This is a polyphenol and an ester of caffeic acid and 3,4-dihydroxyphylllique acid.This is commonly found in Boraginaceae species and Nepettoideae, a Lamiaceaesubfamily. It plays an important role in anti-inflammatory, antitumor, andantiproliferation activities. It shows a dose-dependent inhibition of invasion,migration, and adhesion of LS-174-T human colon carcinoma cells. It inhibits thebone metastasis from breast cancer via NF-κB and its downward IL-8 pathway(Wang et al. 2012). It reduces ERK and COX-2 phosphorylation in colon carcinoma.It reduces the activity of DNA methyltransferase and interferes with RANKL/RANK/OPG networks in breast cancer cells. It targets NF-kB pathway in U938cells and PKA/CREB/MITF pathways in melanoma cells (Singh et al. 2016b). InU938 human leukemic cells, it sensitizes TNF-α-induced apoptosis by affectingNF-kB and ROS and inhibits the activation of NF-kB by inhibiting IκBαphosphorylation and degradation. It also reduces the levels of promoter activity ofCOX-2 protein induced by TPA in HT-29 colon cancer cells and antagonizes TPAstimulating effects on COX-2 expression (Petersen and Simmonds 2003).
IC50 (μg/mL): 1.71 (A2780), 6.96(SW1573), 10.13 (WiDr), 10.13 (T-47D),1.46 (HBL-100) (Guerrero et al. 2006;Zhang et al. 2017)
