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苯妥英的对羟基化作用对中期积累的影响。

The effect of parahydroxylation of diphenylhydantoin on metaphase accumulation.

作者信息

MacKinney A A, Vyas R, Lee S S

出版信息

Proc Soc Exp Biol Med. 1975 Jun;149(2):371-5. doi: 10.3181/00379727-149-38810.

DOI:10.3181/00379727-149-38810
PMID:1153411
Abstract

DPH has a colchicine-like action on metaphase arrest of cultured human lymphocytes. The first step in detoxification of DPH increased its power to accumulate metaphases 3-fold. This hydroxy derivative [5-[4-hydroxyphenyl]-5-phenylhydantoin, HPPH] 3.6 X 10(-4) M was equivalent colchicine 1 x 10(-5) M in its power to inhibit metaphase completion. The effect of HPPH on mitosis was reversible; colchicine effect was not reversed and vincristine effect was partially reversed by washing drug from the medium. Hydroxylation of DPH did not change its inhibition of DNA synthesis and enhanced inhibition of protein synthesis to a minor degree. Detoxification increased the colchicine-like action of DPH.

摘要

DPH对培养的人淋巴细胞中期阻滞具有秋水仙碱样作用。DPH解毒的第一步使其积累中期的能力提高了3倍。这种羟基衍生物[5 - [4 - 羟基苯基] - 5 - 苯基乙内酰脲,HPPH] 3.6×10(-4) M在抑制中期完成的能力上与1×10(-5) M秋水仙碱相当。HPPH对有丝分裂的作用是可逆的;秋水仙碱的作用不可逆,而长春新碱的作用通过从培养基中洗去药物可部分逆转。DPH的羟基化并未改变其对DNA合成的抑制作用,且在较小程度上增强了对蛋白质合成的抑制作用。解毒增强了DPH的秋水仙碱样作用。

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1
The effect of parahydroxylation of diphenylhydantoin on metaphase accumulation.苯妥英的对羟基化作用对中期积累的影响。
Proc Soc Exp Biol Med. 1975 Jun;149(2):371-5. doi: 10.3181/00379727-149-38810.
2
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