体外研究
(In Vitro) | Sertaconazole (0.03-40 μg/mL; 24 h) inhibits 150 strains of yeasts which includes sixCandidaspecies with arithmetic mean MIC of 0.77 μg/mL[1].
Sertaconazole (1 μg/mL; 5, 10, 30, 60 min) activates p38 MAP kinase in a time-dependent manner[2].
Sertaconazole (1, 2 μg/mL; 6, 8, or 24 h) increases a twofold release of PGE2 via COX-2 in keratinocytes, which is dependent on p38 activation[2].
Cetaconazole (10, 20, 30, 40 μM; 24 h) induces strong mitotic arrest by depolymerizing interphase and spindle microtubules, thereby inducing chromosome aggregation defects and causing anti-proliferation effect[3].
Sertaconazole (20, 40 μM; 24 h) induces apoptosis through p53 pathway in HeLa cells[3].
Sertaconazole (20, 30 μM; 24, 48, and 72 h) inhibits the migration of HeLa cells in a concentration-dependent manner[3].
Sertaconazole (15, 30 μM; 24 h) induces autophagy in A549, H460 cells[4].
Cell Viability Assay[1] | Cell Line: | C. albicans,C. guilliermondii,C. krusei,C. parapsilosi,C. tropicalis,C. glabrata | | Concentration: | 0.03-40 μg/m | | Incubation Time: | 24 h | | Result: | Againsted 150 strains of yeasts (sixCandidaspecies) which includedC. albicans,C. guilliermondii,C. krusei,C. parapsilosi,C. tropicalis,C. glabrataspecies with arithmetic mean MIC values of 1.02, 0.51, 0.38, 0.31, 1.67 and 0.78 μg/mL, respectively. |
Western Blot Analysis[2] | Cell Line: | HaCaT cells | | Concentration: | 1 μg/mL | | Incubation Time: | 5, 10, 30, 60 min | | Result: | Showed activity of activating p38 MAP kinase and Hsp27 in a time-dependent manner. |
Western Blot Analysis[2] | Cell Line: | HaCaT cells | | Concentration: | 1, 2 μg/mL | | Incubation Time: | 6 or 8 h | | Result: | Induced 50% expression of COX-2 and resulted in a twofold increased in PGE2 release. |
Western Blot Analysis[2] | Cell Line: | siRNA-transfected HaCaT cells (without p38 MAP kinase expression) | | Concentration: | 1 μg/mL | | Incubation Time: | 24 h | | Result: | Mediated induction of PGE2 was dependent on p38 activation. |
Cell Proliferation Assay[3] | Cell Line: | HeLa, HEK-293, MCF-7, A549 cells | | Concentration: | 0-100 μM | | Incubation Time: | 24 h | | Result: | Showed antiproliferation activity with IC50s of 38, 45.1, 41.5, and 40.8 μM for HeLa, HEK-293, A549, and MCF-7 cells, respectively.
Exhibited mitotic block activity and induced cell death at concentration above 30 μM, but no significant increased in the number of mitotic cells.
Depolymerized interphase and spindle microtubules inducing defect in chromosomal congression. |
Apoptosis Analysis[3] | Cell Line: | HeLa cells | | Concentration: | 10, 20, 40 μM | | Incubation Time: | 24 h | | Result: | Induced approximately 5%, 10%, and 21% cells apoptotic at concentrations of 10, 20 and 40 μM, respectively. |
Western Blot Analysis[3] | Cell Line: | A549 cells | | Concentration: | 20, 40 μM | | Incubation Time: | 24 h | | Result: | Induced apoptosis through p53 pathway that the expression of p53 from 30% to 50% and 95% and p21 from 11 to 39% and 40% respectively.
Resulted in Noxa and Puma, two direct transcriptional targets of p53 to be overexpressed. |
Cell Migration Assay[3] | Cell Line: | HeLa cells | | Concentration: | 20, 30 μM | | Incubation Time: | 24, 48, and 72 h | | Result: | Inhibited the migration of HeLa cells at concentrations lesser than its IC50, which in a concentration-dependent manner. |
Cell Autophagy Assay[4] | Cell Line: | A549, H460 cells | | Concentration: | 15, 30 μM | | Incubation Time: | 24 h | | Result: | Increased endogenous LC3 puncta and LC3 intensity, which indicated induction of autophagy in A549 and H460 cells. |
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