Hydrocortisone acetate exhibits a variety of bioactivities and pharmacological properties across different assays and receptor interactions. It shows strong binding affinity to corticosteroid-binding globulin (CBG) with a log K of 7.553 and a Ki value of 28.18 nM. For glucocorticoid receptors, it has a high relative binding affinity (RBA) in liver (RBA = 10.0 at 4 hr) and moderate affinity in hepatoma tissue cells (RBA = 9.0 at 4 hr, and RBA = 8.0 at 24 hr), but lower affinity in the thymus (RBA = 3.4 at 4 hr, and RBA = 3.3 at 24 hr).
The compound also demonstrates negligible binding to progestin, androgen, and mineralocorticoid receptors. Additionally, it induces Tyrosine Aminotransferase activity to 91% relative to Dexamethasone. Hydrocortisone acetate shows similar potency to fluocinolone 16,17-acetonide in human vasoconstrictor tests and comparable anti-inflammatory effects to hydrocortisone in rat granuloma assays.
From a physicochemical perspective, Hydrocortisone acetate has a logP value of 2.26 (HPLC method) and 2.19 (general method), indicating moderate lipophilicity. It has a high HPLC capacity factor (log k'w = 1.93), suggesting good retention on the HPLC column, and an intrinsic aqueous solubility of logS0 = -4.34 at pH 10.
In antiviral assays, Hydrocortisone acetate inhibits SARS-CoV-2-induced cytotoxicity in VERO-6 cells and shows inhibitory activity against SARS-CoV-2 3CL-Pro protease (13.7% inhibition at 20 µM). It also demonstrates moderate to high inhibition of sodium fluorescein uptake in OATP1B1 and OATP1B3-transfected CHO cells (93.94% and 91.1% inhibition, respectively, at 10 µM).
In various bioactivity assays, Hydrocortisone acetate acts as an inhibitor of pathways such as AmpC Beta-Lactamase, Nrf2 signaling, Histone Lysine Methyltransferase G9a, ERG Ets/DNA interaction, and several others. Additionally, it exhibits antifungal and antibacterial activity against multiple strains, including Candida albicans, Cryptococcus neoformans, Escherichia coli, and Staphylococcus aureus MRSA, among others.
Overall, Hydrocortisone acetate has potential therapeutic applications across various biological pathways and disease models due to its broad spectrum of bioactivities and moderate lipophilicity..
Note: Summary generated by AI. Data source: ChEMBL 