Ginkgolide B

Ginkgolide B (BN-52021), a terpene lactone, is a potent platelet activating factor antagonist. Ginkgolide B protects endothelial cells via the activation of PXR from injuries induced by xeno- and endobiotics. Ginkgolide B can pass through the brain-blood barrier. Ginkgolide B has anti-oxidant, anti-inflammatory, anti-tumor, and anti-apoptotic activity. Ginkgolide B has marked neuroprotective effects against ischemia-induced impairments^[1][2]. In Vitro:Ginkgolide B (BN-52021; 30-150 μM; 24 h) inhibits the up-regulation of VCAM-1 and E-selectin protein expression induced by TNF-α (10 ng/mL)^[1].
Ginkgolide B (30-150 μM; 24, 48 h) increases CYP3A4 mRNA and MDR1 expression^[1].
Ginkgolide B (30-150 μM; pretreated for 24 h) reduces Staurosporine-induced (500 nM; 6 h) apoptosis compared with the positive controls, which exhibited marked apoptosis compared with negative controls. Ginkgolide B does not affect Doxorubicin (5 μM; 24 h) induced apoptosis^[1].
Ginkgolide B regulates PXR activity and does not affect PXR expression^[1].
In Vivo:Ginkgolide B (BN-52021; 20 mg/kg; Intraperitoneally; immediately and 6 hours after ischemia, and thereafter once daily; 14 days) decreases the neurological deficit score^[2].