| In Vitro |
Antifungal agent 22 (compound D16) (0-1 μg/mL, 24 h) inhibits ergosterol biosynthesis, which results in stress-induced upregulation of ERG genes in C. neoformans H99[1]. Antifungal agent 22 (0-8 μg/mL) effectively inhibits the growth of C. neoformans H99 (0-72 h), inhibits the formation of C. neoformans H99 biofilms in a concentration-dependent manner (24 h)[1]. Antifungal agent 22 (0-8 μg/mL, 48-72 h) shows selective anti-Cryptococcus activity, has a fungistatic effect[1]. Antifungal agent 22 (0-100 μM, 48 h) shows low cytotoxicity against a human HUVEC cell line with an IC50 of 20.18 μM[1]. Cell Proliferation Assay Cell Line: C. neoformans H99 cells[1] Concentration: 0, 1, 2, 4, 8 μg/mL Incubation Time: 0, 4, 8, 12, 24, 48, and 72 h Result: Almost completely inhibited the growth of C. neoformans H99 at 8 μg/mL, remained at nearly 100% inhibition rate after 72 h, had minimum fungicidal concentrations of 8 μg/mL. Cell Viability Assay Cell Line: Fungal cells (RPMI 1640 medium)[1] Concentration: 0, 0.5, 1, 2, 4, 8 μg/mL Incubation Time: 48, 72 h Result: Showed selective anti-Cryptococcus activity, with IC50 range of 0.06-2 μg/mL and a MIC50 value (average IC50 values) of 0.62 μg/mL.
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| In Vivo |
Antifungal agent 22 (D16) (15 mg/kg, Intragastrically, daily for 5 days) shows potent anti-Cryptococcal efficacy[1]. Animal Model: ICR female mice (18-22 g, 4-6 weeks, tail vein injected with C. neoformans H99 cells)[1] Dosage: 15 mg/kg Administration: Intragastrically, daily for 5 days Result: Showed potent anti-Cryptococcal efficacy, significantly reduced the number of C. neoformans H99 cells in the brain after 5 days, prolong the median survival time (14 days) of the infected mice at a dose of 15 mg/kg.
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