Drug intelligence / Profile preview

vitexin

Development stage
Phase 1
Lead developer
Hospital of Traditional Medicine
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Vitexin is a naturally occurring flavone glycoside, specifically apigenin 8-C-glucoside, found in various medicinal and food plants such as passion flower, bamboo leaves, and pearl millet. It exhibits a wide range of pharmacological effects including antioxidant, anti-inflammatory, anticancer (antineoplastic), antinociceptive (pain-relieving), neuroprotective, anxiolytic (anxiety-reducing), anticonvulsant, and platelet aggregation inhibitory activities. Mechanistically, vitexin acts through multiple pathways such as inhibition of alpha-glucosidase enzyme activity[1], modulation of GABAergic neurotransmission[5], suppression of oxidative stress via upregulation of antioxidant genes like Nuclear factor erythroid 2–related factor 2 (Nrf2) and Heme oxygenase 1 (HO-1)[6][7], inhibition of pro-inflammatory signaling pathways including p38 mitogen activated protein kinase (p38 MAPK) and Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB)[8], reduction in beta-amyloid formation by inhibiting Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) (β-secretase)[6], and protection against neurodegeneration. Vitexin is under investigation for its potential use in neurological disorders (such as epilepsy and anxiety), cancer prevention/treatment, cardiovascular protection under high glucose conditions (e.g., diabetes-related vascular inflammation), memory impairment, cerebral ischemia/reperfusion injury, myocardial injury, respiratory injury due to oxidative stress-related diseases[4][5][6][7][8]. It is not an approved pharmaceutical drug but is considered investigational or used as a dietary supplement ingredient.

Other names
apigenin 8-C-glucosideapigenin8-C-glucosideapigenin-8-C-glucoside
02

Targets

Sucrase-IsomaltaseAβ (Amyloid-beta peptides and aggregates)BACE1 (Beta-site APP-cleaving enzyme 1)HMOX1 (Heme oxygenase 1)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)NF-κBMAPK14 (p38 mitogen-activated protein kinase alpha)GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)

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