The invention discloses an application of a
piperlongumine / ligustrazine derivative in vascular
restenosis diseases, the derivative is PL-Lig-11, and the
structural formula of the derivative is shown as a formula I. The invention further discloses a preparation method of the
piperlongumine / ligustrazine derivative. The derivative effectively blocks the transformation of VSMC from a contraction
phenotype to a proliferation
phenotype through targeted inhibition of a key
signal protein RhoGDI3, and significantly inhibits the abnormal proliferation and migration ability of VSMC, thereby fundamentally inhibiting the
pathological process of NIH. Compared with parent compounds of
piperlongumine and ligustrazine, the PL-Lig-11 shows higher anti-proliferative activity and higher selectivity, and the expected
cytotoxicity is lower than that of clinically common
chemotherapy drugs such as rapamycin and
paclitaxel. The
medicine can be used for preventing and treating
vascular stenosis diseases caused by
restenosis after PCI (
percutaneous coronary intervention), hypertensive vascular remodeling, atherosclerotic plaque progress and other operations or injuries, and a candidate
medicine with a novel action mechanism and good safety is provided for clinic.