Tripterygium wilfordli Hook is a traditional insecticidal plant in China. We reviewed the bioactivities of the extracts from the plant in five aspects insecticidal activity, antifeedant activity, insect narcosis, development and growth inhibition, population inhibition effects. The major active ompounds include six alkaloids, (wilfordine, wilforine, wilfortrine, wilforgine, wilforzine, euonine) and two diterpenoids (triptolide and triptonide) the alkaloids could target the nerve system and the midgut cells of insects. It was predicted Na^+, K⁺-ATPase was one of the targets of triptolide. The field efficacy incontrolling insect pests was also reviewed.