and daurisoline


Stable HeLa cells overexpressing 3×Flag-TFEB

TFEB nuclear translocation indicates biogenesis of autophagy-lysosome pathway

Opera high content system; Perkin-Elmer

Identify activators of TFEB

Curcumin derivative termed C1