Antioxidant, anti-acetylcholinesterase, and anti-amyloid-β peptide aggregations of hispolon and its analogs in vitro and improved learning and memory functions in scopolamine-induced ICR mice

Background: Hispolon, one of bioactive phenolic compounds from a medicinal mushroom of sang-huang (Phellinus linteus) has been reported to exhibit anticancer and anti-inflammatory activities. The Alzheimer's disease (AD) is ranked one of the top ten leading causes of death worldwide. Little is known about the effects of hispolon on delaying AD progression.

Results: The hispolon (No.1) and its six structural analogs (No.2 to No.7) were assayed by antioxidant, anti-acetylcholinesterase activities and anti-amyloid-β_1-42-peptide aggregations. The No.1, No.6, and No.7 were selected for further molecular docking with acetylcholinesterase and core fragments of amyloid-β-peptide, and also showed capacities to recover cell viabilities in methylglyoxal-treated SH-SY5Y cells and also to enhance neurite outgrowths in PC12 cells. The daily pre-treatments of No.1, No.6, and No.7 for 10-days (40 mg/kg/day) showed to improve learning dysfunctions in scopolamine-induced ICR mice by passive avoidance tests.

Conclusion: The hispolon in the fungus sang-huang might be beneficial to develop functional foods or as lead compounds for treating degenerative disorders.