Definition

A short-chain diterpene ester isolated from the seed of Fontainea picrosperma, with potential antineoplastic activity. Upon intratumoral administration, tigilanol tiglate disrupts mitochondrial functioning and induces mitochondrial swelling, which leads to oncolysis of tumor cells that are in direct contact of the agent. In addition, tigilanol tiglate activates protein kinase C (PKC) signaling cascade, which leads to an acute inflammatory response. This results in hypoxia and activates innate immune cells including neutrophils and macrophages, thereby further killing tumor cells. The activation of the beta-II isoform of PKC (PKC beta II) also increases tumor vasculature permeability, which leads to the destruction of tumor vasculature.