新規アクリジン誘導体のEthidium-DNA蛍光消光効果と抗がん活性

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概要

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• In order to elucidate the relationships between the antitumor activity and the molecular structure of novel acridine derivatives (la-f, and 2a-e in Chart 1) the DNA-binding properties (intercalation) of the derivatives were examined by the quenching in fluorescence of an ethidium-DNA complex, which may be caused by the displacement of DNA-bound ethidium by a second DNA-binding ligand, acridines. The concentration (C_<50> value) of the acridine necessary to reduce the initial fluorescence of DNA-bound ethidium by 50% showed a good correlation with their antitumor activities. The fluorescence quenching of the acridines was examined using 4'-(9-acridinylamino)-methanesulfonanilide (amsacrine, AMSA) as a typical standard of the second DNA-bound ligand, and calf thymus DNA with an apparent site size of two base pairs.

• 社団法人日本薬学会の論文
• 1992-12-25

著者

• 木邑 道夫

  京都大学医学部附属病院

• 木邑 道夫

  Department Of Pharmacy Kyoto University Hospital Faculty Of Medicine Kyoto University

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