The present invention belongs to the field of natural pharmaceuticals and pharmaceutical chemistry, and relates to novel esterified amino acid derivatives of triptolide of general formulae I and II or a pharmaceutically acceptable adduct, complex, salt and catabolites and metabolites thereof, and a method for preparing these compounds, a pharmaceutical composition containing the compound, and a use thereof in the preparation of drugs for against tumours, immunological diseases, or diseases associated with abnormal expressions of XPB or Pol II or oncogene c-myc.