Kacinski B M, Rupp W D
Cancer Res. 1984 Aug;44(8):3489-92.
The anthracycline antineoplastic agents Adriamycin and N-trifluoroacetyl-Adriamycin-14-valerate were assayed in vivo and in vitro for ability to produce DNA lesions recognized by the UVRABC endonuclease, a DNA repair enzyme of Escherichia coli which recognizes large, bulky lesions in DNA. We found that, while both drugs produce DNA lesions, only the lesions produced by Adriamycin were toxic. Hence, anthracycline antineoplastic activity may be related to production of large, bulky lesions in DNA, while toxicity may correlate with toxicity measured in a simple E. coli DNA repair mutant test system.
对蒽环类抗肿瘤药物阿霉素和N - 三氟乙酰阿霉素 - 14 - 戊酸酯进行了体内和体外测定，以检测它们产生能被UVRABC核酸内切酶识别的DNA损伤的能力。UVRABC核酸内切酶是大肠杆菌的一种DNA修复酶，可识别DNA中的大的、 bulky损伤。我们发现，虽然两种药物都能产生DNA损伤，但只有阿霉素产生的损伤具有毒性。因此，蒽环类抗肿瘤活性可能与DNA中产生大的、 bulky损伤有关，而毒性可能与在简单的大肠杆菌DNA修复突变体测试系统中测得的毒性相关。
