Piperlongumine (natural)

Piperlongumine is a cell-permeable, orally bioavailable natural product isolated from the plant species, Piper longum L, which selectively induces cell death in cancer cells that express both wild-type and mutant p53 but not in primary normal cells and non-transformed immortalized cells. Piperlongumine enhances wild-type p53 and PUMA expression, and inhibits the expression of several pro-survival proteins, including BCL2, surviving, and XIAP, in various types of cancer cells, but not in normal cells. It induces ROS and apoptosis in several human cancer cells (EJ, MDA-MB-231, U2OS and MDA-MB-435), possibly through interaction with oxidative stress responders such as GSTP1 and CBR1. Additionally, it exhibits anti-tumour effects and inhibits the formation of blood vessels in xenograft-tumour mice and inhibits tumor growth and their associated metastases in a MMTV-PyVT breast cancer transgenic mouse model (2.4mg/kg, daily for two weeks, i.p.). Piperlongumine possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, anticancer, antiplatelet, anxiolytic, antidepressant and antidiabetic activities.