This invention relates to the use of high isoflavon, coumarin, and derivatives thereof in preparing cell nucleus receptor regulator and DPP4 inhibitor, wherein the high isoflavon derivatives are extracted from Polygonatum odoratum, and coumarin derivatives are extracted from Cnidium monnieri. In the present invention, the high isoflavon, coumarin, and derivatives thereof are used as androgen receptor (AR) antagonists, peroxisome proliferator activated receptor [gamma] (PPAR[gamma]) agonist, dipeptidyl peptidase 4 (DPP4) inhibitor and farnesoid x receptor (FXR) agonist and can be applied to preparing drugs for curing metabolism, liver, androgen related diseases or Alzheimers disease.本發明係關於一種高異黃酮類、香豆素及其衍生物作為製備細胞核受器調節劑及DPP4抑制劑之用途,其中高異黃酮類衍生物係萃取自玉竹,香豆素衍生物係萃取自蛇床子。本發明中,該高異黃酮類、香豆素及其衍生物作為雄性激素受體(AR)拮抗劑、過氧化體增生劑活化受體γ(PPARγ)促效劑、雙基胜肽酶-4(DPP4)抑制劑及膽酸受體(FXR)促效劑之用途,並可應用於製備治療與代謝、肝臟、雄性激素疾病或阿茲海默症藥物之用途。