Antifungal agent 22 (compound D16) 是一种潜在的口服有效的抗真菌药物，其IC50值为 0.5 μg/mL。Antifungal agent 22 能穿透血脑屏障，通过破坏真菌细胞膜的完整性杀死C. neoformansH99 细胞。Antifungal agent 22 具有选择性抗隐球菌活性，代谢稳定性好，细胞毒性低。
| 生物活性 | Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with anIC50of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill theC. neoformansH99 cells by destroying the integrity offungalcell membranes. Antifungal agent 22 shows selective anti-Cryptococcusactivity with good metabolic stability and low cytotoxicity[1]. |
| IC50& Target | IC50: 0.5 μg/mL (Fungal)[1]. |
体外研究
(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 inC. neoformansH99[1].
Antifungal agent 22 (0-8 μg/mL) effectively inhibits the growth ofC. neoformansH99 (0-72 h), inhibits the formation ofC. neoformansH99 biofilms in a concentration-dependent manner (24 h)[1].
Antifungal agent 22 (0-8 μg/mL, 48-72 h) shows selective anti-Cryptococcusactivity, has a fungistatic effect[1].
Antifungal agent 22 (0-100 μM, 48 h) shows low cytotoxicity against a human HUVEC cell line with an IC50of 20.18 μM[1].
Cell Proliferation Assay | Cell Line: | C. neoformansH99 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 ofC. neoformansH99 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-Cryptococcusactivity, withIC50range of 0.06-2 μg/mL and aMIC50value (averageIC50values) of 0.62 μg/mL. |
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体内研究
(In Vivo) | Antifungal agent 22 (D16) (15 mg/kg, Intragastrically, daily for 5 days) shows potent anti-Cryptococcalefficacy[1].
| Animal Model: | ICR female mice (18-22 g, 4-6 weeks, tail vein injected withC. neoformansH99 cells)[1] | | Dosage: | 15 mg/kg | | Administration: | Intragastrically, daily for 5 days | | Result: | Showed potent anti-Cryptococcalefficacy, significantly reduced the number ofC. neoformansH99 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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