ANTI-CANCER AGENT COMPRISING 4-HEXADECANOYL-1,1-DIMETHYL-PIPERAZIN-1-IUM IODIDE

摘要

Disclosed herein is an anticancer agent comprising 4- hexadecanoyl-1,1-dimethyl-piperazin-1-ium iodide. The piperazine derivative effectively inhibits the proliferation of various cancer cells(in vitro), and statistically significantly reduces tumor size and tumor weight in nude mice xenografted with human gastric carcinoma NUGC-3 cells when administered intraperitoneally to the mice (in vivo). Also, the piperazine derivative blocks Ras signaling by downregulating farnesyltransferase, thereby inhibiting cell proliferation, and activates RhoB to thus upregulate JNKl/ JNK2, which causes the dysregulation of signaling via the mitochondria and increase the phosphorylation of Bcl-2, involved in cell survival, thereby inducing apoptosis within cells. Since the piperazine derivative inhibits the growth of tumor cells and induces apoptosis, it is useful in the treatment of various types of cancer.