Description
Esculetin is a coumarin lactone found in chicory and other plants; it exhibits anticoagulant, anti-obesity, anti-hyperlipidemic, anti-inflammatory, anticancer, antioxidative, and neuroprotective activities. Esculetin decreases levels of NO, PPARγ, TNF-α, and MCP-1 and increases levels of heme oxygenase 1 (HO-1) in macrophages. In animal models of Parkinson’s disease, esculetin inhibits MPTP-induced neurotoxicity and neuronal apoptosis. In high fat diet-fed rats, this compound decreases body weight, triglyceride levels, total cholesterol, and glucose levels. Additionally, esculetin induces cell cycle arrest, DNA fragmentation, activation of caspases 3 and 9, reduction of the mitochondrial membrane potential, and apoptosis in acute promyelocytic leukemia (APL) cells. Esculetin also inhibits proliferation of colon cancer cells by directly inhibiting β-catenin. This compound also acts as a radical scavenger in vitro.
References
Kim Y, Park Y, Namkoong S, et al. Esculetin inhibits the inflammatory response by inducing heme oxygenase-1 in cocultured macrophages and adipocytes. Food Funct. 2014 Aug 20;5(9):2371-7. PMID: 25088305.
Rubio V, Calviño E, García-Pérez A, et al. Human acute promyelocytic leukemia NB4 cells are sensitive to esculetin through induction of an apoptotic mechanism. Chem Biol Interact. 2014 Jul 1;220C:129-139. PMID: 24995577.
Medina ME, Galano A, Alvarez-Idaboy JR. Theoretical study on the peroxyl radicals scavenging activity of esculetin and its regeneration in aqueous solution. Phys Chem Chem Phys. 2014 Jan 21;16(3):1197-207. PMID: 24292723.
Lee SY, Lim TG, Chen H, et al. Esculetin suppresses proliferation of human colon cancer cells by directly targeting β-catenin. Cancer Prev Res (Phila). 2013 Dec;6(12):1356-64. PMID: 24104353.
Karmase A, Birari R, Bhutani KK. Evaluation of anti-obesity effect of Aegle marmelos leaves. Phytomedicine. 2013 Jul 15;20(10):805-12. PMID: 23632084.
Subramaniam SR, Ellis EM. Neuroprotective effects of umbelliferone and esculetin in a mouse model of Parkinson's disease. J Neurosci Res. 2013 Mar;91(3):453-61. PMID: 23184853.
