Drug intelligence / Profile preview

ginkgolide b

Development stage
Phase 1
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Ginkgolide B is a diterpene lactone and the most potent member of the ginkgolide family, isolated from the leaves of the Ginkgo biloba tree. It is a major active component of standardized Ginkgo biloba extracts (notably EGb 761). Ginkgolide B acts primarily as a potent antagonist of platelet-activating factor (PAF) by binding to and inhibiting the PAF receptor, which underlies its anti-inflammatory, anti-allergic, antioxidant, neuroprotective, and anti-coagulant effects. Additional mechanisms include inhibition of TLR4-mediated inflammatory responses, scavenging free radicals via NF-kB inhibition, modulation of glutamatergic transmission in the central nervous system, reduction in Ca2+-stimulated intracellular events, and promotion of endothelial progenitor cell proliferation through vascular endothelial growth factor (VEGF) pathways. It has been studied for use in migraine prophylaxis as a nutraceutical approach and may have potential anticancer effects by inducing apoptosis or inhibiting oxidative stress generation[1][2][4][5][6].

Other names
ginkgolide B
02

Targets

Glycine receptorMEKNF-κBPTAFR (Platelet-activating factor receptor)TLR4 (Toll-like receptor 4)TUBA (Tubulin alpha/beta dimer)

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