Bergamottin (CAS 7380-40-7)

Bergamottin, a furanocoumarin present in grapefruit juice, lemon, lime, and bergamot oils, exhibits a wide range of biological activities. In vitro studies have demonstrated that bergamottin hampers the migration and invasion of HT-1080 fibrosarcoma cells at non-toxic concentrations by suppressing the expression of matrix metalloproteinase-9 (MMP-9). Moreover, it displays dose-dependent antiproliferative effects on HepG2 liver, HL-60 leukemia, and BGC-823 gastric cancer cell lines, and triggers cell death in CHO cells upon exposure to near ultraviolet irradiation. Bergamottin acts as an inhibitor of cytochrome P450 isoform 3A4 (CYP3A4), with a Ki value of 7.7 μM, and exhibits mixed inhibition towards simvastatin drug metabolism (Ki = 174 μM). Furthermore, bergamottin has the ability to activate the transcription factor NF-κB, which plays a vital role in regulating inflammation, cell growth, and apoptosis. It can induce apoptosis by activating the caspase-3 signaling pathway. Additionally, bergamottin has demonstrated inhibitory effects on various enzymes, including cytochrome P450 3A4 involved in drug metabolism. It also exhibits inhibitory activity against a range of bacteria, such as Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa.