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The aim of this special issue on “Bioactive Compounds of Food: Their Role in the Prevention and Treatment of Diseases” is to provide a representation of the new trends of bioactive compounds of food involved in different pathologies. Food bioactive compounds are extranutritional constituents that typically occur in small quantities in foods. In summary, numerous bioactive compounds appear to have beneficial health effects. Much scientific research needs to be conducted before we can begin to make science-based dietary recommendations. Despite this, there is sufficient evidence to recommend consuming food sources rich in bioactive compounds. From a practical perspective, this translates to recommending a diet rich in a variety of fruits, vegetables, whole grains, legumes, oils, and nuts. Therefore, the current issue will be focused on identifying as well as understanding the mechanistic role of food bioactive compounds in a range of human pathologies. This issue is logically divided into four main areas: (a) bioactive compounds and inflammation, (b) functional food in chronic diseases, (c) bone health and polyphenols, and (d) neuroprotective effects of bioactive compounds. Forty-four papers were selected through our routine rigorous double-blind external peer review by qualified experts. Due to the capacity limitation, some papers have already appeared earlier in the last issue (volume 2019, No. 2019). Some papers are briefly introduced below.