sappanchalcone

Sappanchalcone is a natural chalcone derivative, primarily isolated from the heartwood of *Caesalpinia sappan*, that is being investigated for its potent anticancer properties against non-small cell lung cancer (NSCLC). Its mechanism of action is multifaceted, involving the induction of oxidative stress and the accumulation of reactive oxygen species (ROS), which leads to DNA damage and the activation of the DNA damage response. Sappanchalcone also perturbs ion homeostasis by downregulating the mechanosensitive ion channel PIEZO1 and inducing intracellular calcium elevation. This calcium signaling triggers endoplasmic reticulum (ER) stress pathways, specifically through the phosphorylation and activation of IRE1α and PERK. These combined effects result in the upregulation of P21 and GADD45α, the suppression of the CDK1/Cyclin B1 complex, and the induction of G2/M phase cell cycle arrest and apoptosis in cancer cells.

Other names

SC