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].
IC50 & Target
Human Endogenous Metabolite
体外研究 (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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis
Cell Line:
SH-SY5Y cells
Concentration:
5 and 10 μM
Incubation Time:
24 hours
Result:
Induced a significant increase in levels of p-Akt (Ser473 and Thr308).
体内研究 (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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Wistar rats (250-350 g)[1]
Dosage:
20 mg/kg
Administration:
I.p. injection 60 min before NMDA infusion
Result:
Lowered basal choline efflux only slightly (by 7%) but fully antagonized the NMDA-induced increase of choline release. The convulsive effect of NMDA was almost completely suppressed.
分子量
326.30
Formula
C15H18O8
CAS 号
33570-04-6
中文名称
白果内酯
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. O Weichel, et al. Bilobalide, a constituent of Ginkgo biloba, inhibits NMDA-induced phospholipase A2 activation and phospholipid breakdown in rat hippocampus. Naunyn Schmiedebergs Arch Pharmacol. 1999 Dec;360(6):609-15.
[2]. Chun Shi, et al. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Apoptosis. 2010 Jun;15(6):715-27.