Tanshindiol C (1-10 μM; for 24 h) activates Nrf2 and upregulates Prdx1 expression and mRNA levels in macrophages. Tanshindiol C protects macrophages from oxidized low-density lipoprotein (oxLDL) induced foam cell formation via activation of Prdx1/ABCA1 signaling[1].
Tanshindiol C inhibits both wild-type and A667G mutant (Ki value of 176 nM) EZH2 activity with similar potencies[2].
Tanshindiol C inhibits growth of the cell lines such as Pfeiffer, U-2932 and Daudi (lymphoma), PC3 (prostate cancer), T98G and U87MG (glioma), and A549 (lung cancer), with GI50 values of 1.5 μM, 9.5 μM, 10.6 μM, 4 μM, 6 μM, 5.7 μM and 4.2 μM, respectively[2].
Tanshindiol C (1-5 μM; 72 hours) induces accumulation of Pfeiffer cells in sub-G1 phase, which indicates cells in late apoptosis and necrosis[2].
Tanshindiol C (1-3 μM; 72 hours) increases protein levels of the important apoptosis related protein markers, cleaved caspase-3, caspase-7 and poly ADP-ribose polymerase (PRAP) in the cells.Tanshindiol C significantly decreases the levels of H3K27me3 in cells[2].
References:
[1]. Yuyu Yang, et al. Tanshindiol C inhibits oxidized low-density lipoprotein induced macrophage foam cell formation via a peroxiredoxin 1 dependent pathway. Biochim Biophys Acta Mol Basis Dis. 2018 Mar;1864(3):882-890.
[2]. Jimin Woo, et al. Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2486-92.