Bilobalide is a biologically active terpenic trilactone present in Ginkgo biloba.
Bilobalide/白果内酯 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Primary neurons
12 μg/ml
6 hours
Pretreatment with Bilobalide significantly protected neurons against NMDA-induced excitotoxicity but failed to protect against oxidative stress induced by t-BuOOH and H2O2.
Neurobiol Dis. 2012 Apr;46(1):180-9.
APP/PS1 neurons
5 μM
Bilobalide-pretreated astrocytes rescued synaptic protein expression, cell viability, and ROS levels in APP/PS1 neurons.
Transl Psychiatry. 2021 Oct 20;11(1):542.
Primary astrocytes
1, 5, 10 μM
24 hours
Bilobalide induces the expression of NEP, IDE, and MMP2 to facilitate Aβ clearance.
Transl Psychiatry. 2021 Oct 20;11(1):542.
Rat cortical neurons
50, 100 μM
12 hours
To evaluate the protective effects of Bilobalide on oxygen-glucose deprivation/reoxygenation (OGD/R)-induced neuronal injury. Results showed that Bilobalide pretreatment significantly increased cell viability, reduced LDH release, and down-regulated the expression of NO, TNF-α, IL-1β, p-JNK1/2, and p-p38 MAPK.
J Neuroinflammation. 2014 Sep 26;11:167.
HepG2-CYP2D6*10
100 μmol/L
90 min
Bilobalide competitively inhibited the catalytic activity of CYP2D6*1 and CYP2D6*10 with an inhibition rate >50%.
Acta Pharmacol Sin. 2014 May;35(5):685-96.
HepG2-CYP2D6*1
100 μmol/L
90 min
Bilobalide competitively inhibited the catalytic activity of CYP2D6*1 and CYP2D6*10 with an inhibition rate >50%.
Acta Pharmacol Sin. 2014 May;35(5):685-96.
Bilobalide/白果内酯 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Male Kunming mice
Scopolamine-induced memory impairment model
Intragastric administration
10 mg/kg, 20 mg/kg, 30 mg/kg
Once daily for 30 days
Ameliorate scopolamine-induced learning and memory impairment in young mice
Neurosci Bull. 2009 Aug;25(4):203-8
C57BL/6 mice
Transient middle cerebral artery occlusion model
Oral
6 mg/kg
Once daily for 7 days
Pretreatment with Bilobalide significantly reduced infarct volumes and improved neurologic deficit scores.
Neurobiol Dis. 2012 Apr;46(1):180-9.
APP/PS1 mice
Alzheimer's disease model
Intraperitoneal injection
0.5 mg/kg
Once a week for 4 weeks
Bilobalide reduced Aβ levels and inflammatory cytokines (TNF-α, IL-1β, and IL-6), increased NEP, IDE, and MMP2 expression, and improved synaptic protein expression.
Transl Psychiatry. 2021 Oct 20;11(1):542.
Mice
CF-1 mice
Oral
30 mg/kg, 100 mg/kg, 300 mg/kg
Single dose
Evaluate the convulsant effects of Bilobalide
Biochem Pharmacol. 2018 Sep;155:61-70
Male Sprague-Dawley rats
Middle cerebral artery occlusion/reperfusion (MCAO/R) model
Intraperitoneal injection
5, 10 mg/kg
Single administration, lasting 24 hours
To evaluate the neuroprotective effects of Bilobalide on cerebral ischemia-reperfusion injury. Results showed that Bilobalide pretreatment significantly improved neurological scores, reduced infarct volume and brain edema, increased SOD activity, decreased levels of MDA, NO, TNF-α, and IL-1β, and down-regulated the expression of p-JNK1/2 and p-p38 MAPK.
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