DuVernay V H, Crooke S T
J Antibiot (Tokyo). 1980 Sep;33(9):1048-53. doi: 10.7164/antibiotics.33.1048.
The class II anthracycline antitumor antibiotics musettamycin, rudolfomycin, aclacinomycin and marcellomycin, which were shown in earlier studies to preferentially inhibit the synthesis of nucleolar RNA in intact tumor cells, were studied in an isolated nucleolar transcriptional assay. Their effects were compared with those of the nucleolar non-selective anthracyclines adriamycin, carminomycin and pyrromycin, as well as with the 10-descarbomethoxy-analogs of marcellomycin and rudolfomycin. The isolated nucleolar transcriptional assay was found to have linear activity for 30 minutes at 30 degrees C. At increasing concentrations of alpha-amanatin up to 200 micrograms/ml, the maximum degree of inhibition of transcriptional activity was found to be 6 approximately 7%. The ranking of nucleolar RNA synthesis inhibitory potencies of the class I and II anthracyclines and the 10-descarbomethoxy-analogs obtained previously in intact cells was reproduced in the isolated nucleoli assay system described here. Thus, evidence for the use of this assay as a screen for nucleolar active antitumor agents is presented.
在早期研究中显示优先抑制完整肿瘤细胞中核仁RNA合成的II类蒽环类抗肿瘤抗生素，如穆塞他霉素、鲁道夫霉素、阿克拉霉素和马塞尔霉素，在一项分离核仁转录试验中进行了研究。将它们的作用与核仁非选择性蒽环类药物阿霉素、卡米诺霉素和吡咯霉素，以及马塞尔霉素和鲁道夫霉素的10-去甲氧基类似物的作用进行了比较。发现分离核仁转录试验在30℃下30分钟具有线性活性。在α-鹅膏蕈碱浓度增加至200微克/毫升时，发现转录活性的最大抑制程度约为6%至7%。在此描述的分离核仁试验系统中重现了先前在完整细胞中获得的I类和II类蒽环类药物以及10-去甲氧基类似物对核仁RNA合成抑制效力的排序。因此，本文提供了使用该试验作为核仁活性抗肿瘤药物筛选方法的证据。
