High Throughput Screening for Colorectal Cancer Specific Compounds

Abstract

The development of new anti-cancer therapeutic agents is necessary to improve antitumor efficacy and reduce toxicities. Here we report using a systematic anticancer drug screening approach we developed previously, to concurrently screen colon and glioma cancer cell lines for 2000 compounds with known bioactivity and 1920 compounds with unknown activity. The hits specific to each tumor cell line were then selected, and further tested with the same cells transfected with EGFP (Enhanced Green Fluorescent Protein) alone. By comparing the percentage of signal reduction from the same cells transfected with the sensor-conjugated reporter system; hits preferably causing apoptosis were identified. Among the known lead compounds, many cardiac glycosides used as cardiotonic drugs were found to effectively and specifically kill colon cancer cells, while statins (hypolipidemic agents) used as cholesterol lowering drugs were relatively more effective in killing glioma cells.

Anticancer Potential of Ficus religiosa (Linn) Against Human Breast Cancer Cell Line MDA-MB-231 and its Phytoconstituents by HR-LCMS

“…Convallatoxin is natural glycoside found in many organisms, including plants. This substance is reported as inhibitor of cancer cell growth [24]. It is also reported as effective anti-proliferative agent against some cancer types [25,26].…”

Improving the power of drug toxicity measurements by quantitative nuclei imaging

“…Optimization the consistency between NADH or ATP-based assays, measurements of cell area or LIVE/DEAD assays was addressed by numerous studies, providing either protocol optimizations, metric selection or method combination [15][16][17][18] . Advances in microscopy and image processing algorithms led to new high-content screening methods using fluorescence microscopy 19 , that also allow viable cells counting [20][21][22][23][24][25] . Microscopy provides the most direct approach to measure cell proliferation and drug toxicity 20 , as it does not require extensive processing of cells, such as trypsinization and cell lysis, highly customizable by the use of fluorescent stains and proteins which allows measurement of cell cycle and cell death 26 , protein activity [27][28][29] , cell differentiation 30 , metabolites levels and cellular morphology 31 .…”