Bergapten

Bergapten is a furanocoumarin derivative that has been found in grapefruit peel oil and has diverse biological activities.^1,2,3,4 It decreases the viability of DLD-1 and LoVo colorectal cancer cells in a concentration-dependent manner, halts the cell cycle at the G₀/G₁ and sub-G₁ phases, and induces apoptosis when used at a concentration of 50 μM.² Bergapten has photosensitizing activity and increases the number of sunburn cells in guinea pig skin in response to UVA radiation.³ It increases the pain threshold in assays for mechanical, cold, and hot allodynia, as well as mechanical hyperalgesia, in a rat model of vincristine-induced neuropathic pain when administered at a dose of 10 mg/kg. ⁴ Bergapten inhibits vincristine-induced increases in plasma TNF-α and IL-1β levels and decreases in glutathione (GSH) levels in the spinal cord and sciatic nerve in rats. It also inhibits the cytochrome P450 (CYP) isoform CYP3A4 with IC₅₀ value of approximately 25 μM in human liver microsomes.¹

WARNING This product is not for human or veterinary use.

1. Ho, P.C., and Saville, D.J. Inhibition of human CYP3A4 activity by grapefruit flavonoids, furanocoumarins and related compounds. J. Pharm. Pharm. Sci. 4(3), 217-227 (2001).

2. Lin, C.P., Lin, C.S., Lin, H.H., et al. Bergapten induces G₁ arrest and pro-apoptotic cascade in colorectal cancer cells associating with p53/p21/PTEN axis. Environ. Toxicol. 34(3), 303-311 (2019).

3. Yasui, Y., and Hirone, T. Action spectrum for bergamot-oil phototoxicity measured by sunburn cell counting. J. Dermatol. 21(5), 319-322 (1994).

4. Singh, G., Singh, A., Singh, P., et al. Bergapten ameliorates vincristine-induced peripheral neuropathy by inhibition of inflammatory cytokines and NFκB signaling. ACS Chem. Neurosci. 10(6), 3008-3017 (2019).