Chitnis M P, Menon R S, Basrur V S, Adwankar M K, Satyamoorthy K
J Cancer Res Clin Oncol. 1985;110(3):221-4. doi: 10.1007/BF00399277.
Reversal of natural resistance to bouvardin (NSC 259968) has been attained in vitro and in vivo, by the calcium influx blocker verapamil in sarcoma 180 cells insensitive to bouvardin. Verapamil increased the in vitro lethality of the tumor cells following exposure with cells for 1 and 3 h as a result of the cytotoxic effect of bouvardin. Similar results were observed in vivo when the tumor cells were exposed to verapamil and then treated with bouvardin, showing a significant percent increase in the lifespan to 30% and 45%. This suggested that this calcium channel blocker had interacted with tumor cell membrane to modulate the response of the cells, and make them more amenable to the drug action.
在体外和体内,钙内流阻滞剂维拉帕米已使对布法地辛(NSC 259968)天然耐药的肉瘤180细胞对其产生敏感性。由于布法地辛的细胞毒性作用,维拉帕米在与细胞接触1小时和3小时后增加了肿瘤细胞的体外杀伤力。当肿瘤细胞暴露于维拉帕米然后用布法地辛治疗时,在体内观察到了类似的结果,寿命显著增加了30%和45%。这表明这种钙通道阻滞剂与肿瘤细胞膜相互作用,调节细胞反应,使其更易受药物作用影响。