The positive health effects of phenolic compounds (PCs) have been extensively reported in the literature. An understanding of their bioaccessibility and bioavailability is essential for the elucidation of their health benefits. Before reaching circulation and exerting bioactions in target tissues, numerous interactions take place before and during digestion with either the plant or host's macromolecules that directly impact the organism and modulate their own bioaccessibility and bioavailability. The present work is focused on the gastrointestinal (GI) interactions that are relevant to the absorption and metabolism of PCs and how these interactions impact their pharmacokinetic profiles. Non-digestible cell wall components (fiber) interact intimately with PCs and delay their absorption in the small intestine, instead carrying them to the large intestine. PCs not bound to fiber interact with digestible nutrients in the bolus where they interfere with the digestion and absorption of proteins, carbohydrates, lipids, cholesterol, bile salts and micronutrients through the inhibition of digestive enzymes and enterocyte transporters and the disruption of micelle formation. PCs internalized by enterocytes may reach circulation (through transcellular or paracellular transport), be effluxed back into the lumen (P-glycoprotein, P-gp) or be metabolized by phase I and phase II enzymes. Some PCs can inhibit P-gp or phase I/II enzymes, which can potentially lead to drug-nutrient interactions. The absorption and pharmacokinetic parameters are modified by all of the interactions within the digestive tract and by the presence of other PCs. Undesirable interactions have promoted the development of nanotechnological approaches to promote the bioaccessibility, bioavailability, and bioefficacy of PCs.

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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.

The search for foods with biological potential for the prevention of chronic diseases has highlighted sorghum, and numerous studies have been conducted to determine the best processing conditions without compromising the nutritional, functional or sensory qualities. We conducted a review of the scientific literature on the techniques used in sorghum and their effects on phenolic compounds and antioxidant capacity. This review allowed us to conclude that the type and content of phenolic compounds in the different varieties of sorghum must be considered for the selection of adequate technologies that allow the retention of phenolic compounds with improved bioaccessibility and biological potential. The available information has been mostly focused on the content of total phenols and the antioxidant activity of sorghum, while the digestibility, absorption, utilization and excretion of phenolic compounds have been poorly studied. On this regard, there is a clear need for further studies on sorghum with the aim of including sorghum as part of a healthy diet.