Hu Y P, Lin J, Wang Q D, Yie Q X, Zhang T M
Henan Institute of Medical Sciences, Zhengzhou.
Yao Xue Xue Bao. 1993;28(1):75-8.
The effectiveness of adriamycin (ADR) in the treatment of cancer has been limited by the development of drug resistance. Verapamil and ligustrazini were found to show significant potentiating effect on the cytotoxicity of ADR in vitro and decreased the IC50 of ADR by 84.85% and 30.82% of the resistant line, respectively, and no effect was found on the IC50 in the sensitive line. The Glutathione-S-transferase activity of ADR-resistant and sensitive mouse EAC was determined in vivo. The activity in resistant cancer was 1.72-fold higher than that in sensitive cancer. Administration of verapamil or ligustrazini decreased the GST activity of resistant EAC by 35.50% or 26.05%, respectively and no effect was observed on sensitive cancer. The results show that verapamil and ligustrazini can reverse partly the ADR-resistance in resistant mouse EAC.
阿霉素（ADR）治疗癌症的有效性受到耐药性发展的限制。发现维拉帕米和川芎嗪在体外对ADR的细胞毒性显示出显著的增强作用，使耐药细胞系中ADR的半数抑制浓度（IC50）分别降低了84.85%和30.82%，而对敏感细胞系的IC50没有影响。在体内测定了耐ADR和敏感小鼠艾氏腹水癌（EAC）的谷胱甘肽 - S - 转移酶活性。耐药癌中的活性比敏感癌高1.72倍。给予维拉帕米或川芎嗪分别使耐药EAC的谷胱甘肽 - S - 转移酶活性降低35.50%或26.05%，而对敏感癌没有影响。结果表明，维拉帕米和川芎嗪可部分逆转耐药小鼠EAC中的ADR耐药性。
