Enilospirone

Apoptotic effect and mechanism of ethacrynic acid methyl ester in human acute myeloid leukemia HL-60 cells;

依他尼酸甲酯诱导人急性髓性白血病HL-60细胞凋亡作用和机制的初步探讨

AIM To design and synthesize ethacrynic acid derivatives as GSTπ inhibitors.

依他尼酸(EA)是GSTπ抑制剂,能显著提高许多化疗药物对耐药性肿瘤细胞的细胞毒性。

Objective: To investigate the relationship between the expression and activity of glutathione S-transferasesπ(GST-π) treated with ethacrynic acid (EA ) and resistance to anti-cancer drug cisplatin, adriamycin and VP-16 in vitro in lung adenocarcinoma SPCA-1, lung large cell carcinoma NCI-H- 460 and small cell lung caner NCI-H-446 cell lines.

目的:通过分别检测依他尼酸(Ethacrynic acid,EA)作用下人肺腺癌SPCA-1、大细胞癌NCI-H-460、小细胞癌NCI-H-446细胞株中谷胱甘肽S转移酶-π(Glutathione S-transferasesπ,GST-π)的蛋白表达水平、酶活性及三种细胞在顺铂、阿霉素、VP-16三种化疗药物分别作用下的细胞生存率,来研究GST-π表达及活性的变化与三种肺癌细胞对该三种化疗药耐药的相关性。