CAS 145414-76-2: 6′,7′-Dihydroxybergamottin

Applications A minor metabolite of Bergamottin (B318400). Metabolization of Bergamottin by cytochromes P 450 2B6 and 3A5. References Lin, H., et al.: J. Pharmacol. Exp. Ther., 301, 160 (2002), Hesselink, D., et al.: Clin. Pharmacol. Ther., 74, 245 (2003), Evans, D., et al.: Chem. Res. Toxicol., 17, 3 (2004), Friesner, R., et al.: J. Med. Chem., 47, 1739 (2004), Bumpus, N., et al.: Drug Metab. Dispos., 33, 795 (2005),

Bergamottin is a naturally occurring flavonoid that is found in grapefruit and other citrus fruit. It has been shown to inhibit the activity of the P-glycoprotein (P-gp) transporter in human cells, which may lead to drug interactions. A number of analytical methods have been developed for the determination of bergamottin in biological samples such as humans, rat liver microsomes, and natural compounds. Bergamottin has been shown to be a potent inhibitor of cytochrome P450 enzymes and can inhibit skin cancer development in mice by inhibiting the growth of human keratinocytes (HK-2 cells). Bergamottin also inhibits tumorigenesis in mice by decreasing cell proliferation and inducing apoptosis in hk-2 cells.