Chemosensitizing interactions of clofazimine and B669 with human K562 erythroleukaemia cells with varying levels of expression of P-glycoprotein

Cancer Lett. 1996 Jan 19;99(1):73-8. doi: 10.1016/0304-3835(95)04039-0.

Abstract

Differential expression of a permeability glycoprotein (P-gp) in human myeloleukaemia K562 cells grown in the presence of the anti-cancer drug, doxorubicin, gave rise to subclones with varying degrees of resistance to other anti-tumour drugs such as vinblastine and daunorubicin. Subclones K562/MMB, MMG and MMF were produced from the parental (K562/P) cell line via limiting dilution and their MDR nature confirmed with flow cytometry using an MRK 16 monoclonal antibody directed at a surface epitope of the P-gp pump. The pattern of increasing P-gp expression in the series K562/P, MMF, MMG and MMB was paralleled by increasing resistance to vinblastine and daunorubicin. When the subclones were pre-incubated with the chemosensitizing drugs clofazimine and B669, a pattern of increasing reversal of resistance to vinblastine and daunorubicin was seen in the series K562/P, MMF, MMG and MMB.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / biosynthesis
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents, Phytogenic / pharmacokinetics
  • Clofazimine / analogs & derivatives*
  • Clofazimine / pharmacology*
  • Drug Interactions
  • Drug Resistance, Multiple
  • Drug Screening Assays, Antitumor
  • Ethacrynic Acid / pharmacology
  • Flow Cytometry
  • Genistein
  • Humans
  • Isoflavones / pharmacology
  • Leukemia, Erythroblastic, Acute / drug therapy*
  • Leukemia, Erythroblastic, Acute / metabolism*
  • Tritium
  • Tumor Cells, Cultured / drug effects
  • Vinblastine / pharmacokinetics

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Antineoplastic Agents
  • Antineoplastic Agents, Phytogenic
  • Isoflavones
  • Tritium
  • Vinblastine
  • B 669
  • Clofazimine
  • Genistein
  • Ethacrynic Acid