Structure of the adriamycin-cardiolipin complex. Role in mitochondrial toxicity

Biophys Chem. 1990 Apr;35(2-3):247-57. doi: 10.1016/0301-4622(90)80012-v.


Adriamycin and its derivatives are among the most efficient antimitotics used in clinical therapy. A specific cardiotoxicity places a limit on the total dose of adriamycin that may be administered. The mechanism of cardiac toxicity is complex. Data accumulated from in vitro and in vivo studies indicate a possible common cause for the inhibition of numerous enzymes and tissue degradation by a free radical mechanism: the binding of adriamycin to the inner mitochondrial membrane cardiolipin. The structure of the adriamycin-cardiolipin complex has been investigated by using physico-chemical techniques and via conformational analysis. The results open a rational way to design new structures that are less cardiotoxic.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Cardiolipins / metabolism*
  • Chemical Phenomena
  • Chemistry, Physical
  • Doxorubicin / metabolism
  • Doxorubicin / toxicity*
  • Heart / drug effects*
  • Humans
  • Mitochondria / drug effects*
  • Mitochondria / enzymology
  • Mitochondria / metabolism
  • Myocardium / metabolism


  • Cardiolipins
  • Doxorubicin