Phytochemical investigation of the leaf of Ilex centrochinensis led to the isolation and characterization of four flavans, one flavanone (5), and one flavone (6), including a new compound whose structure was elucidated as (2S)-5,3',4'-trihydroxy-7-methoxyflavan (1) and a new natural product whose structure was elucidated as (2S)-5-hydroxy-7,3',4'-trimethoxyflavan (4) on the basis of spectroscopic methods especially 1D and 2D NMR, CD, and mass spectral analyses. Compounds 1 and 4 exhibited weak cytotoxic activity against Huh7 cell line and no cytotoxic activity against Caco-2 cell line.