Abstract
Traditional Chinese medicines (TCMs) have been used in clinic for thousands of years. These TCMs display reliable therapeutic efficacy and are important resources for drug discovery. Elucidating mechanisms of action (MOAs) of active compounds is essential to the development and clarification of TCMs. As one of new generation pharmacological assays, label-free cell phenotypic assays can provide a holistic view of ligand–receptor interactions in living cells with wide pathway coverage, high throughput, and high temporal resolution, thus enabling effectively elucidating the MOAs of TCMs. For identifying active compounds from TCMs, effective separation and purification methods are indispensable since TCMs usually contain hundreds or even thousands of compounds. This chapter provides a general protocol of preparative techniques and label-free cell phenotypic assays to determine the target engagement of active TCM fractions and compounds.
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6 Glossary
- TCM
-
Traditional Chinese medicine
- MOA
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Mechanism of action
- FDA
-
Food and Drug Administration
- HPLC
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High-performance liquid chromatography
- 2D-LC
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Two-dimensional liquid chromatography
- RPLC
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Reversed-phase liquid chromatography
- HILIC
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Hydrophilic interaction liquid chromatography
- IEX
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Ion-exchange chromatography
- FMCs
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Fine multicomponents
- ADME/Tox
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Absorption, distribution, metabolism, excretion and toxicity
- RWG
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Resonant waveguide grating
- DMR
-
Dynamic mass redistribution
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Liang, X., Wang, J., Zhang, X., Fang, Y. (2015). Label-Free Cell Phenotypic Identification of Active Compounds in Traditional Chinese Medicines. In: Fang, Y. (eds) Label-Free Biosensor Methods in Drug Discovery. Methods in Pharmacology and Toxicology. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-2617-6_13
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