In order to identify the bioactive components in Pu-erh tearesponsible for its hypolipidaemic effect, the aqueous extractand its fractions were analysed for regulation of transcription factors involved in lipid metabolism using reporter geneassays. Bioactive compounds from the fraction that had thegreatest hypolipidaemic potential were identified using MS, NMRand UPLC-MS/MS. Identifying the bioactive compounds of Puerh tea responsible for the reported hypolipidaemic propertiescould provide a scientific foundation for its medicinal value.