Tripterygium wilfordii has complex chemical components. To study and summarize the advance in studies on the anti-inflammatory and immunoregulatory activities and toxicology of known monomers of T. wilfordii, the pertinent literatures related to the studies on the pharmacology, toxicology and pharmacokinetics of T. wilfordii over past 30 years were searched. According to the findings, more than ten anti-inflammatory and immunoregulatory monomers were found in T. wilfordii. The pharmacology and toxicology of wilforidine, triptolidenol, triptonide, demethylzeylasteral shall be further studied.