Determination of P-glycoprotein ATPase activity using luciferase

Tamihide Matsunaga, Eiji Kose, Sachiyo Yasuda, Hirohiko Ise, Uichi Ikeda, Shigeru Ohmori

Research output: Contribution to journalArticlepeer-review

11 Citations (Scopus)


We investigated whether P-glycoprotein (P-gp) ATPase activity of Caco-2 cell membranes could be estimated by measuring consumption of ATP using luciferin-luciferase reaction, and whether the results would be useful for assessment of the interactions between P-gp and drugs. The vanadate-sensitive ATPase activity of Caco-2 cell membranes was measured rapidly with high sensitivity using luciferin-luciferase reaction. Cyclosporin A, verapamil, digoxin and quinidine stimulated the ATPase activity concentration-dependently with Km values of 5.3, 0.9, 1.2 and 4.1 μM, respectively. These values except for digoxin were comparable with previous reports. The ATPase activity and P-gp mRNA expression in Caco-2 cells were induced by all-trans-retinoic acid, digoxin and levothyroxine, but not dexamethasone or rifampicin. This method was useful to assess interactions with P-gp and drugs, and was used to elucidate the mechanisms of interaction of levothyroxine and digoxin.

Original languageEnglish
Pages (from-to)560-564
Number of pages5
JournalBiological and Pharmaceutical Bulletin
Issue number3
Publication statusPublished - Mar 2006
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science


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