bergapten

Bergapten, also known as 5-methoxypsoralen, is a naturally occurring furanocoumarin compound found in various plants, especially those in the Apiaceae (carrot) and Rutaceae (citrus) families. It is a linear furanocoumarin and was first isolated from bergamot essential oil. Bergapten acts primarily as a photosensitizing agent and has been used in oral photochemotherapy for conditions such as psoriasis due to its efficacy and relatively low risk of phototoxic or drug-insensitive reactions compared to other agents like 8-methoxypsoralen[1][4]. Its mechanism of action involves photosensitization—upon exposure to ultraviolet light, it intercalates into DNA and inhibits processes such as RNA synthesis, leading to therapeutic effects but also potential toxicity[1][4]. Preclinical studies have shown that bergapten exhibits anti-inflammatory, antibacterial, anticancer, antioxidant, neuroprotective, hypolipemic (lipid-lowering), antidiabetic, analgesic, anticoagulant, hepatoprotective and anticonvulsant properties[4][5]. It has demonstrated inhibitory effects on enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), monoamine oxidase (MAO), cyclooxygenase (COX), topoisomerase I and 5-lipoxygenase[4][6]. Bergapten can cross the blood–brain barrier. Its clinical use is limited by its phototoxicity when combined with UV light; however this property is exploited therapeutically in photochemotherapy for skin diseases like psoriasis[1][6]. Bergapten is under investigation for additional indications including diabetes-induced osteoporosis, epilepsy, Alzheimer's disease and cancer; however further studies are needed to clarify its molecular targets and safety profile[5].

Brand names

HeraclinMajudinPsoradermPentadermGeralen

Other names

5-methoxypsoralen5 methoxypsoralenBP