| 川芎嗪和维拉帕米纠正阿霉素对小鼠艾氏腹水癌的抗药性 |
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| 引用本文： | 胡艳平,刘健,王庆端,叶启霞,张覃沐.川芎嗪和维拉帕米纠正阿霉素对小鼠艾氏腹水癌的抗药性[J].药学学报,1993(1). |
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| 作者姓名： | 胡艳平 刘健 王庆端 叶启霞 张覃沐 |
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| 作者单位： | 河南省医学科学研究所药理室，河南省医学科学研究所药理室，河南省医学科学研究所药理室，河南省医学科学研究所药理室，河南省医学科学研究所药理室 郑州 450052，郑州 450052，郑州 450052，郑州 450052，郑州 450052 |
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| 基金项目： | 国家自然科学基金,编号 39170831 |
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| 摘 要： | 阿霉素(adriamycin,ADR)广泛应用于肿瘤临床,但易产生抗药性及多药抗药性(multidrug resistance,MDR),从而限制了其临床疗效的发挥。MDR与细胞表型改变有关。抗ADR的人乳腺癌细胞和小鼠SEWA癌细胞内,谷胱甘肽-S-转移酶(GST)的活性增高。ADR的MDR可被钙拮抗剂逆转,但是否与GST有关尚未见报道。
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| 关 键 词： | 维拉帕米 川芎嗪 阿霉素 多药抗药性 谷胱甘肽-S-转移酶 |
REVERSAL OF ADRIAMYCIN RESISTANCE BY VERAPAMIL AND LIGUSTRAZINI IN MOUSE EHRLICH ASCITES CANCER |
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| YP Hu,J Lin,QD Wang,QX Yie and TM Zhang.REVERSAL OF ADRIAMYCIN RESISTANCE BY VERAPAMIL AND LIGUSTRAZINI IN MOUSE EHRLICH ASCITES CANCER[J].Acta Pharmaceutica Sinica,1993(1). |
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| Authors: | YP Hu J Lin QD Wang QX Yie and TM Zhang |
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| Abstract: | 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 IC_(50) of ADR by 84.85% and 30. 82% of the resistant line, respectively, and no effect was found on the IC_(50) in the sensitive line. The Glutathione-S-transfers 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. |
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| Keywords: | Verapamil Ligustrazini Adriamycin Multidrug resistance Glutathines-S-transfers |
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