“Nutraceuticals” are food-derived products largely used for their presumed healthpromoting
or disease-preventing effects. In the recent years, many efforts have been aimed at
assessing nutraceutical efficacy and safety, but these factors are difficult to address because
of the complex chemical compositions and multiple mode of actions. Thus, the study of nutraceutical
ingredients poses several challenges for the medicinal chemistry field, some of
which are related to extraction and chemical characterization, some to in vitro and in vivo
bioactivity evaluation, and some to the bioavailability and interaction of these natural mixtures
with organs and microbiota. Furthermore, because of their nature as medicinal and food
products, these nutraceuticals can also be considered as a valuable source of new “lead compounds”,
creating the opportunity to discover new classes of therapeutic agents. This review
provides information on these themes, showing the new challenges that comprehensive medicinal
chemistry research is called to answer in the field of nutraceuticals.
Keywords: Nutraceuticals, natural products, metabolomics, antioxidants, flavonoids, microbiota.
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