ABSTRACT:The possibility of interactions between natural products/supplements and conventional prescription medicines is one of the most important issues in pharmacotherapeutic safety. Recently, we reported that some terpenoids such as (R)-(؉)-citronellal and glycyrrhetic acid, which are present in herbal medicines, can act as inhibitors of P-glycoprotein (MDR1/ABCB1). In the present study, the effects of seven terpenoids on multidrug resistance-associated protein 2 (MRP2/ABCC2) and breast cancer resistance protein (BCRP/ ABCG2)-mediated transport were investigated in vitro. Membrane vesicles were prepared from MRP2 cDNA transfected Sf9 cells derived from pupal ovarian tissue of Spodoptera frugiperda, a fall armyworm, and BCRP cDNA transfected LLC-PK1 cells derived from porcine kidney. MRP2-or BCRP-mediated efflux transport was measured as ATP-dependent accumulation of [ 3 H]estradiol
17--D-glucuronide (E 2 17G) into membrane vesicles collected by a rapid filtration technique. The effects of (R)-(؉)-citronellal, (S)-(؊)--citronellol, ␣-terpinene, terpinolene, (؊)--pinene