Bilobalide

SKU: orb1222355

Description

Bilobalide is a biologically active terpenic trilactone present in Ginkgo biloba. Bilobalide is important for producing several of the effects of Gingko biloba extracts. It has neuroprotective effects, as well as effects inducing the liver enzymes CYP3A1 and 1A2, which may be partially responsible for interactions between gingko and other herbal medicines or pharmaceutical drugs. Bilobalide has recently been found to be a negative allosteric modulator at the GABAA and GABAA-rho receptors. Of GABAA, it may possibly be selective for the subunits predominantly implicated in cognitive and memory functioning such as α1.

Key Properties

• CAS Number: 33570-04-6
• MW: 326.3
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₈O₈
• SMILES: C1(=O)O[C@H]2[C@@]3([C@]41[C@H](C[C@@]3(O)C(C)(C)C)OC(=O)C4)[C@H](C(=O)O2)O
• Target: AChR
• Solubility: DMSO : ≥ 100 mg/mL; 306.47 mM

Bioactivity

• 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. Animal model: Male Wistar rats (250-350 g). 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.
• 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. 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. Bilobalide (5 and 10 μM; 24 h) treatment dose-dependently increases levels of p-Akt (Ser473 and Thr308) in SH-SY5Y cells. 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

(-)-Bilobalide | Bilobalide | Bilobalid

Quick Database Links

Gene Symbol

AChR