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BACKGROUND AND PURPOSE An ATP‐binding cassette (ABC) transporter, breast cancer resistance protein (BCRP)/ABCG2, limits oral bioavailability of sulphasalazine. Here we examined the effect of curcumin, the principal curcuminoid of turmeric, on oral bioavailability of microdoses and therapeutic doses of sulphasalazine in humans.

EXPERIMENTAL APPROACH Effects of curcumin were measured on the ATP‐dependent sulphasalazine uptake by hBCRP‐expressing membrane vesicles and on oral bioavailability of sulphasalazine in wild‐type and Bcrp(–/–) mice. Eight healthy Japanese subjects received an oral dose of sulphasalazine suspension (100 µg) or tablets (2 g) alone or after curcumin tablets (2 g). Uptake of sulphasalazine was studied in HEK293 cells transfected with the influx transporter (OATP)2B1.

KEY RESULTS Curcumin was a potent hBCRP inhibitor in vitro (K_i 0.70 ± 0.41 µM …