Grdina D J, Sigdestad C P, Peters L J
Br J Cancer. 1980 Nov;42(5):677-83. doi: 10.1038/bjc.1980.301.
The cytotoxic effects in vivo of single doses of either adriamycin (ADM), 1-beta-D-arabinofuranosylcytosine (Ara-C), bleomycin (BLM), cis-diamminedichloroplatinum (II) (cis-DDP), or cyclophosphamide (CY) on murine fibrosarcoma (FSa) cell populations were determined. Tumour cells were separated and synchronized by centrifugal elutriation. Viable tumour cells from selected elutriator fractions were then injected i.v. into whole-body-irradiated mice. Twenty minutes later selected doses of ADM, Ara-C, BLM, cis-DDP or CY were administered to selected groups of these animals. Fourteen days later the mice were killed. Killing of injected tumour cells by each of the chemotherapeutic agents was evidenced by a reduction in the lung cells by each of the chemotherapeutic agents was evidenced by a reduction in the lung colonies per cell injected in treated animals. Under these conditions the response of FSa cells in vivo to the 5 drugs tested differed both qualitatively and quantitatively. Ara-C was S-phase-specific in toxicity. ADM, BLM, and cis-DDP were preferentially toxic to S, G2+M and G1 cells respectively. CY, a drug requiring bioactivation to form alkylating metabolites, was found to be equally toxic to G1 and G2+M enriched populations, but less effective in killing cell populations enriched with early-S cells.
测定了单剂量阿霉素（ADM）、1-β-D-阿拉伯呋喃糖基胞嘧啶（Ara-C）、博来霉素（BLM）、顺二氨二氯铂（II）（顺铂）或环磷酰胺（CY）对小鼠纤维肉瘤（FSa）细胞群体的体内细胞毒性作用。通过离心淘析分离并同步肿瘤细胞。然后将来自选定淘析组分的活肿瘤细胞静脉注射到全身照射的小鼠体内。20分钟后，给这些动物的选定组施用选定剂量的ADM、Ara-C、BLM、顺铂或CY。14天后处死小鼠。每种化疗药物对注射的肿瘤细胞的杀伤作用通过处理动物中每注射一个细胞的肺集落减少来证明。在这些条件下，FSa细胞在体内对所测试的5种药物的反应在定性和定量方面都有所不同。Ara-C在毒性上具有S期特异性。ADM、BLM和顺铂分别对S期、G2+M期和G1期细胞具有优先毒性。CY是一种需要生物活化以形成烷基化代谢产物的药物，发现它对富含G1期和G2+M期的细胞群体具有同等毒性，但在杀死富含早S期细胞的群体方面效果较差。
