Interaction of doxorubicin with nuclei isolated from rat liver and kidney

Tetsuya Terasaki, Tatsuji Iga, Yuichi Sugiyama, Manabu Hanano

Research output: Contribution to journalArticlepeer-review

14 Citations (Scopus)

Abstract

The interaction of doxorubicin with nuclei isolated from rat liver and kidney was studied by fluorospectrometry. The nuclei had at least two different types of binding sites for the drug. Both Mg2+ and Ca2+ competitively inhibited the binding of doxorubicin to the nuclei, which showed a remarkable temperature dependency. No significant difference was observed between the numbers of binding sites (n =6.70 × 10−2 mol/mol of DNA for liver; 6.41 × 10−2 mol/mol of DNA for kidney) or the affinity constants (Ka =4.85 × 105 M−1 for liver; 5.41 × 105 M−1 for kidney) under quasi‐physiological conditions. These results obtained from in vitro binding experiments support previous suggestions that the differences in the in vivo distribution of doxorubicin among tissues are not due to differences in the nuclear binding of the drug. The amount of nuclei per gram of tissue is the primary determinant of the characteristic tissue distribution of doxorubicin.

Original languageEnglish
Pages (from-to)524-528
Number of pages5
JournalJournal of Pharmaceutical Sciences
Volume73
Issue number4
DOIs
Publication statusPublished - 1984 Apr
Externally publishedYes

Keywords

  • Binding—interaction of doxorubicin with nuclei isolated from rat liver and kidney, distribution
  • Distribution—interaction of doxorubicin with nuclei isolated from rat liver and kidney, binding
  • Doxorubicin—interaction with nuclei isolated from rat liver and kidney, binding, distribution
  • Nuclei, liver and kidney—interaction with doxorubicin, rats, binding, distribution

ASJC Scopus subject areas

  • Pharmaceutical Science

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