Numerous studies have demonstrated the availability of high-quality bioactive compounds in food along with their determination and quantification techniques. Many of these identified compounds have been claimed to possess health benefits such as anti-inflammatory, anti-cancer, antioxidant, anti-allergic, anti-fungal, antimicrobial and cardioprotective spasmolytic properties. However, mere presence of these compounds does not directly correlate with their potential health effects upon consumption. Since any food consumed does not reach the blood stream in the original form and as they are broken down to various compounds it is mandatory to consider their bioavailability and metabolism that takes place upon absorption. Furthermore, the efficacy of these bioactive compounds depends on various factors including the dosage, food matrix and stability of the compound during metabolism. Various bioavailability studies indicate that the parent bioactive compound is broken into various metabolites via oxidation, dehydroxylation, de-esterification, hydrolysis, carboxylation, α- and β-oxidation processes inside the human body. Therefore, this leads to an interesting conundrum that whether the proposed health effects are due to the parent bioactive compound or due to the metabolites formed during absorption. Some details in relation to the metabolism and metabolites of food bioactives are presented in this contribution.