Sesamol is a constituent of sesame oil. Sesamol shows a free radical scavenging activity. Sesamol shows an IC50=5.95±0.56 μg/mL in the DPPH assay. Anti-oxidant activities[1]. Anticancer activities[2].
Sesamol has also been shown to be a classical inhibitor of lipid peroxidation[1]. Sesamol (0-1 mM) efficiently induces the apoptosis of human liver hepatocellular carcinoma (HepG2) cells[2]. Sesamol suppresses cell proliferation and induces intrinsic and extrinsic apoptosis in HepG2 cells[2]. Sesamol treatment elicites mitochondrial dysfunction by inducing a loss of mitochondrial membrane potential. Sesamol inhibits mitophagy and autophagy through impeding the PI3K Class III/Belin-1 pathway. Sesamol decreases the expression of anti-apoptotic protein Bcl-2, but shows no effect on the expression of apoptotic signal Bax. Sesamol improves the protein expression of Fas/FasL, and activates tBid and caspase-8 which are all involved in the extrinsic apoptosis pathway[2].
Sesamol treatment for 35 days does not significantly impact body weight, although the tumor volume is dramatically inhibited (40.56% size inhibitory rate with Sesamol at 200 mg/kg compared to the control group). However, a lower dose (100 mg/kg Sesamol) only has significant anti-tumor growth effect up to 27 days after the first treatment[2]. The Bcl-2/Bax ratio in tumor tissues is also decreased. Moreover, in the Sesamol treatment group, levels of the cell proliferation marker Ki76 are down-regulated, and levels of the cell apoptosis marker cleaved-caspase 3 are increased when compared to control. The expression of LC3 protein is remarkably decreased by Sesamol in a dose-dependent manner[2].
[1]. Kapadia GJ, et al. Chemopreventive effect of resveratrol, sesamol, sesame oil and sunflower oil in the Epstein-Barrvirus early antigen activation assay and the mouse skin two-stage carcinogenesis. Pharmacol Res. 2002 Jun;45(6):499-505. [2]. Liu Z, et al. Sesamol Induces Human Hepatocellular Carcinoma Cells Apoptosis by Impairing MitochondrialFunction and Suppressing Autophagy. Sci Rep. 2017 Apr 4;7:45728.