APPLICATION OF IMAGE-BASED HIGH CONTENT ANALYSIS FOR THE SCREENING OF BIOACTIVE NATURAL PRODUCTS
Keywords:cell-based assay, high-content screening, automated microscope, imaging technology, bioactive natural products.
Each bioactive compound induces phenotypic changes in target cells that can be made visible by labelling selected molecules of the cells with fluorescent dyes and/or directly observed under the high-throughput microscope. A comparison of the cellular phenotype induced by a compound of interest with known cellular targets allows predicting its mode of action. Over the past 15 years, high-throughput microscopy has been one of the fastest growing fields in cell biology. When combined with automated multiparametric image and data analysis, it is referred to as high-content screening (HCS). Whilst HCS has been successfully applied to the bioactivity characterization of natural products, recent studies used automated microscopy and software to increase speed and to reduce subjective interpretation. In 2017, Institute of Natural Products Chemistry (INPC-VAST) has been equipped with a HCS platform (Olympus Scan^R) that designed for fully automated image acquisition and analysis of biological samples to visually inspect the cellular morphology induced by hit compounds as well as to discriminate from false positives. Accordingly, this short review covers the concepts of HCS and its application in screening of biologically active natural products whose molecular targets could be identified through such approaches.
Newman D. - Screening and identification of novel biologically active natural compounds. F1000Research, 6 (2017) doi: 10.12688/f1000research.11221.1.
Rahman A. U., M. I. Choudhary, and W. J. Thomson - Bioassay techniques for drug development, Harwood Academic Publishers, Australia, Amsterdam, The Netherlands, 2005.
Carlson E. E. - Natural products as chemical probes. ACS Chem Biol., 5 (2010) 639-653.
Fetz V., H. Prochnow, M. Bronstrup, and F. Sasse - Target identification by image analysis. Nat Prod Rep., 33 (2016) 655-667.
Usaj M. M., E. B. Styles, A. J. Verster, et al. - High-Content Screening for Quantitative Cell Biology. Trends in Cell Biol., 26 (2016) 598-611.
Gough A. H. and P. A. Johnston - Requirements, features, and performance of high content screening platforms. Method Molecular Biol., 356 (2007) 41-61.
Haney S. A. - High content screening: Science, Techniques and Application, John Wiley & Sons, Inc., Hoboken, New Jersey, 2008.
Lee S. and B. J. Howell - High-content screening: emerging hardware and software technologies. Method Enzymol., 414 (2006) 468–483.
Stockwell B. R. - Exploring biology with small organic molecules. Nature, 432 (2004) 846-854.
Dorval T., B. Chanrion, M. E. Cattin, and J. P. Stephan - Filling the drug discovery gap: is high-content screening the missing link? Curr Opin Pharmacol., 42 (2018) 40–45.
Giuliano K. A., R. L. DeBiasio, R. T. Dunlay, et al. - High content screening: a new approach to easing key bottlenecks in the drug discovery process. J Biomol Screen, 2 (1997) 249-259.
Taylor D. L., J. R. Haskins, and K. Giuliano - High Content Screening: A Powerful Approach to Systems Cell Biology and Drug Discovery in Methods in Molecular Biology, J.M. Walker, Editor^Editors, ©Humana Press, Inc., Totowa, New Jersey, 2007.
Zheng W., N. Thorne, and J. C. McKew - Phenotypic screens as a renewed approach for drug discovery. Drug Discov Today, 18 (2013) 1067-1073.
Auld D. andN. Thorne - Molecular sensors for the transcriptional and post-transcriptional assays, in Chemical Genomics, H. Fu, Editor^Editors, Cambridge University Press, UK, 2012, p. 173-197.
Moffat J. G., F. Vincent, J. A. Lee, et al. - Opportunities and challenges in phenotypic drug discovery: an industry perspective. Nature Rev Drug Discov., 16 (2017) 531-543.
Gasparri F., M. Mariani, F. Sola, and A. Galvani - Quantification of the proliferation index of human dermal fibroblast cultures with the ArrayScan high content screening reader. J Biomol Screen., 9 (2004) 232-243.
Vogt A, K. A. Cooley, M. Brisson, et al. - Cell-active dual specificity phosphatase inhibitors identified by high-content screening. Chem Biol., 10 (2003) 733-742.
Keefer S. andJ. Zock - Approaching high content screening and analysis: Practical advice for users, in High content screening: Science, Techniques and Application, S.A. Haney, Editor^Editors, John Wiley & Sons, Inc., Hoboken, New Jersey, 2008, p. 3-24.
Horvath P., N. Aulner, M. Bickle, et al. - Screening out the irrelevant cell-based models of disease. Nature Rev., 15 (2016) 751-769.
Boutros M., F. Heigwer, and C. Laufer - Microscopy-based high-content screening. Cell, 163 (2015) 1314-1325.
Conway B., L. Minor, J. Xu, et al. - Quantitation of G-protein coupled receptor internalization using G-protein coupled receptor-green fluorescent protein conjugates with the ArrayScan high-content screening system. J Biomol Screen., 4 (1999) 75-86.
Ding G., P. Fischer, R. Boltz, et al. - Characterization and quantitation of NF-KB nuclear translocation induced by interleukin-1 and tumor necrosis factor-α: development and use of a hight capacity fluorescence cytometric system. J Biol Chem., 273 (1998) 28897-28905.
Young D. W., A. Bender, J. Hoyt, et al. - Integrating high-content screening and ligand-target prediction to identify mechanism of action. Nat. Chem. Biol., 4 (2008) 59-68.
Caie P. D., R. E. Walls, A. Ingleston-Orme, et al. - High-content phenotypic profiling of drug response signatures across distinct cancer cells. Mol Cancer Ther., 9 (2010) 1913-1926.
Perlman Z. E., M. D. Slack, Y. Feng, et al. - Multidimensional drug profiling by automated microscopy. Science, 306 (2004) 1194-1198.
Marks K. M., E. S. Park, A. Arefolov, et al. - The selectivity of Austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes. J Nat Prod., 74 (2011) 567-573.
Wang D., Y. Feng, M. Murtaza, et al. - A Grand challenge: Unbiased phenotypic function of metabolites from Jaspis splendens against Parkinson's disease. J Nat Prod., 79 (2016) 353-361.
Vial M. L., D. Zencak, T. Grkovic, et al. - A grand challenge: Phenotypic profiling of a natural product library on Parkinson's patient-derived cells. J Nat Prod., 79 (2016) 1982-1989.
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