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柔红霉素及其衍生物对原噬菌体λ的诱导作用与抗肿瘤活性的相关性。

Induction of prophage lambda by daunorubicin and derivatives correlation with antineoplastic activity.

作者信息

Anderson W A, Moreau P L, Devoret R, Maral R

出版信息

Mutat Res. 1980 Mar;77(3):197-208. doi: 10.1016/0165-1218(80)90051-8.

Abstract

The antineoplastic drug daunorubicin and 15 other anthracyclines were tested for their ability to induce prophage lambda in Escherichia coli K12. Prophage lambda induction by daunorubicin was obtained in excision-repair deficient uvr- bacteria at doses about 3-fold lower than in excision-repair proficient uvr+ cells; this suggests that some of the lesions produced in DNA by daunorubicin are subject to excision repair and may be adducts. Daunorubicin seems to be converted to active species capable of causing prophage inducing lesions in DNA by bacterial enzymes. The antineoplastic and prophage inducing potencies of the anthracyclines were compared in a blind test. These two parameters were correlated for two thirds of the compounds. Such a correlation supports the idea that the antineoplastic activity of the anthracyclines is a consequence of their capacity to damage DNA.

摘要

对抗肿瘤药物柔红霉素及其他15种蒽环类药物诱导大肠杆菌K12中λ原噬菌体的能力进行了测试。在切除修复缺陷的uvr-细菌中,柔红霉素诱导λ原噬菌体所需的剂量比切除修复 proficient的uvr+细胞低约3倍;这表明柔红霉素在DNA中产生的一些损伤可进行切除修复,且可能是加合物。柔红霉素似乎被细菌酶转化为能够在DNA中引起原噬菌体诱导损伤的活性物质。在一项盲测中比较了蒽环类药物的抗肿瘤和诱导原噬菌体的效力。三分之二的化合物这两个参数存在相关性。这种相关性支持了蒽环类药物的抗肿瘤活性是其损伤DNA能力的结果这一观点。

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