The present invention belongs to the field of natural medicines and medicinal chemistry, and relates to novel esterified amino acid derivatives of triptolide of general formula I and general formula II or pharmaceutically acceptable adducts, complexes, salts, and catabolites and metabolites thereof, preparation methods of these compounds, pharmaceutical compositions comprising the compound, and uses thereof in preparing drugs against tumors, immune diseases, or diseases related to abnormal expression of XPB or Pol II or oncogene c-myc.