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$Cu^{2+}$-Anthraquinone Complexes : Formation, Interaction with DNA, and Biological Activity

  • Ko, Thong-Sung (Department of Biochemistry, Chungnam National University) ;
  • Maeng, Hack-Young (Department of Biochemistry, Chungnam National University) ;
  • Park, Mi-Kyeong (Department of Biochemistry, Chungnam National University) ;
  • Park, Il-Hyun (Department of Biochemistry, Chungnam National University) ;
  • Park, In-Sang (Department of Biochemistry, Chungnam National University) ;
  • Kim, Byoung-Sun (Department of Biochemistry, Chungnam National University)
  • Published : 1994.05.20

Abstract

Growth inhibition potency of the anthraquinones, anthraquinone-1,5-disulfonic acid and carminic acid, for Sarcoma 180 and L1210 leukemia cells in vivo and in vitro, was induced by the divalent transition metal ion, $Cu^{2+}$. On the other hand spectroscopic titration data show that the anthraquinone drugs form $Cu2^+$ chelate complexes (carminic acid : $Cu^{2+}$ = 1 : 6; anthraquinone-1,5-disulfonic acid : $Cu^{2+}$ = 1 : 3). Furthermore the $Cu^{2+}$-drug complexes associate with DNA to form the $Cu^{2+}$-anthraquinone-DNA ternary complexes. The formation of the complexes was further supported by the $H_2O_2-dependent$ DNA degradation, which can be inhibited by ethidium bromide, caused by the $Cu^{2+}$-drug complexes. It is likely that the $Cu^{2+}$-mediated cytotoxicity of the anthraquinone drugs is related with the $Cu^{2+}-mediated$ binding of the anthraquinone drugs to DNA and DNA degradation.

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