REVIEW Bilobalide is a naturally occurring biologically active terpenic trilactone or sesquiterpenoid present in the leaves of Ginkgo biloba. The leaves and their extracts are used as a herbal supplement to boost memory and prevent dementia. Bilobalide is important for producing several of the effects of Gingko biloba extracts, and it has neuroprotective effects, as well as 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 an antagonist 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 alpha1.
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Umegaki K, Taki Y, Endoh K, Taku K, Tanabe H, Shinozuka K, Sugiyama T. Bilobalide in Ginkgo biloba extract is a major substance inducing hepatic CYPs. J Pharm Pharmacol. 2007 Jun;59(6):871-7.
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Huang SH, Duke RK, Chebib M, Sasaki K, Wada K, Johnston GA. Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1 beta2 gamma2L GABA(A) receptors. Eur J Pharmacol. 2003 Mar 7;464(1):1-8.
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