Bergamottin

Bergamottin is a naturally occurring furanocoumarin compound found primarily in grapefruit, pomelo, and the bergamot orange. It was first isolated from the oil of the bergamot orange (Citrus bergamia), which gives it its name[1][4][7]. Bergamottin is best known as a potent inhibitor of several cytochrome P450 enzymes, especially CYP3A4, but also CYP1A2, 2A6, 2C9, 2C19, 2D6, and 2E1[1][2][3]. By inhibiting these enzymes in the gut and liver, it can significantly increase the bioavailability of drugs metabolized by these pathways—this underlies the well-known "grapefruit effect," where consumption of grapefruit or its juice can lead to elevated blood levels and increased side effects for certain medications[1][3]. Beyond its role in drug interactions, research has shown that bergamottin possesses anti-oxidative, anti-inflammatory (notably via inhibition of NF-κB signaling), antiviral (e.g., Junin virus inhibition), and anticancer properties demonstrated in vitro and in vivo models[2][5][8]. Its mechanism includes direct enzyme inhibition as well as modulation of cellular signaling pathways such as SIRT1/NF-κB. While not currently approved or marketed as a pharmaceutical drug on its own for any indication, there is ongoing research into potential therapeutic applications including cancer chemoprevention and adjunctive use to enhance oral bioavailability of other drugs.

Other names

5-geranoxypsoralen