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新蒽环类抗生素变活霉素由五种组分组成:变活霉素A、B、C、D和7-脱氧变活霉酮A。变活霉素各组分体外抑制人红白血病K-562细胞生长和诱导其分化活性各不相同。经联苯胺染色,变活霉素C诱导后K-562细胞血红蛋白表达百分率为86%。联苯胺染色阳性细胞最大值出现在第五或第六天;去除药物后,分化细胞为部分可逆性;诱导细胞失去在软琼脂上克隆生长的能力。与其它已知蒽环类抗生素比较,变活霉素C的促分化动力学变化与阿霉素、表阿霉素和柔红霉素相似。但变活霉素C较阿克拉霉素A促分化活性要强。构效关系研究表明,蒽环类抗生素的促分化活性与蒽环上C_3、C_11或C_9或C_10位的取代基以及C_7位的取代糖有很大关系。
Neonitracycline The activein consists of five components: the survivin A, B, C, D and 7-deoxyactivatedin A. Inactivation of various components of mutamycin in vitro inhibited the growth of human erythroleukemia K-562 cells and induced their differentiation activity. After benzidine staining, the percentage of hemoglobin in K-562 cells induced by mutamycin C was 86%. The maximum of benzidine-stained positive cells appeared on the fifth or sixth day; after the drug was removed, the differentiated cells were partially reversible; the cells were induced to lose their ability to grow on soft agar. Compared with other known anthracycline antibiotics, the change in the activity of mutamycin C is similar to doxorubicin, epirubicin and daunorubicin. However, mutamycin C was more effective than aclacinomycin A in promoting differentiation. The study of structure-activity relationship shows that the promoting activity of anthracyclines is closely related to the substituent of C_3, C_11 or C_9 or C_10 on anthracene ring and the substitution sugar of C_7.