Many food-derived phytochemicals and their derivatives represent a cornucopia of new
anti-cancer compounds. Luteolin (3,4,5,7-tetrahydroxy flavone) is a flavonoid found
in different plants such as vegetables, medicinal herbs, and fruits. It acts as an
anticancer agent against various types of human malignancies such as lung, breast,
glioblastoma, prostate, colon, and pancreatic cancers. It also blocks cancer development
in vitro and in vivo by inhibition of proliferation of tumor cells, protection from
carcinogenic stimuli, and activation of cell cycle arrest, and by inducing apoptosis
through different signaling pathways. Luteolin can additionally reverse epithelial-mesenchymal
transition (EMT) through a mechanism that involves cytoskeleton shrinkage, induction
of the epithelial biomarker E-cadherin expression, and by down-regulation of the mesenchymal
biomarkers N-cadherin, snail, and vimentin. Furthermore, luteolin increases levels
of intracellular reactive oxygen species (ROS) by activation of lethal endoplasmic
reticulum stress response and mitochondrial dysfunction in glioblastoma cells, and
by activation of ER stress-associated proteins expressions, including phosphorylation
of eIF2α, PERK, CHOP, ATF4, and cleaved-caspase 12. Accordingly, the present review
article summarizes the progress of recent research on luteolin against several human
cancers.