Citropten (Synonyms: 5,7-Dimethoxycoumarin)

Citropten is a coumarin that has been found in bergamot extracts and has diverse biological activities.1,2,3,4 It reduces IL-8 mRNA accumulation induced by TNF-α or heat-inactivated P. aeruginosa in IB3-1 cells derived from cystic fibrosis patients.1 Citropten induces cell cycle arrest at the G1 phase and inhibits proliferation of A375, MCF-7, PC3, and SW620 cancer cells (IC50s = 250-325 μM).2 It is active against various Gram-positive and Gram-negative bacteria (MICs = 16-64 μg/ml).3 Citropten increases prothrombin time in isolated rat platelet-poor plasma. In vivo, citropten (10 mg/kg) prevents decreases in locomotor activity and increases in hippocampal monoamine oxidase A (MAO-A) levels in a rat model of chronic mild stress-induced depression.4

|1. Borgatti, M., Mancini, I., Bianchi, N., et al. Bergamot (Citrus bergamia Risso) fruit extracts and identified components alter expression of interleukin 8 gene in cystic fibrosis bronchial epithelial cell lines. BMC Biochem. 12, 15 (2011).|2. Alesiani, D., Cicconi, R., Mattei, M., et al. Cell cycle arrest and differentiation induction by 5,7-dimethoxycoumarin in melanoma cell lines. Int. J. Oncol. 32(2), 425-434 (2008).|3. Rosselli, S., Maggio, A., Bellone, G., et al. Antibacterial and anticoagulant activities of coumarins isolated from the flowers of Magydaris tomentosa. Planta Med. 73(2), 116-120 (2006).|4. Yang, W., and Wang, H. 5,7-Dimethoxycoumarin prevents chronic mild stress induced depression in rats through increase in the expression of heat shock protein-70 and inhibition of monoamine oxidase-A levels. Saudi J. Biol. Sci. 25(2), 253-258 (2018).