Abstract: Plant-derived natural products with unique skeletons and bioactivities provide considerable drug leads and candidates，thereby constituting a hotspot in the field of drug discovery.This article reviews recent progress on bioactivities of plant-derived macrocyclic diterpenoid compounds，focusing on their pharmaceutical potentials in combating cancers，AIDS as well as other serious diseases.The possible obstacles and promising advantages involved in the development and application of plant-derived macrocyclic diterpenoids as pharmaceutical agents are also discussed.