Hori S, Shirai M, Hirano S, Oki T, Inui T, Tsukagoshi S, Ishizuka M, Takeuchi T, Umezawa H
Gan. 1977 Oct;68(5):685-90.
New anthracycline antibiotics have been isolated from the culture of Streptomyces galilaeus MA144-M1. Among 14 anthracycline compounds, aclacinomycin-A showed the strongest activity in inhibiting leukemia L-1210 and had lower toxicity than others. Antitumor activity of aclacinomycin-A against leukemia L-1210 and P-388, solid sarcoma-180, and lymphosarcoma 6C3HED was examined in comparison with adriamycin and daunomycin. Aclacinomycin-A showed the same degree of activity against leukemia L-1210 and P-388, when administered intraperitoneally, as daunomycin and somewhat less than adriamycin. In oral administration, aclacinomycin-A also exhibited a significant activity on leukemia L-1210. The degree of inhibition of the growth of sarcoma-180 and 6C3HED lymphosarcoma transplanted subcutaneously by aclacinomycin-A was almost the same as that of adriamycin and daunomycin, although the optimal dose was about twice more than adriamycin. Acute cardiotoxicity of aclacinomycin-A by a test using hamsters was more than 10 times lower than that of adriamycin.
从加利利链霉菌MA144-M1的培养物中分离出了新的蒽环类抗生素。在14种蒽环类化合物中，阿克拉霉素A在抑制白血病L-1210方面表现出最强的活性，且毒性比其他化合物低。将阿克拉霉素A与阿霉素和柔红霉素相比，检测了其对白血病L-1210和P-388、实体肉瘤-180以及淋巴肉瘤6C3HED的抗肿瘤活性。当腹腔注射时，阿克拉霉素A对白血病L-1210和P-388的活性程度与柔红霉素相同，略低于阿霉素。口服时，阿克拉霉素A对白血病L-1210也表现出显著活性。阿克拉霉素A对皮下移植的肉瘤-180和6C3HED淋巴肉瘤生长的抑制程度与阿霉素和柔红霉素几乎相同，尽管最佳剂量约为阿霉素的两倍。通过仓鼠试验，阿克拉霉素A的急性心脏毒性比阿霉素低10倍以上。
