Organic anion transporting polypeptide-C mediates arsenic uptake in HEK-293 cells

J Biomed Sci. 2006 Jul;13(4):525-33. doi: 10.1007/s11373-006-9071-0. Epub 2006 Feb 15.


Arsenic is an established human carcinogen. The role of aquaglyroporins (AQPs) in arsenic disposition was recently identified. In order to examine whether organic anion transporting polypeptide-C (OATP-C) also plays a role in arsenic transport, OATP-C cDNA was transfected into cells of a human embryonic kidney cell line (HEK-293). Transfection increased uptake of the model OATP-C substrate, estradiol-17beta-D-glucuronide, by 10-fold. In addition, we measured uptake and cytotoxicity of arsenate, arsenite, monomethylarsonate(MMA(V)), and dimethylarsinate (DMA(V)). Transfection of OATP-C increased uptake and cytotoxicity of arsenate and arsenite, but not of MMA(V) or DMA(V). Rifampin and taurocholic acid (a substrate of OATP-C) reversed the increased toxicity of arsenate and arsenite seen in OATP-C-transfected cells. The increase in uptake of inorganic arsenic was not as great as that of estradiol-17beta-D-glucuronide. Our results suggest that OATP-C can transport inorganic arsenic in a (GSH)-dependent manner. However, this may not be the major pathway for arsenic transport.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arsenates / metabolism
  • Arsenic / metabolism*
  • Arsenites / metabolism
  • Biological Transport, Active / physiology
  • Cacodylic Acid / metabolism
  • Cell Line
  • DNA Primers
  • DNA, Complementary / genetics
  • Estradiol / analogs & derivatives
  • Estradiol / metabolism
  • Humans
  • Immunoblotting
  • Lethal Dose 50
  • Liver-Specific Organic Anion Transporter 1 / genetics
  • Liver-Specific Organic Anion Transporter 1 / metabolism*
  • Reverse Transcriptase Polymerase Chain Reaction
  • Rifampin
  • Taurocholic Acid
  • Tetrazolium Salts
  • Thiazoles
  • Toxicity Tests
  • Transfection


  • Arsenates
  • Arsenites
  • DNA Primers
  • DNA, Complementary
  • Liver-Specific Organic Anion Transporter 1
  • Tetrazolium Salts
  • Thiazoles
  • estradiol-17 beta-glucuronide
  • Estradiol
  • Taurocholic Acid
  • Cacodylic Acid
  • thiazolyl blue
  • arsenite
  • Arsenic
  • arsenic acid
  • Rifampin