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Citrus reticulata "Chachi" (CRC) leaves contain abundant flavonoids, indicating that they possess good nutritional/pharmacological research and development potential. This study aims to explore chemical antioxidant quality markers based on the spectrum-effect relationship and quality control strategy of CRC leaves. The ultrahigh performance liquid chromatography (UPLC) system was used to establish chromatographic fingerprints of Citrus reticulata "Chachi" leaves. Simultaneously, they were evaluated by using similarity analysis (SA), hierarchical cluster analysis (HCA), and principal component analysis (PCA). Afterwards, the DPPH assay was adopted to study the antioxidant effects. The spectrum-effect relationship between UPLC fingerprints and DPPH radical-scavenging activities was studied with grey relational analysis (GRA). Analysis results indicated that there were twenty-one common peaks of fourteen batches of CRC leaves which were from different regions of Guangdong province, and their similarities ranged from 0.648 to 0.997. HCA results showed that fourteen batches of samples of CRC leaves could be divided into six classes at Euclidean distance of 5. The results from GRA showed that tangeretin and hesperidin were the main flavonoids responsible for the antioxidant activity in CRC leaves. In conclusion, this research established a chromatographic analysis method suitable for CRC leaves and demonstrated that chromatographic fingerprints analysis combined with the antioxidant activity could be used to evaluate the material basis of CRC leaves and may provide a reference to establish a quality standard. [ABSTRACT FROM AUTHOR]