Sambutoxin is a 4-hydroxy-2-pyridone fungal metabolite initially produced by Fusarium samucinum isolated from rotted potato tubers by Kim and co-workers, Seoul National University, Korea in 1995. Sambutoxin is a potent and selective inhibitor of mitochondrial respiration. Sambutoxin inhibits platelet aggregation, decreases platelet activating factor-induced disaggregation time in a dose-dependent manner and decreases thrombin and arachidonic acid-induced ATP release. Sambutoxin has remarkable antiproliferative effects, inhibiting ROS production and inducing G2/M arrest and apoptosis by activating the mitochondrial apoptosis pathway.