ACTIVITY OF RAPAMYCIN (AY-22,989) AGAINST TRANSPLANTED TUMORS
ACTIVITY OF RAPAMYCIN (AY-22,989) AGAINST TRANSPLANTED TUMORS
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DOI：
10.7164/antibiotics.37.1231
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发表时间：
1984-01-01
影响因子：
3.3
通讯作者：
VEZINA, C
中科院分区：
文献类型：
--
作者：
ENG, CP;SEHGAL, SN;VEZINA, C
雷帕霉素对几种腹水和实体可移植肿瘤有活性；它对白血病有轻微的活性或无活性。在重量基础上，雷帕霉素的活性低于5-氟尿嘧啶、环磷酰胺和阿霉素，但雷帕霉素对结肠38肿瘤的最大活性与5-氟尿嘧啶和环磷酰胺相似。它的活性是这样的，它可以显著抑制肿瘤在任何发展阶段的生长。在有效剂量范围内，雷帕霉素的毒性低于其他药物。在结肠38肿瘤模型中，给定剂量的雷帕霉素在ig、ig、im和s.c.给药时表现出相同的活性；口服后，其活性降低，但未完全消除。雷帕霉素与5-氟尿嘧啶和环磷酰胺配伍。5-氟尿嘧啶-雷帕霉素-环磷酰胺序贯处理对结肠癌小鼠的保护作用优于5-氟尿嘧啶-阿霉素-环磷酰胺序贯处理。29-去甲氧基雷帕霉素对P388淋巴细胞白血病仅具有边际活性；对B16黑色素瘤和结肠38实体瘤无活性。
Rapamycin exhibits activity against several ascites and solid transplantable tumors; it is slightly active to inactive against leukemias. On a weight basis, rapamycin was less active than 5-fluorouracil, cyclophosphamide and adriamycin, but rapamycin''s maximal activity against Colon 38 tumor was similar to that of 5-fluorouracil and cyclophosphamide. Its activity was such that it significantly inhibited tumor growth at any stage of development. In the active dose range, rapamycin appeared less toxic than the other drugs. In the Colon 38 tumor model, rapamycin at a given dose exhibited the same activity when administered i.p, i.v., i.m. and s.c.; upon oral administration, its activity was reduced but not abolished. Rapamycin was compatible with 5-fluorouracil and cyclophosphamide. The sequential treatment 5-fluorouracil-rapamycin-cyclophosphamide was superior to the sequence 5-fluorouracil-adriamycin-cyclophosphamide in protecting Colon 38 tumor-bearing mice. 29-Demethoxyrapamycin exerted only marginal activity against P388 lymphocytic leukemia; it was inactive against B16 melanocarcinoma and Colon 38 solid tumor.