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This study compared the phytochemical composition and antioxidant activity of five different varieties of citrus physiological premature fruit drop (CPFD). Untargeted metabolomics was employed to identify variations in metabolites among different CPFDs, and their antilipidemic effects in vitro were assessed. The results showed that Citrus aurantium L. \u2018Daidai\u2019 physiological premature fruit drop (DDPD) and Citrus aurantium \u2018Changshan-huyou\u2019 physiological premature fruit drop (HYPD) exhibited higher levels of phytochemicals and stronger antioxidant activity. There were 97 differential metabolites identified in DDPD and HYPD, including phenylpropanoids, flavonoids, alkaloids, organic acids, terpenes, and lipids. Additionally, DDPD and HYPD demonstrated potential antilipidemic effects against oleic acid (OA)-induced steatosis in HepG2 hepatocytes and 3T3-L1 adipocytes. 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