2-Methoxy-1,4-naphthoquinone, isolated from the leaves of Impatiens glandulifera, specifically suppressed the expression of PKC βI, δ, and ζ in a concentration-dependent manner in Raji cells.
2-Methoxy-1,4-naphthoquinone (MNQ) exhibits antifungal, antimicrobial activities and showed strong killing effect on K562, HL-60, Raji, MCF-7, H-23, IMR-32, LA-174-T, HSC-2, and SK-MEL-28. MNQ is able to trigger the intrinsic apoptotic pathway in K562 cells, as well as causing p53-dependent cell cycle arrest in the p53-wild type cell line. MNQ inhibits the TCF/β-catenin (TOP) transcriptional activity at IC50 2.9 μM, while it decreases the transcriptional activity of FOP (mutated TCF-binding site)-transfected cell. MNQ exerts an anti-metastatic effect against MDA-MB-231 cells. MNQ has remarkable selectivity towards PKCβI and ζ suppression. MNQ suppresses PKCδ moderately, where MNQ suppresses half of the PKCδ expression at the concentration of 10 μM. MNQ does not suppress PKC βII[1]. MNQ is able to inhibit the invasion and migration characteristics of a highly metastatic MDA-MB-231 cancer cell line[2].
[1] Wong Teck Yew, et al. Journal of Applied Pharmaceutical Science. 2015, 5(08), pp001-005. [2] Liew K, et al. Toxicol In Vitro. 2014, 28(3):335-9.