TABLE 3

Summary of the effects of TNF-α and IL-6 on human hepatic transporter expression a

Transporter
TNF-α
IL-6
mRNA
Protein
Activity
mRNA
Protein
Activity
MDR1 ↔b ↔ N.D.c ↓d ↔ N.D.
BSEP ↓ N.D. N.D. ↔ N.D. N.D.
MRP2 ↔ ↔ N.D. ↓ ↓ N.D.
MRP3 ↔ ↑e N.D. ↔ ↑ N.D.
MRP4 ↔ N.D. N.D. ↔ N.D. N.D.
BCRP ↔ ↑ N.D. ↓ ↓ N.D.
NTCP ↓ ↓ ↓ ↓ ↓ ↓
OATP2B1 ↓ N.D. ↓f ↓ N.D. ↓f
OATP1B1 ↓ ↓ ↓f ↓ ↓ ↓f
OATP1B3 ↓ N.D. ↓f ↓ N.D. ↓f
OCT1 ↓ N.D. ↓ ↓ N.D. ↓
OAT2
↓
N.D.
N.D.
↓
N.D.
N.D.

  • ↵ a Human hepatocytes were exposed to cytokines for 48 h.

  • ↵ b ↔, no change.

  • ↵ c N.D., not done.

  • ↵ d ↓, significant repression.

  • ↵ e ↑, significant induction.

  • ↵ f Activity was measured used the pan-OATP substrate estrone-3 sulfate and therefore may not reflect specific OATP2B1-, OATP1B1-, or OATP1B3-mediated transport.