Glyoxalase activity during differentiation of human leukaemia cells in vitro

Leuk Res. 1987;11(12):1141-8. doi: 10.1016/0145-2126(87)90169-x.


The activities of glyoxalase I and glyoxalase II were determined in human promyelocytic leukaemia HL60 and erythroleukaemia K562 cells in culture. The activity of glyoxalase I is ca 10-20 times greater than the activity of glyoxalase II under assay conditions. When HL60 and K562 cell lines were incubated with N-methylformamide and 8-carbamoyl-3-methylimidazo-[5,1-d]-1,2,3,5-tetrazin-4(3H)-one (CCRG 81045), substantial changes in the glyoxalase activities were induced. With HL60 cells, treatment with N-methylformamide and CCRG 81045, both of which induce functional differentiation of this cell line, there is a dose-dependent decrease in glyoxalase I activity and a concomitant dose-dependent increase in glyoxalase II activity, both of which are directly proportional to the number of differentiated cells. With K562 cells, N-methylformamide and CCRG 81045 induce an increase in both glyoxalase I and glyoxalase II activities, although only CCRG 81045 induces the appearance of haemoglobin producing cells. N-Methylformamide and CCRG 81045 do not activate or inhibit the activities of glyoxalase I and glyoxalase II from HL60 and K562 cells when studied in cell-free systems. The changes in the glyoxalase activities of HL60 and K562 cells during the incubations therefore appear to be due to alteration in the synthesis and/or regulatory modification of the glyoxalase enzymes induced by N-methylformamide and CCRG 81045. Despite the apparent disparity of the effect of differentiation on the glyoxalase system in the two cell lines, in both cases the glyoxalase I/glyoxalase II activity ratio decreases with the appearance of differentiated cells. Since glyoxalase II catalyses the rate-determining step in the glyoxalase system, this suggests that immature cells have an impaired capacity to metabolise S-D-lactoylglutathione.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Differentiation
  • Dacarbazine* / analogs & derivatives*
  • Formamides / pharmacology
  • Humans
  • Imidazoles / pharmacology
  • In Vitro Techniques
  • Lactoylglutathione Lyase / metabolism*
  • Leukemia, Erythroblastic, Acute / enzymology
  • Leukemia, Myeloid, Acute / enzymology*
  • Lyases / metabolism*
  • Temozolomide
  • Thiolester Hydrolases / metabolism*
  • Tumor Cells, Cultured / enzymology


  • Formamides
  • Imidazoles
  • Dacarbazine
  • Thiolester Hydrolases
  • hydroxyacylglutathione hydrolase
  • Lyases
  • Lactoylglutathione Lyase
  • methylformamide
  • Temozolomide