Simultaneously, the development of molecular biology system attributes to the rapid growth of biological probes and fluorophores. Fluorescence microscopy emerged as a robust tool substituted for conventional optical equipment, which can analyze spatiotemporal information in biology to uncover the mysterious veils of cellular events. The advancement of optical instruments greatly accelerated the process of modern biology and the drug discovery industry. Meanwhile, this article also discusses the advantages and limitations of HSC technology in drug discovery from TCM libraries. The review introduces the concept and principle of high content screening, lists and compares the currently used HCS instruments, and summarizes the examples from ours and others research work which applied HCS in TCM-derived compounds screening. The advent of high content screening technology has absolutely contributed to a breakthrough in compounds discovery and influenced the evolution of technology in screening field. To dissect the mystery of TCM, modern technologies such as omics approaches (proteomics, genomics, metabolomics) and drug screening technologies (high through-put screening, high content screening and virtual screening) have been widely applied to either identify the drug target of TCM or identify the active component with certain bio-activity. It has been valued as the renewable source for the discovery of novel drugs, owing to its long-term proved efficacy in human diseases and abundant biologically active components pools. Traditional Chinese medicine (TCM) represents the crystallization of Chinese wisdom and civilization.
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