Resveratrol is a naturally occurring phenolic compound found in foods like grapes, berries, and peanuts. It has attracted substantial interest for its potential human health benefits, including antioxidant and anti-inflammatory effects. Research indicates that resveratrol may contribute to cardiovascular health, protect cognitive function, and exhibit anticancer properties. However, various factors such as pH levels, exposure to light, specific enzymes, and metal ions can alter its chemical structure, affecting its biological activities. These reactions can lead to the formation of different metabolites and polymers, which may affect the stability and bioactivity of resveratrol. This review examines the transformation of resveratrol from its natural sources to its consumption by humans. Additionally, we explore the biological activities of the resulting compounds of resveratrol transformations.