Potentiated Susceptibility of Ascites Tumor to Acyl Derivatives of Ascorbate Caused by Balanced Hydrophobicity in the Molecule

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<jats:p>Orders of susceptibility of Ehrlich ascites tumor to L-ascorbic acid (Asc), its 6-stearoyl (6S), 6-palmitoyl (6P) and 2,6-dipalmitoyl (DP) derivatives were assessed in vitro and in vivo: 6P (a 50% growth inhibitory concentration (IC50) for cultured cells, 12 µM; an increased life-span of treated mice, 283%) >6S (61 µM; 240%)& &gt&;>Asc (430 µM; 122%) ≧DP (>200 µM; 89%), indicating that the enhanced susceptibility was due to acyl moiety substituted at C6-hydroxyl group of Asc, but was retracted by further substitution at C2-hydroxyl group. Equimolar mixture of Asc and palmitic acid, stearic acid or their methyl esters was much less cytotoxic than 6P or 6S. Thus the enhanced susceptibility was not primarily due to an additive cytotoxic effect of ascorbyl and acyl moieties, but to a balanced hydrophobicity introduced into the molecule by a poorly cytotoxic acyl moiety.</jats:p>

収録刊行物

  • Pathobiology

    Pathobiology 54 (5-6), 245-249, 1986

    S. Karger AG

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