Ginkgolide B: Origin, Pharmacokinetics and Neuroprotective Effects

General Description

Ginkgolide B, derived from Ginkgo biloba, showcases potent neuroprotective properties, particularly in treating ischemic strokes. Its pharmacokinetic studies highlight efficient absorption and distribution in the body, contributing to its health benefits. Research underscores Ginkgolide B's ability to reduce infarct size, brain edema, and enhance neuronal survival in stroke models. The compound regulates neurotransmitter levels, ion balance, and exerts antioxidant, anti-inflammatory, and anti-apoptotic effects. Notably, its antagonist action at the PAF receptor plays a crucial role in neuroprotection. Overall, Ginkgolide B emerges as a promising natural compound with therapeutic potential for ischemic stroke by targeting diverse cellular pathways.

Figure 1. Ginkgolide B

Origin

Ginkgolide B is a bioactive compound derived from Ginkgo biloba, a prominent Chinese medicinal plant. Ginkgo biloba is renowned for its various health benefits, including enhancing cognitive function, combating different types of cancer, and improving cardiovascular health. Recent research has predominantly focused on the pharmacological properties of Ginkgolide B, a specific diterpene found in Ginkgo biloba. Studies have established the therapeutic potential of Ginkgolide B in treating both ischemic and hemorrhagic strokes. The protective mechanisms of Ginkgolide B against stroke involve its modulation of inflammatory gene expression, suppression of NF-κB and PI3K/Akt pathways, inhibition of toll-like receptor 4 (TLR4)/nuclear factor kappa-B, improvement of vascular function, as well as its antioxidant and antiapoptotic effects. These findings underscore the significance of Ginkgolide B as a promising natural compound with neuroprotective properties derived from Ginkgo biloba. ¹

Pharmacokinetics

Ginkgolide B exhibits significant pharmacokinetic properties that influence its potential health effects. Pharmacokinetics refers to the study of how a substance is absorbed, distributed, metabolized, and excreted in the body over time. Research conducted on 12 healthy volunteers revealed crucial insights into the pharmacokinetics of Ginkgolide B. After single-dose administration of Ginkgo biloba extract via oral and intravenous routes, the compound exhibited high bioavailability. Bioavailability coefficients, such as the area under the curve (AUC), indicated favorable values for Ginkgolide B, suggesting efficient absorption and distribution within the body. In a more recent study involving 24 volunteers, the pharmacokinetics of commercially available Ginkgolide B preparations were investigated. The study assessed plasma concentrations of Ginkgolides A, Ginkgolide B, and bilobalide following oral administration of the preparations. The results indicated that these bioactive compounds were bioavailable across different formulations, as evidenced by comparable pharmacokinetic parameters, particularly the total AUC. Furthermore, the concentrations of Ginkgolide B and other bioactive compounds in the preparations were determined, highlighting their presence and potential for systemic distribution within the body. Overall, these studies underscore the favorable pharmacokinetic profile of Ginkgolide B, indicating efficient absorption, distribution, and bioavailability, which are essential factors contributing to its potential health benefits. These findings provide valuable insights for further understanding the therapeutic implications of Ginkgolide B in clinical applications. ²

Neuroprotective Effects

Ginkgolide B has garnered significant attention for its neuroprotective effects, particularly in the context of ischemic stroke. Numerous studies across various experimental models have demonstrated the efficacy of Ginkgolide B in mitigating the detrimental effects of cerebral ischemia. Research on animal models, including mice and rats subjected to different ischemic stroke conditions such as middle cerebral artery occlusion (tMCAO and pMCAO), photochemically induced thrombotic cerebral ischemia, and intracerebral hemorrhage (SAH), have consistently shown that pre- and post-treatments with Ginkgolide B lead to a reduction in infarct size, brain edema, and an extension of neuronal cell survival. Moreover, Ginkgolide B treatment has been associated with the normalization of neurotransmitter levels in the affected brain regions, such as noradrenaline, dopamine, and 5-hydroxytryptamine, demonstrating its regulatory effects on neurotransmission. Additionally, Ginkgolide B has shown the ability to modulate ion levels, particularly sodium, calcium, and water, in the penumbra region following ischemic insults, highlighting its role in maintaining cellular homeostasis. The neuroprotective mechanisms of Ginkgolide B involve its potent antioxidant, anti-inflammatory, and anti-apoptotic activities, along with its ability to mitigate mitochondrial dysfunction and inhibit specific proteases. Furthermore, Ginkgolide B's antagonist action at the platelet-activating factor (PAF) receptor is considered a key mode of action in exerting its neuroprotective effects. Overall, the multifaceted neuroprotective properties of Ginkgolide B underscore its potential as a therapeutic agent for ischemic stroke by targeting various cellular pathways involved in neuronal damage and survival. ³

Reference

1. Woelkart K, Feizlmayr E, Dittrich P, et al. Pharmacokinetics of bilobalide, ginkgolide A and B after administration of three different Ginkgo biloba L. preparations in humans. Phytother Res. 2010;24(3):445-450.

2. Tang C, Wei X, Yin C. Analysis of ginkgolides and bilobalide in Ginkgo biloba L. extract injections by high-performance liquid chromatography with evaporative light scattering detection. J Pharm Biomed Anal. 2003;33(4):811-817.

3. Nabavi SM, Habtemariam S, Daglia M, et al. Neuroprotective Effects of Ginkgolide B Against Ischemic Stroke: A Review of Current Literature. Curr Top Med Chem. 2015;15(21):2222-2232.

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