Bilobalide

Bilobalide, a sesquiterpene trilactone constituent of Ginkgo biloba, inhibits the NMDA-induced efflux of choline with an IC₅₀ value of 2.3 µM. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons^[1][2]. In Vitro: Bilobalide (1-100 µM) completely suppresses the NMDA-evoked release of choline in a concentration-dependent manner with IC₅₀ value of 2.3 µM^[1].
Bilobalide (1, 5 and 10 μM) alone for 24 h does not affect cell viability of SH-SY5Y cells. Pre-treatment of cells with Bilobalide concentration-dependently prevents Aβ 1-42-, H₂O₂- and serum deprivation-induced decrease of cell viability, with the best protective effect obtained at 10 μM^[2].
Bilobalide (5 and 10 μM; 24 h) treatment dose-dependently increases levels of p-Akt (Ser473 and Thr308) in SH-SY5Y cells^[2].
In Vivo: Bilobalide (20 mg/kg) completely suppresses the NMDA-induced release of choline in vivo while basal choline levels were not significantly affected. NMDA causes a release of choline in vivo when infused into the hippocampus of freely moving rats by retrograde dialysis. Bilobalide (20 mg/kg i.p.) completely inhibits the effect induced by NMDA^[1].