Uematsu A, Ho D H, Drewinko B, Yang L Y, Brown N S, Bodey G P, Krakoff I H
Anticancer Res. 1986 Jan-Feb;6(1):1-3.
The lethal effects of peplomycin and bleomycin on cultured human colon cancer cells (LoVo) were compared by using the technique of inhibition of colony formation. The survival of LoVo cells after treatment for 1 h with either peplomycin or bleomycin was characterized by a biphasic exponential curve. When the exposure time was extended to 24 h, both drugs produced much greater cytotoxic effects, with survival decreased to less than 0.10% for bleomycin and less than 0.02% for peplomycin. Both peplomycin and bleomycin, in a dose-dependent manner, inhibited the incorporation of thymidine into cells. On an equal-weight basis, the cytotoxicity of peplomycin (24-h exposure) was similar to that of bleomycin. Both agent also inhibited the incorporation of leucine and uridine after 24 h of drug exposure, but to a lesser extent than inhibition of thymidine incorporation. However, after 1 h of exposure, such inhibitory effects were minimal. These results demonstrate that prolonged peplomycin or bleomycin exposure produces greater cell-kill than shorter drug exposure. Schedules with continuous drug administration should be explored clinically.
采用集落形成抑制技术比较了培普利霉素和博来霉素对培养的人结肠癌细胞（LoVo）的致死作用。培普利霉素或博来霉素处理1小时后，LoVo细胞的存活情况呈双相指数曲线。当暴露时间延长至24小时时，两种药物均产生了更大的细胞毒性作用，博来霉素处理后细胞存活率降至0.10%以下，培普利霉素处理后细胞存活率降至0.02%以下。培普利霉素和博来霉素均以剂量依赖的方式抑制胸苷掺入细胞。以等重量为基础，培普利霉素（24小时暴露）的细胞毒性与博来霉素相似。两种药物在暴露24小时后也抑制亮氨酸和尿苷的掺入，但程度低于对胸苷掺入的抑制。然而，暴露1小时后，这种抑制作用很小。这些结果表明，与较短时间的药物暴露相比，长时间的培普利霉素或博来霉素暴露产生更大的细胞杀伤作用。临床上应探索持续给药方案。
