Ergosterol exhibits multifaceted bioactivities, including anti-inflammatory, antibacterial, antiviral, and anticancer properties. It inhibits NO production with IC50 values of 27,900 nM in NOX inhibition in fMLP-induced PMN cells and 30,600 nM in iNOS inhibition in mouse BV2 microglial cells, suggesting potential modulation of inflammatory pathways. It demonstrates antibacterial activity against Legionella pneumophila Corby with an MIC of 250.0 µg/mL, and also inhibits the growth of Pseudomonas aeruginosa and Staphylococcus aureus with inhibition zones of 8.7 mm and 11.2 mm respectively at a concentration of 2 mg/mL.
Antiviral activities include inhibiting SARS-CoV-2-induced cytotoxicity in Caco-2 and VERO-6 cells at 10 µM concentration, with respective inhibition rates of 11.1% and 0.04%. The compound also shows 2.051% inhibition of SARS-CoV-2 3CL-Pro protease at 20 µM concentration. In addition, it inhibits sodium fluorescein uptake in OATP1B1 and OATP1B3-transfected CHO cells by 31.68% and 52.34% at 10 µM, respectively.
In cancer research, Ergosterol demonstrates cytotoxicity against various cell lines, including mouse L5178Y (EC50: 12,600 nM), human COLO 205 (IC50: 4,900 nM), COLO 320 (IC50: 6,500 nM), and MRC5 (IC50: 500 nM). It shows antiproliferative activity against human NCI-H157 and A549 cells, with IC50 values of 23,300 nM and 19,200 nM, respectively. Significant antitumor activity is observed in xenografted mouse models with Lewis lung cancer cells, with 100% growth inhibition at 12.5 µg/mL after 48 hours and evidence of metastasis inhibition or tumor regression. Despite some toxicity-related net weight reduction, the compound maintains 100% survival rates in treated mouse models.
Additionally, Ergosterol exhibits specific bioactivities such as inhibiting TNFalpha-induced NF-kappaB activity in HeLa cells with an IC50 of 0.91 µg/mL and inhibiting human HDAC6 with 26.56% inhibition in an enzymatic assay. However, it shows no activity against UGT1A1 and slight negative inhibition in a custom peptide substrate HDAC6 assay. The compound also potentiates doxorubicin-induced cytotoxicity by inhibiting P-glycoprotein activity in COLO 320 cells..
Note: Summary generated by AI. Data source: ChEMBL 