Overview of the absorption, metabolism, and targets of resveratrol. Upon oral intake, resveratrol and its precursors enter the gut and are partially metabolized by gut microbiota to produce microbiota-derived resveratrol derivatives and resveratrol. Like resveratrol, other resveratrol derivatives like piceatannol and dihydroresveratrol can also be absorbed into the blood circulation. Free resveratrol is conjugated in the liver, from where conjugated forms can return to the intestine. Resveratrol glucuronidation and sulfation in the liver to form resveratrol glucuronide and sulfate derivatives. After delivery to the target organ, resveratrol can be deconjugated to stimulate a biological response via regulation of its molecular targets, by which it benefits against cardiovascular disease and kidney disease. AhR = aryl hydrocarbon receptor. SIRT-1 = silent information regulator-1. mTOR = mammalian target of rapamycin. NF-κB = nuclear factor-kappa B. AMPK = adenosine monophosphate-activated protein kinase. ERα = estrogen receptor α. ATF2 = activating transcription factor 2. Nrf2 = nuclear factor (erythroid-derived 2)-like 2. PPAR = peroxisome proliferator-activated receptor. COX-2 = cyclooxygenase-2.