millepachine

Millepachine is a **natural chalcone compound** derived from *Millettia pachycarpa* Benth, exhibiting **antitumor activity primarily via inhibition of topoisomerase II and tubulin polymerization**.[1][2] It operates through dual mechanisms: (1) it **irreversibly inhibits the colchicine-binding site of β-tubulin**, disrupting microtubule assembly and inducing G2/M cell cycle arrest; (2) it **inhibits topoisomerase II**, stabilizing the topoisomerase II-DNA cleavable complex, causing DNA double-strand breaks and apoptosis in tumor cells. Millepachine has demonstrated activity against multiple cancer cell lines, including ovarian and hepatocellular carcinoma, and can overcome multidrug resistance in in vitro models.[1][2][3][4] Importantly, **NF-κB pathway activation** occurs following DNA damage induced by millepachine, contributing to pro-apoptotic effects in tumor cells.[1] Amino acid prodrugs and other derivatives of millepachine have been synthesized to enhance its solubility and antitumor potency.[3][4]

Other names

MIL