Salvicine is a novel diterpenoid quinone compound obtained by structural modi-fication of a natural product lead isolated from a Chinese herb with potent growthinhibitory activity against a wide spectrum of human tumor cells in vitro and inmice bearing human tumor xenografts. Salvicine has also been found to have aprofound cytotoxic effect on multidrug-resisitant (MDR) cells. Moreover, Salvicinesignificantly reduced the lung metastatic foci of MDA-MB-435 orthotopicxenograft. Recent studies demonstrated that salvicine is a novel non-intercalativetopoisomerase II (Topo II) poison by binding to the ATPase domain, promotingDNA-Topo II binding and inhibiting Topo II-mediated DNA relegation and ATPhydrolysis. Further studies have indicated that salcivine-elicited ROS plays acentral role in salvicine-induced cellular response including Topo II inhibition,DNA damage, circumventing MDR and tumor cell adhesion inhibition. Salvicine is a novel diterpenoid quinone compound obtained by structural modi-fication of a natural product lead isolated from a Chinese herb with potent growth ofhibitory activity against a wide spectrum of human tumor cells in vitro and inmice bearing human tumor xenografts. Salvicine has also been to have aprofound cytotoxic effect on multidrug-resisitant (MDR) cells. Moreover, Salvicinesignificantly reduced the lung metastatic foci of MDA-MB-435orthotopicxenograft. Recent studies have demonstrated that salvicine is a novel non-intercalativetopoisomerase II (Topo II) poison by binding to the ATPase domain, promoting DNA-Topo II binding and inhibiting Topo II-mediated DNA relegation and ATPhydrolysis. Further studies have indicated that salcivine-elicited ROS plays acentral role in salvicine-induced cellular response including Topo II inhibition, DNA damage, circumventing MDR and tumor cell adhesion inhibition.