Drug intelligence / Profile preview

esculetin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intraperitoneal (experimental)
01

Overview

Esculetin is a naturally occurring hydroxycoumarin (6,7-dihydroxycoumarin) found in several plants including chicory (*Cichorium intybus*), *Bougainvillea spectabilis*, *Artemisia capillaris*, among others. It is a small aromatic molecule with a benzene ring fused to a lactone, notable for its antioxidant, anti-inflammatory, anti-arthritic, antifungal, antidiabetic, anticancer, neuroprotective, cardiovascular protective, and antimicrobial properties[2][3][5][6][7][8]. Its mechanism of action involves inhibition of pro-inflammatory cytokines (including TNF-α, IL-1β, IL-6) and key enzymes such as matrix metalloproteinases (MMP-1, MMP-3, MMP-13), cyclooxygenase (COX-2), lipoxygenases (5-, 12-LO), and signaling pathways like NF-κB and Akt[1][6]. Esculetin's pharmacological activities are being investigated for diseases such as arthritis, cancer, diabetes, atherosclerosis, Alzheimer's disease, Parkinson's disease, and hepatic disorders[1][3][5]. It is not an approved pharmaceutical drug but is widely researched for therapeutic applications[3][7].

Other names
6,7-dihydroxycoumarinaesculetincichorigeninesculetolesculatinasculetinecichoriin agluconesculin aglucon6,7-dihydroxy-2-benzopyrone
02

Targets

ALOX12 (Arachidonate 12-lipoxygenase, 12S type)C/EBPβ (CCAAT/enhancer-binding protein beta)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)MMP9 (Matrix metalloproteinase-9)IL1B (Interleukin-1 beta)IL-6 (Interleukin 6)MMP1 (Matrix metalloproteinase-1)MMP13 (Matrix metalloproteinase-13)MMP3 (Matrix metalloproteinase-3)RELA (Nuclear Factor Kappa B Subunit p65)AKT (RAC-alpha serine/threonine-protein kinase)TNFA (Tumor necrosis factor alpha (soluble))

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