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Table 2 Summary of HSC for drug discovery from TCM

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

Models Principle Platform Purpose Identified compound Refs.
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 [31]
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 [32]
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 [33]
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 [34]
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) [35]
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 Quinocinnolinomycins [36]
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 Resveratrol [37]
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 Niclosamide [38]
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 [39]
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 Sanguinarine [40]
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 [41]
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 BIPM [42]
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 [43]
HepG2 cell Apoptotic markers reflect cells death Assay Scan VTI HCS Reader Investigate the anti-proliferative and apoptotic effects of TMP Tetramethylpyrazine [44]
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 [45]
Apoptotic markers staining on MCF7 cancer cells Apoptotic markers reflect cells death Eclipse TE2000-S microscope (Nikon, Tokyo, Japan) Identify anti-cancer compounds Koenimbin [46]
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) [47]
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 [48]
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 [49]
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 [50]
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 [51]