Agut J, Palacín C, Salgado J, Casas E, Sacristán A, Ortiz J A
Research Centre, Ferrer Group, Barcelona, Spain.
Arzneimittelforschung. 1992 May;42(5A):721-4.
The direct action of 7-chloro-3-[1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethoxy- methyl]benzo[b]thiophene (sertaconazole, FI-7045, CAS 99592-32-2) on the membrane integrity of C. albicans is studied by quantifying the leakage of intracellular adenosine triphosphate (ATP) into the medium as an index of the changes in membrane permeability and integrity and cell viability of the culture used. Sertaconazole caused a dose-dependent decrease in intracellular ATP after only 10-min exposure and a concomitant significant increase in extracellular ATP. This behaviour is characteristic of antifungals which are fungicidal as a result of a direct membrane damage. Thus sertaconazole, in addition to the mechanism of action responsible for its fungistatic activity (inhibition of ergosterol synthesis), has a second mechanism of action providing a significant fungicidal activity due to direct cell membrane damage.
通过量化细胞内三磷酸腺苷（ATP）泄漏到培养基中的情况，以其作为膜通透性、完整性及所用培养物细胞活力变化的指标，研究了7-氯-3-[1-(2,4-二氯苯基)-2-(1H-咪唑-1-基)乙氧基甲基]苯并[b]噻吩（舍他康唑，FI-7045，CAS 99592-32-2）对白色念珠菌膜完整性的直接作用。仅暴露10分钟后，舍他康唑就使细胞内ATP呈剂量依赖性减少，同时细胞外ATP显著增加。这种行为是因直接膜损伤而具有杀真菌作用的抗真菌药物的特征。因此，舍他康唑除了具有导致其抑菌活性的作用机制（抑制麦角甾醇合成）外，还具有第二种作用机制，即由于直接的细胞膜损伤而具有显著的杀真菌活性。
