摘要
本文利用流式细胞术(FCM)和动物整体水平的同位素标记药物示踪方法探讨了维拉帕米(VP)增强博莱霉素A_5(BLM)抗癌活性的机制。实验发现VP显著增强BLM对S-180和HEP-2细胞的G_2期阻断效应。VP改变了^(57)Co-BLM在荷瘤小鼠部分器官中的分布,增加厂该药在肿瘤中的积聚。VP增強BLM抗癌活性可能是通过增加药物在肿瘤中的积聚,增强药物的G_2期阻断效应以及其它作用实现的。
The mechanism of enhancement of Bleomycin A_5 antitumor activity by verapamil was explored by flow cytometry and tracing the radiolabelled bleomycin A_5 in vivo. Verapamil was found to increase the G_2 blocking effect of bleomycin A_5 prominently in mouse S-180 and human HEP-2 cell lines. The distribution of ^(57)Co-bleomycin A_5 in mice bearing S - 180 sarcoma was changed by verapamil and accumulation of the drug in tumor was increased. In contrast, the labelled drug in the lung was decreased. It seems that the effects of verapamil in enhancing the antitumor activity of bleomycin A_5 are to increase the accumulation of the drug in tumor cells and enhance the G_2 blocking effect of the drug in cell cycle.
出处
《药学学报》
CAS
CSCD
北大核心
1991年第1期15-19,共5页
Acta Pharmaceutica Sinica
基金
国家自然科学基金
