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5-甲基四氢叶酸对小鼠甲氨蝶呤毒性的逆转作用。

Reversal of methotrexate toxicity in mice by 5-methyltetrahydrofolic acid.

作者信息

Blair J A, Searle C E

出版信息

Br J Cancer. 1970 Sep;24(3):603-9. doi: 10.1038/bjc.1970.73.

Abstract
  1. Mice have been compeletly protected against the lethal effects of repeated injections of methotrexate by 5-methyltetrahydrofolic acid. Methotrexate-resistant cells probably owe their resistance to their high content of this substance.2. Daily small doses were much more effective than fewer but larger doses.3. The reduced efficiency found in counteracting high dosages of methotrexate may be due to interference with folate transport across cell walls.4. 5-Methyltetrahydrofolic acid and citrovorum factor did not differ greatly in their ability to inhibit methotre toxicity. It is suggested that the pharmaceutical effects of citrovorum factor are due to its conversion to 5-methyltetrahydrofolic acid.
摘要
  1. 5-甲基四氢叶酸可使小鼠完全免受反复注射甲氨蝶呤的致死作用。耐甲氨蝶呤的细胞可能因其该物质含量高而具有抗性。

  2. 每日小剂量比少次但大剂量更有效。

  3. 在对抗高剂量甲氨蝶呤时发现效率降低可能是由于干扰了叶酸跨细胞壁的转运。

  4. 5-甲基四氢叶酸和亚叶酸在抑制甲氨蝶呤毒性的能力上差异不大。有人认为亚叶酸的药理作用是由于其转化为5-甲基四氢叶酸。

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Reversibility of the toxicity of methotrexate by dihydrofolate in mice.
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Folate transport in the central nervous system.中枢神经系统中的叶酸转运
Am J Physiol. 1975 Sep;229(3):777-82. doi: 10.1152/ajplegacy.1975.229.3.777.

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