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These high UA levels are associated with increased purine ingestion and metabolization and\/or its decreased excretion. In this field, xanthine oxidase (XO), by converting hypoxanthine and xanthine to UA, plays an important role in hyperuricemia control. Based on limitations and adverse effects associated with the use of allopurinol and febuxostat, the most known approved drugs with XO inhibitory effect, the search for new molecules with XO activity is growing. However, despite the high number of studies, it was found that the majority of tested products with relevant XO inhibition were left out, and no further pharmacological evaluation was performed. Thus, in the present review, available information published in the past six years concerning isolated molecules with <jats:italic>in vitro<\/jats:italic> XO inhibition complemented with cytotoxicity evaluation as well as other relevant studies, including <jats:italic>in vivo<\/jats:italic> hypouricemic effect, and pharmacokinetic\/pharmacodynamic profile was compiled. Interestingly, the analysis of data collected demonstrated that molecules from natural sources or their mimetics and semisynthetic derivatives constitute the majority of compounds being explored at the moment by means of <jats:italic>in vitro<\/jats:italic> and <jats:italic>in vivo<\/jats:italic> animal studies. Therefore, several of these molecules can be useful as lead compounds and some of them can even have the potential to be considered in the future clinical candidates for the treatment of hyperuricemia.<\/jats:p>","DOI":"10.1155\/2020\/9531725","type":"journal-article","created":{"date-parts":[[2020,2,25]],"date-time":"2020-02-25T23:32:02Z","timestamp":1582673522000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":17,"title":["From Xanthine Oxidase Inhibition to <i>In Vivo<\/i> Hypouricemic Effect: An Integrated Overview of <i>In Vitro<\/i> and <i>In Vivo<\/i> Studies with Focus on Natural Molecules and Analogues"],"prefix":"10.1155","volume":"2020","author":[{"given":"Jo\u00e3o 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