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编 号:F545981
分子式:C20H15Cl3N2OS
分子量:437.77
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Sertaconazole (FI7056 free base) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells.

体内研究:
Sertaconazole (1% (w/v); apply to the left ear, once) suppresses of TPA-induced ear edema CD-1 mice.Animal Model:CD-1 mice (TPA-induced ear edema model).
Dosage:1% (w/v)
Administration:Apply to the left ear, once.
Result:Exhibited a significant reduction of inflammation in mice by mediating PGE2 release.

体外研究:
Sertaconazole (0.03-40 μg/mL; 24 h) inhibits 150 strains of yeasts which includes six Candida species with arithmetic mean MIC of 0.77 μg/mL.Sertaconazole (1 μg/mL; 5, 10, 30, 60 min) activates p38 MAP kinase in a time-dependent manner.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.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.Sertaconazole (20, 40 μM; 24 h) induces apoptosis through p53 pathway in HeLa cells.Sertaconazole (20, 30 μM; 24, 48, and 72 h) inhibits the migration of HeLa cells in a concentration-dependent manner.Sertaconazole (15, 30 μM; 24 h) induces autophagy in A549, H460 cells.
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