Oridonin, an ent-kaurane diterpenoid, is found in the Chinese herb Rabdosia rubescens and some related species, and has various biological activities such as anti-tumor, anti-microbial, anti-inflammatory, and so on.This review provides an overview of the multifunctional effects of the structural modification of oridonin since 2000, suggesting that it may be effective choice for improving pharmacological activities.