Gupta S, Kim J, Gollapudi S
Division of Basic and Clinical Immunology, University of California, Irvine 92717.
J Clin Invest. 1991 Apr;87(4):1467-9. doi: 10.1172/JCI115154.
Itraconazole is a recently developed triazole antifungal agent that inhibits cell membrane sterol biosynthesis. Itraconazole, in a dose-dependent manner, enhanced intracellular accumulation of daunorubicin and reversed the drug resistance in murine leukemia P388/ADR cells. In addition, itraconazole corrected the altered plasma membrane potentials of P388/ADR cells. The concentrations of itraconazole that reversed drug resistance are comparable to the plasma levels achieved by therapeutic dosage used in the treatment of fungal infections. Therefore, itraconazole is a potential candidate for in vivo use to reverse multidrug resistance in cancer with added benefit of its antifungal property.
伊曲康唑是一种最近研发的三唑类抗真菌药物,可抑制细胞膜甾醇生物合成。伊曲康唑以剂量依赖的方式增强柔红霉素在细胞内的蓄积,并逆转小鼠白血病P388/ADR细胞的耐药性。此外,伊曲康唑纠正了P388/ADR细胞改变的质膜电位。逆转耐药性的伊曲康唑浓度与治疗真菌感染所用治疗剂量所达到的血浆水平相当。因此,伊曲康唑是体内逆转癌症多药耐药性的潜在候选药物,且具有抗真菌特性这一额外益处。