Drug intelligence / Profile preview

esculin

Development stage
Phase 4
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Topical, Rectal
01

Overview

Esculin is a natural hydroxycoumarin glycoside found in horse chestnut and other plants. It is the 6-O-beta-D-glucoside of esculetin. Esculin has been used as a vasoprotective agent to improve capillary permeability and fragility, and it exhibits antioxidant, anti-inflammatory, and potential anti-cancer properties[2][3][4][5][8]. Its mechanism of action includes inhibition of catabolic enzymes such as hyaluronidase and collagenase (preserving perivascular connective tissue), direct antioxidant effects, modulation of oxidative stress-related enzyme activities (such as SOD and GSH), attenuation of NF-κB signaling activity, promotion of PPAR-γ nuclear localization[4][5], and inhibition of the PI3K/Akt pathway in cancer cells[6]. Esculin is also used in microbiology for bacterial identification due to its hydrolysis by certain bacteria[2]. Oral bioavailability is low (~0.62%), but it can be absorbed when applied to open wounds or mucosa[4].

Other names
æsculinaesculin6-beta-glucoside-7-hydroxycoumarin
02

Targets

TNFA (Tumor necrosis factor alpha (soluble))RELA (Nuclear Factor Kappa B Subunit p65)MMP12 (Macrophage Metalloelastase)GAPDH (Glyceraldehyde-3-phosphate dehydrogenase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)HYAL (Hyaluronidase family (HYAL))PPARG (Peroxisome proliferator-activated receptor gamma)

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