Comparative in vitro evaluation of dequalinium B, a new boron carrier for neutron capture therapy (NCT)

Anticancer Res. Sep-Oct 2000;20(5B):3395-402.

Abstract

A boronated derivative of dequalinium, a delocalized lipophilic cation (DLC), was synthesized as a potential boron carrier for the selective targeting of mitochondria in malignant versus benign cells for boron neutron capture therapy (BNCT), a binary modality for the treatment of cancer. This agent, designated DEQ-B, was taken up and retained in vitro in the KB, F98, and C6 tumor cell lines but not in the normal epithelial cell line CV1. DEQ-B was also less toxic in the latter cell line at lower exposure concentrations The uptake, retention, and toxicity profiles of DEQ-B are comparable to those of the non-boronated DLCs, dequalinium, MKT 077, RH 123, and tetraphenylphosphonium chloride. Our results suggest that the synthesis and further evaluation of boronated DLCs as potential delivery agents for BNCT is warranted.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / toxicity
  • Boranes / chemical synthesis
  • Boranes / pharmacokinetics
  • Boranes / toxicity
  • Boron Neutron Capture Therapy / methods*
  • Brain Neoplasms / metabolism
  • Cell Line
  • Chlorocebus aethiops
  • Dequalinium / analogs & derivatives*
  • Dequalinium / pharmacokinetics
  • Dequalinium / toxicity
  • Drug Carriers
  • Epithelial Cells / metabolism
  • Glioma / metabolism
  • Humans
  • KB Cells / metabolism
  • Onium Compounds / pharmacokinetics
  • Onium Compounds / toxicity
  • Organophosphorus Compounds / pharmacokinetics
  • Organophosphorus Compounds / toxicity
  • Pyridines / pharmacokinetics
  • Pyridines / toxicity
  • Rats
  • Rats, Inbred F344
  • Rhodamine 123 / pharmacokinetics
  • Rhodamine 123 / toxicity
  • Thiazoles / pharmacokinetics
  • Thiazoles / toxicity
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Boranes
  • Drug Carriers
  • Onium Compounds
  • Organophosphorus Compounds
  • Pyridines
  • Thiazoles
  • Rhodamine 123
  • MKT 077
  • Dequalinium
  • tetraphenylphosphonium