APPLICATION OF IMAGE-BASED HIGH CONTENT ANALYSIS FOR THE SCREENING OF 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