Drug intelligence / Profile preview

auraptene

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Auraptene (7-geranyloxycoumarin) is a naturally occurring monoterpene coumarin ether, primarily isolated from citrus fruits (e.g., oranges, grapefruits, lemons) and some edible plants of the *Ferula* genus. It is structurally derived from coumarin, with a geranyl group attached at position 7. Auraptene exhibits a broad range of biological activities, including potent anti-inflammatory, anticancer, anti-bacterial, antioxidant, neuroprotective, and hepatoprotective properties. Its anticancer effects have been demonstrated in vitro (e.g., inhibition of multiple cancer cell lines, induction of apoptosis, downregulation of BCL2, upregulation of p53) and in vivo, with proposed mechanisms involving modulation of leukocyte activation, induction of phase II detoxifying enzymes, and inhibition of enzymes such as β-secretase (BACE1). It shows promising therapeutic value for chronic illnesses such as hypertension, nonalcoholic fatty liver disease, cystic fibrosis, and potentially neurodegenerative diseases like Alzheimer's disease. Auraptene is under active investigation as a chemopreventive agent, often in dietary and nutraceutical research[1][5][7][3][4][6].

Other names
7-geranyloxycoumarin7-geranyloxycoumarineaurapten7-O-geranylumbelliferone(E)-7-((3,7-Dimethylocta-2,6-dien-1-yl)oxy)-2H-chromen-2-one7-((2E)-3,7-dimethylocta-2,6-dienoxy)chromen-2-one7-(geranyloxy)coumarin7-{[(2E)-3,7-dimethylocta-2,6-dien-1-yl]oxy}-2H-chromen-2-one7-(((2E)-3,7-dimethylocta-2,6-dien-1-yl)oxy)-2H-chromen-2-oneO-geranylumbelliferoneCoumarin, 7-(geranyloxy)-
02

Targets

BCL-2 (BCL-2 family)TP53 (Cellular Tumor Antigen p53 R175H)BACE1 (Beta-site APP-cleaving enzyme 1)

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