RELATIONSHIP OF THE REDUCTIVE METABOLISM OF INDICINE N-OXIDE TO ITS ANTI-TUMOR ACTIVITY

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  • 1 January 1979
    • journal article
    • research article
    • Vol. 24  (3) , 559-569
Abstract
Several pyrrolizidine alkaloids have been demonstrated to have antitumor activity in experimental tumor systems. In general the free base form of the alkaloid exhibits greater biological activity than the corresponding N-oxide and the N-oxide must be metabolized to the base for the subsequent formation of alkylating intermeditates. Indicine N-oxide is an exception in that it is a more active antitumor agent than its free base indicine. Studies of the antitumor activity and metabolism of indicine N-oxide, and the closely related compound, heliotrine N-oxide, given orally and i.p. to mice bearing P-388 leukemia, suggest that converstion of indicine N-oxide to indicine is not essential for its antitumor activity.