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Bergaptol is a furanocoumarin that has been found in A. dahurica and has diverse biological activities.1,2,3,4 It inhibits the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 24.92 µM).2 It scavenges DPPH (Item No. 14805) and ABTS (Item No. 27317) radicals in cell-free assays (EC50s = 26.66 and 13.55 µg/ml, respectively).1 Bergaptol reduces the replication of L. donovani, T. b. brucei, and T. cruzi in L6 myoblasts (IC50s = 2.5, 22.1, and 68 µg/ml, respectively).3 It induces cell cycle arrest at the S phase and apoptosis in MCF-7 breast cancer cells in a concentration-dependent manner.4 Bergaptol also decreases the proliferation of HeLa cervical carcinoma and HepG2 liver cancer cells (IC50s = 58.57 and 68.42 µM, respectively).1
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1. Coumarins from the roots of Angelica dahurica with antioxidant and antiproliferative activities. J. Funct. Foods 20, 453-462 (2016).
2. Radical scavenging and cytochrome P450 3A4 inhibitory activity of bergaptol and geranylcoumarin from grapefruit. Bioorg. Med. Chem. 15(11), 3684-3691 (2007).
3. Antitrypanosomal and antileishmanial activities of flavonoids and their analogues: In vitro, in vivo, structure-
4. Antitumor and apoptotic effects of bergaptol are mediated via mitochondrial death pathway and cell cycle arrest in human breast carcinoma cells. Bangladesh J. Pharmacol. 11(2), 489-494 (2016).