| Description | Aurantiamide acetate (Asperglaucide) was isolated from the fermentation broth of Aspergillus penicilloides for the first time. Aurantiamide acetate is a selective and orally active cathepsin inhibitor. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases[1][2]. |
| In vitro | Aurantiamide acetate 在体外条件下对U87和U251癌细胞的活性产生抑制作用，当浓度在10至100 μM范围内时，能显著降低这些癌细胞的活力。此外，Aurantiamide acetate 特别针对半胱氨酸蛋白酶，尤其是对cathepsin L和B的抑制作用明显，其IC50分别为12 μM和49 μM。 |
| In vivo | Aurantiamide acetate 在两种模型中表现出了显著的生物活性。在 U87 小鼠异种移植模型中，通过肿瘤内注射给药，1 mg 的剂量即可减缓肿瘤生长。同时，在辅助性关节炎大鼠模型中，通过皮下注射将此化合物以 10 mg/kg 体重的剂量给药，有效抑制了后爪肿胀。 |
| Target activity | Cathepsin B:49 μM, Cathepsin L:12 μM |
| Synonyms | 金色酰胺醇酯, Asperglaucide |
| molecular weight | 444.52 |
| Molecular formula | C27H28N2O4 |
| CAS | 56121-42-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 55 mg/mL (123.73 mM) |
| References | 1. K Isshiki, et al. Aurantiamide Acetate, a Selective Cathepsin Inhibitor, Produced by Aspergillus Penicilloides. Biosci Biotechnol Biochem. 2001 May;65(5):1195-7. 2. Chi-Su Yoon, et al. Anti-neuroinflammatory Effect of Aurantiamide Acetate From the Marine Fungus Aspergillus Sp. SF-5921: Inhibition of NF-κB and MAPK Pathways in Lipopolysaccharide-Induced Mouse BV2 Microglial Cells.Int Immunopharmacol. 2014 Dec;23(2):568-74. |