Tau-aggregation and neuroinflammation-IN-1

Tau-aggregation and neuroinflammation-IN-1 is a potent tau-aggregation and neuroinflammation inhibitor. Tau-aggregation and neuroinflammation-IN-1 exhibits remarkable inhibitory activities against AcPHF6 and full-length tau aggregation. Tau-aggregation and neuroinflammation-IN-1 has a low cytotoxicity and reduced NO release in LPS-stimulated BV2 cells. Tau-aggregation and neuroinflammation-IN-1 can reverse okadaic acid-induced memory impairment in rats[1].

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

AcPHF6, tau-aggregation, NO[1]

Tau-aggregation and neuroinflammation-IN-1 (compound 30) (0-40 μM) reduces the survival of SH-SY5Y cells at 30 μM, and exerts no significant hepatotoxicity in LO2 cells at high concentrations, also exerts no effect on BV2 cell viability at 20 μM[1]. Tau-aggregation and neuroinflammation-IN-1 (2.5, 5 and 10 μM; 24 hours) retains the anti-inflammatory activity of sodium usnate and inhibits NO release rate by 41% in LPS-stimulated BV2 cells at 10 μM[1]. Cell Cytotoxicity Assay Cell Line: SH-SY5Y, LO2 and BV-2 cells[1] Concentration: 0, 10, 20, 30 and 40 μM Incubation Time: 24 hours Result: Reduced the survival of SH-SY5Y cells at 30 μM, and exerted no significant hepatotoxicity in LO2 cells even at high concentrations (up to 40 μM), also exerted no effect on BV2 cell viability at 20 μM.

Tau-aggregation and neuroinflammation-IN-1 (5 and 10 mg/kg; for 14 days) leads to a substantial improvement of the conventional reference spatial memory and cognitive abilities of OA-induced rats[1]. Animal Model: Male SD rats (250-270 g; OA was microinjected into the right dorsal hippocampus)[1] Dosage: 5 and 10 mg/kg Administration: IP; for 7 days, and after OA-injection continued IP for 7 days Result: Led to a substantial improvement of the conventional reference spatial memory and cognitive abilities of rats.

[1]. Shi CJ, Peng W, Zhao JH, et al. Usnic acid derivatives as tau-aggregation and neuroinflammation inhibitors. Eur J Med Chem. 2020;187:111961.