A number of prenylated phenols, mainly flavonoids, have been identified as active constituents of medicinal plants. Due to their beneficial effects on human health, this class of compounds has received a great deal of attention, not only from the pharmaceutical industry, but also from
other areas of applied sciences, including the food, brewing, and cosmetics industries. The addition of prenyl residues through the activity of isoprenyltransferases, the key biosynthetic enzymes for these plant metabolites, endows flavonoids with a variety of biological activities, mostly
due to improved interaction with membranes and proteins. The role of prenylated flavonoids in plants correlates with their activities as antioxidant or anti-infectious agents. In connection with these effects, these compounds have been evaluated for multiple potential uses, e.g. as antibacterial,
antiprotozoal, antifungal, anti-inflammatory, antitumor, estrogenic, antidiabetic, or antithrombotic agents, among others. The present review, in principle focused on phenolic derivatives containing a non-cyclized isoprenyl chain, discusses the most relevant pharmacological reports for the
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