3-Hydroxy-3-methylglutaryl-coenzyme A reductase (HMGR) catalyzes the rate-limiting step in the mevalonate pathway. To elucidate the functions of HMGR in triterpene biosynthesis, Platycodon grandiflorum was transformed with a construct expressing Panax ginseng HMGR (PgHMGR). We used PCR analysis to select transformed hairy root lines and selected six lines for further investigation. Quantitative real-time PCR showed higher expression levels of HMGR and total platycoside levels (1.5-2.5-fold increase) in transgenic lines than in controls. Phytosterols levels were also 1.1-1.6-fold higher in transgenic lines than in controls. Among these lines, line T7 produced the highest level of total platycosides (1.60 ± 0.2 mg g(-1) dry weight) and α-spinasterol (1.78 ± 0.16 mg g(-1) dry weight). These results suggest that metabolic engineering of P. grandiflorum by Agrobacterium-mediated genetic transformation may enhance production of phytosterols and triterpenoids.