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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
http://www.ebi.ac.uk/chebi/
- Bilobalide
http://www.ncbi.nlm.nih.gov/
- Bilobalide
http://sydney.edu.au/
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.
http://www.columbia.edu/
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.
Local
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.
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