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Pharmacological Management of Alzheimer’s Disease
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Rakesh Kumar, Rajan Kumar, Abhinav Anand, Neha Sharma, Navneet Khurana
Ginkgo biloba belongs to family Ginkgoaceae, a member of the gymnosperms. The rest plants of the Ginkgoaceae family are now extinct and found as fossils. Ginkgo biloba is a small tree that originated in China but now planted worldwide as an ornamental plant. It is also cultivated in Korea, France, and the United States. The major chemical constituents present in Ginkgo biloba as the mixture of flavonoids and terpenoids. The dried leaves of Ginkgo biloba contain ginkgolides (A, B, C, J, and M), bilobalide and 0.1–0.25% terpene, and lactones. 30–40% of the mixture is bilobalide whereas ginkgolide A is present in maximum amount and accounts about 30% of the mixture. The nature of ginkgolides is diterpenoid while bilobalide is sesquiterpenoid (Paul, 2002).
Herbs with Antidepressant Effects
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
The leaves of Ginkgo biloba contain a variety of flavonol glycosides, biflavones, proanthocyanidins, alkylphenols, simple phenolic acids, and polyprenols. Some of these substances, such as quercetin, isorhamnetin, myricetin, rutin, luteolin, and kaempferol, are common in medicinal plants. Ginkgo biloba also contains a number of unique phytochemicals, e.g., the terpene trilactones, ginkgolides A, B, C, J, and bilobalide.2
Phytotherapeutic Agents in Epilepsy
Published in Vikas Kumar, Addepalli Veeranjaneyulu, Herbs for Diabetes and Neurological Disease Management, 2018
Bilobalide is a sesquiterpene trilactone isolated from the leaves of Ginkgo biloba L. (Fam. Ginkgoaceae) which shows significant reduction in convulsions induced by 4-O-methylpyridoxine (MPN) or INH in mice. The study indicates that the anticonvulsant effect of bilobalide against MPN-induced convulsions partly involves modulation of hepatic drug-metabolizing enzyme activity leading to accelerated elimination of MPN.73 Further, bilobalide can elevate GABA levels, possibly through potentiation of GABA synthesis.
The effect of intravenous ginkgolide on clinical improvement of patients with acute ischemic stroke
Published in Neurological Research, 2020
Yi Dong, Huiqin Li, Qiang Dong
Ginkgolide (Baiyu®) is consisted with two major components, includes ginkgoid and bilobalide. Early in-vitro studies found that ginkgolide injection could inhibit platelet aggregation and that the antagonism of platelet-activating factor (PAF)-induced platelet aggregation was superior to that of aspirin and clopidogrel [35,36]. Clinically, ginkgolide has been reported the potential efficacy in the treatment of atherosclerotic cerebral infarction, recanalization of occluded basilar arteries and treatment of acute ischemic stroke when given in combination with alteplase (within the thrombolysis time window) [37,38]. Bilobalide has been reported as neuroprotection, maintains the integrity of vascular endothelial cells, promotes angiogenesis and inhibits microglia [39], and numerous studies have demonstrated that bilobalide can attenuate infarct volume, cerebral edema, neuronal damage and neurologic deficits [40,41]. Clinically, a combination of bilobalide with mecobalamin might be associated with a better outcome in the treatment of diabetic peripheral neuropathy than mecobalamin alone [42].
What dominates the changeable pharmacokinetics of natural sesquiterpene lactones and diterpene lactones: a review focusing on absorption and metabolism
Published in Drug Metabolism Reviews, 2021
Ziwei Yu, Ziqiang Chen, Qijuan Li, Ke Yang, Zecheng Huang, Wenjun Wang, Siyu Zhao, Huiling Hu
Diabetes and diabetic nephropathy appear to cause the slower elimination and the more effective absorption of ginkgolide A, B, C and bilobalide (Huang et al. 2014; Tang et al. 2014). The changed PK of diabetes model may come from the different intestinal flora under pathological status (Ma, Li, et al. 2019). Compared with normal rats, gastric ulcer rats reduced the speed and quantity in absorption of costunolide and dehydrocostus lactone (Dong et al. 2018). Yet it is different from bilobalide, the rat gut microbiota is ineffective to both (Cui 2010).
Structure–activity relationship of a peptide permeation enhancer
Published in Tissue Barriers, 2023
L-R5 is more successful in increasing the permeability of FD-4 compared to the PEs bilobalide and latrunculin A (Figure 2A). The mechanisms of action of these two molecules are similar, as they both influence the cytoskeleton of the cell. By interacting with the adenosine A1 receptor, bilobalide causes contraction of the actin filament, which transiently opens intercellular junctions.41 Latrunculin A enters the cell and disrupts the cytoskeletal filaments, distorting the cell and allowing larger molecules to pass through cellular junctions.42 L-R5 has been designed to inhibit the activity of PKC ζ in phosphorylating TJs proteins. Opening of TJs may be also due to influence of L-R5 cytoskeleton, as the enzyme was shown to be involved in cytoskeletal organization.31,45 The opening induced by L-R5 appears to lead to a higher permeability with a faster onset, however, it should be noted that the applied concentrations of the other two molecules necessary to open TJs are much lower. An equivalent concentration of the peptide may give the same or even better results. The problem is that since latrunculin A is derived from a sponge toxin,46 an increase in concentration may lead to safety issues. By contrast, bilobalide showed no cytotoxicity at a concentration of 625 µM and may be more effective at higher concentrations if no increase in toxicity is observed.41 The fast increase in the first 15 minutes of each condition may be due to a hormetic effect,47 even if this difference is not significant. More specifically, the modification of the ambient environment will inevitably force the cell to adapt. A greater disruption of the cell membrane by FAs is also a potential reason for this increase, which would lead to a short increase in paracellular permeability. Another explanation of this short greater permeation enhancement the formation of micelles between FD-4 and FAs.