They are hydroxylated, methylated, sulfated and glucuronized conjugates. In this study, we initiated the investigation of the metabolism and disposition of phenolic acid monomers from Danshen by dosing of single compound. By comparing the metabolism of different compounds, we found that methylation occurred firstly in liver, but further metabolism of methylated conjugates was inhibited except glucuronization. The double bond on the side chain in CA, FA and IFA was critical for the drug distribution in bile and enriches the type of metabolites. This study provided scientific basis for further studies on the measurement of the bioactivity of the metabolites and structure modification for drugs with better bioactivity and pharmacokinetic parameters..