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Drug Information Portal (U.S. National Library of Medicine) - Bilobalide

PubChem Compound Summary - Bilobalide

Drug Bank - Bilobalide

KEGG (Kyoto Encyclopedia of Genes and Genomes) -  Bilobalide -  Bilobalide - Bilobalide
The sesquiterpene trilactone bilobalide is one of the active constituents of the 50:1 Ginkgo biloba leaf extract widely used to enhance memory and learning. Bilobalide was found to antagonise the direct action of g-aminobutyric acid (GABA) on recombinant a1h2g2L GABAA receptors. The effect of bilobalide on the direct action of GABA at a1h2g2L GABAA receptors expressed in Xenopus laevis oocytes using two-electrode voltage-clamp method was evaluated and compared with the effects of the classical GABAA receptor competitive antagonist bicuculline and noncompetitive antagonist picrotoxinin. Bilobalide (IC50 = 4.6F0.5 AM) was almost as potent as bicuculline and pictrotoxinin (IC50 = 2.0F0.1 and 2.4F0.5 AM, respectively) at a1h2g2L GABAA receptors against 40 AM GABA (GABA EC50). While bilobalide and picrotoxinin were clearly noncompetitive antagonists, the potency of bilobalide decreased at high GABA concentrations suggesting a component of competitive antagonism.
Ginkgo biloba, the ginkgo tree, is the oldest living tree, with a long history of use in traditional Chinese medicine. In recent years, the leaf extracts have been widely sold as phytomedicine in Europe and as a dietary supplement worldwide. Effects of Ginkgo biloba extracts have been postulated to include improvement of memory, increased blood circulation, as well as beneficial effects to sufferers of Alzheimer's disease. The most unique components of the extracts are the terpene trilactones, that is, ginkgolides and bilobalide. These structurally complex molecules have been attractive targets for total synthesis. Terpene trilactones are believed to be partly responsible for the neuromodulatory properties of Ginkgo biloba extracts, and several biological effects of the terpene trilactones have been discovered in recent years, making them attractive pharmacological tools that could provide insight into the effects of Ginkgo biloba extracts.

The medical benefits of GINKGO BILOBA EXTRACT rely primarily on two groups of active components: the ginkgo flavone glycosides and the terpene lactones. The 24% ginkgo flavone glycoside designation on GBE labels indicates the carefully measured balance of bioflavonoids. These bioflavonoids are primarily responsible for GBE's antioxidant activity and ability to inhibit platelet aggregation. These two actions may help GBE prevent circulatory diseases such as atherosclerosis and support the brain and central nervous system. The unique terpene lactone components found in GBE, known as ginkgolides and bilobalide typically make up 6% of the extract. They are associated with increased circulation to the brain and other parts of the body as well as exert a protective action on nerve cells. Ginkgolides may improve circulation and inhibit platelet-activating factor. Bilobalide protects the cells of the nervous system.





Yellow Powder

Assay (HPLC)


27.0% min



7.0% min



1.2% min


4.0% max

Residual solvent

0.5% max


4.0% max

Heavy metals

10ppm max

Total Microbiological plate coun

max 1,000 per gram


max 100 per gram