An improved synthesis of piperlongumine and the preliminary imaging evaluation on tumor targeting

Piperlongumine is a natural product that exhibited anti-cancer effect for various tumor types. For in vivo metabolism, I-125 labeled piperlongumine ( 125 I-PL) was expelled by kidney soon post injection, so tumor targeting was achieved at 30 min post injection; 125 I-PL reached a 2.33 ± 0.51 ratio of tumor/liver in SMMC-7721 (HCC tumor cells line) subcutaneous tumor BALB/c nude mice, but a negative uptake was observed in MHCC97h subcutaneous tumor mice. Therefore, piperlongumine was conveniently synthesized via amidation approach, and the fast clearance and tumor targeting were manifested for the first time.