Phenolic compounds that cross the blood-brain barrier exert positive health effects as central nervous system antioxidants

The blood-brain barrier (BBB) is a physical structure whose main function is to strictly regulate access to circulating compounds into the central nervous system (CNS). Vegetable-derived phenolic compounds have been widely studied, with numerous epidemiologic and interventional studies confirming their health-related bioactivities across multiple cells, organs and models. Phenolics are non-essential xenobiotics, and should theoretically be unable to cross the BBB. The present work summarizes current experimental evidence that reveals that not only are phenolic compounds able to cross the BBB and bioaccumulate in the brain, but there is some stereoselectivity, which suggests the presence of specific transporters that allow them to reach the brain. Some molecules cross the BBB intact, while others do so only after being biotransformed or metabolized elsewhere. Once inside the CNS, they prevent or counter oxidative stress, which maintains the molecular, cellular, structural and functional integrity of the brain, and subsequently, overall human health. The ability of phenolic compounds to cross the blood-brain barrier and reach the central nervous system is discussed. There are knowledge gaps that require additional experimentation, such as inconclusive transport mechanisms and lack of human data.