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Aim: To establish and validate an in vitro system to screen drug inducers of CYP3A4,CYP2B6, and CYP2C9 and study hPXR (human pregnane X receptors)-mediated transcriptional regulation of CYP3A4, CYP2B6, and CYP2C9 by a traditional Chinese medicine helicid and its two metabolites.