Bilobalide - CAS 33570-04-6
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Not Intended for Therapeutic Use. For research use only.
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Bilobalide is a biologically active terpenic trilactone present in Ginkgo biloba.
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1.Current Perspectives on the Beneficial Role of Ginkgo biloba in Neurological and Cerebrovascular Disorders.
Nash KM1, Shah ZA2. Integr Med Insights. 2015 Nov 9;10:1-9. doi: 10.4137/IMI.S25054. eCollection 2015.
Ginkgo biloba extract is an alternative medicine available as a standardized formulation, EGb 761(®), which consists of ginkgolides, bilobalide, and flavonoids. The individual constituents have varying therapeutic mechanisms that contribute to the pharmacological activity of the extract as a whole. Recent studies show anxiolytic properties of ginkgolide A, migraine with aura treatment by ginkgolide B, a reduction in ischemia-induced glutamate excitotoxicity by bilobalide, and an alternative antihypertensive property of quercetin, among others. These findings have been observed in EGb 761 as well and have led to clinical investigation into its use as a therapeutic for conditions such as cognition, dementia, cardiovascular, and cerebrovascular diseases. This review explores the therapeutic mechanisms of the individual EGb 761 constituents to explain the pharmacology as a whole and its clinical application to cardiovascular and neurological disorders, in particular ischemic stroke.
2.GABAA receptor cysteinyl mutants and the ginkgo terpenoid lactones bilobalide and ginkgolides.
Ng CC1, Duke RK1, Hinton T1, Johnston GA2. Eur J Pharmacol. 2016 Apr 15;777:136-46. doi: 10.1016/j.ejphar.2016.03.007. Epub 2016 Mar 4.
The terpenoid lactones from Ginkgo biloba, bilobalide and ginkgolides, have been shown to act as negative modulators at α1β2γ2L GABAA receptors. They have structural features similar to those of the chloride channel blocker picrotoxinin. Unlike picrotoxinin, however they are not known to produce convulsant effects. Using two-electrode voltage clamp electrophysiology, this study compared the effect of mutation of 2', 6' and 15' pore facing M2 domain residues to cysteine on the action of picrotoxinin, bilobalide and ginkgolides at α1β2γ2L GABAA receptors expressed in Xenopus oocytes. Picrotoxinin was affected by mutation differently from the ginkgo terpenoid lactones. Although some of these compounds were affected by the mutation at same position and/or subunit, the changes in their potency were found to be dissimilar. The results suggest that the intracellular pore binding site for picrotoxinin, bilobalide, ginkgolide A, ginkgolide B and ginkgolide C is comprised of 2'β-6'β6'γ, 2'α2'β-6'α6'β, 2'α2'β2'γ-6'β6'γ, 2'α, 2'β2'γ-6'β and 2'α2'β, respectively.
3.Noncompetitive Inhibition of 5-HT3 Receptors by Citral, Linalool, and Eucalyptol Revealed by Nonlinear Mixed-Effects Modeling.
Jarvis GE1, Barbosa R1, Thompson AJ2. J Pharmacol Exp Ther. 2016 Mar;356(3):549-62. doi: 10.1124/jpet.115.230011. Epub 2015 Dec 15.
Citral, eucalyptol, and linalool are widely used as flavorings, fragrances, and cosmetics. Here, we examined their effects on electrophysiological and binding properties of human 5-HT3 receptors expressed in Xenopus oocytes and human embryonic kidney 293 cells, respectively. Data were analyzed using nonlinear mixed-effects modeling to account for random variance in the peak current response between oocytes. The oils caused an insurmountable inhibition of 5-HT-evoked currents (citral IC50 = 120 µM; eucalyptol = 258 µM; linalool = 141 µM) and did not compete with fluorescently labeled granisetron, suggesting a noncompetitive mechanism of action. Inhibition was not use-dependent but required a 30-second preapplication. Compound washout caused a slow (∼180 seconds) but complete recovery. Coapplication of the oils with bilobalide or diltiazem indicated they did not bind at the same locations as these channel blockers. Homology modeling and ligand docking predicted binding to a transmembrane cavity at the interface of adjacent subunits.
4.Effect of Ginkgo Leaf Tablets on the Pharmacokinetics of Amlodipine in Rats.
Wang R1, Zhang H2, Sun S2, Wang Y1, Chai Y3, Yuan Y4. Eur J Drug Metab Pharmacokinet. 2015 Dec 9. [Epub ahead of print]
BACKGROUND AND OBJECTIVE: Ginkgo leaf tablet (GLT) is an effective traditional Chinese multi-herbal formula, which is often combined with amlodipine for treating senile hypertension in clinic. The aim of this study was to study the pharmacokinetics of amlodipine after oral administration of amlodipine and GLT and to investigate the potential for pharmacokinetic herb-drug interactions between GLT and amlodipine in rats.
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CAS 33570-04-6 Bilobalide

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