Neuroprotective effects and improvement of learning and memory elicited by erythravine and 11α-hydroxy-erythravine against the pilocarpine model of epilepsy

Gelfuso, Erica Aparecida; Reis, Suelen L; Pereira, Ana Maria Soares; Aguiar, Daiane Santos Rosa; Beleboni, Renê Oliveira

doi:10.1016/j.lfs.2019.117072

Cited by 4 publications

(2 citation statements)

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“…[28] In addition many studies have investigated their role against different neurological disorders like anxiety, [29][30][31] epilepsy and convulsions [31][32][33] and Alzheimer's disease. [34][35][36] A drug that displays efficacy by inhibiting or stimulating a certain target, whether in laboratory or computational settings, does not necessarily guarantee its success in clinical trials. That's because for a drug to reach its biological target in the human body, specifically oral drug, it must passes through many obstacles and barriers that may affect its concentration at the target, starting with gastrointestinal (GI) absorption which control its access to bloodstream and liver metabolism which can completely change the structure of the drug rendering it ineffective before reaching its target, [37] also for drugs targeting CNS they must display sufficient permeability through blood brain barrier (BBB) and resistance to P-glycoprotein (P-gp) which is the main efflux transporter in BBB.…”

Section: Introductionmentioning

confidence: 99%

Insights into the Role of Erythrina corallodendron L. in Alzheimer's Disease: in Vitro and in Silico Approach

Salem

Mostafa

Al‐Sayed

et al. 2023

Chemistry & Biodiversity

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Alzheimer's disease (AD) is a major health problem. Cholinergic transmission is greatly affected in AD. Phytochemical investigation of the alkaloid rich fraction (AF) of Erythrina corallodendron L leaves resulted in isolation of five known alkaloids: erysodine, erythrinine, 8-oxoerythrinine, erysovine N-oxide and erythrinine N-oxide. In this study, eysovine N-oxide was reported for the second time in nature. AF was assayed for cholinesterase inhibition at the concentration of 100 μg mL À 1 . AF showed a higher percent inhibition for butyrylcholinesterase enzyme (BuChE) (83.28 %) compared to acetylcholinesterase enzyme (AChE) (64.64 %). The isolated alkaloids were also assayed for their anti-BuChE effect. In-silico docking study was done for the isolated compounds at the binding sites of AChE and BuChE to determine their binding pattern and interactions, also molecular dynamics were estimated for the compound displaying the best fit for AChE and BuChE. In addition, ADME parameters and toxicity were predicted for the isolated alkaloids compared to donepezil.

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Section: Introductionmentioning

confidence: 99%

Insights into the Role of Erythrina corallodendron L. in Alzheimer's Disease: in Vitro and in Silico Approach

Salem

Mostafa

Al‐Sayed

et al. 2023

Chemistry & Biodiversity

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“…Indeed, the plant flowerings reserve a huge collection of alkaloids with different chemical structures and pharmacological activities, attending as a natural library for a chemical diversity of compounds for which structure-activity relationship deserves strong pharmaceutical attention (Feitosa et al, 2012;Majinda, 2018). Previous studies have demonstrated that (+)-erythravine and (+)-11α-hydroxy-erythravine alkaloids are among those responsible for antiepileptic and anxiolytic properties exhibited by E. mulungu flowerings (Faggion et al, 2011;Flausino et al, 2007;Gelfuso et al, 2020;Santos Rosa et al, 2012). However, scarce information is presented about the mechanism of action of these alkaloids both at molecular and cellular levels (Flausino et al, 2007;Setti-Perdigão et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

New insights in the mode of action of (+)-erythravine and (+)-11α-hydroxy-erythravine alkaloids

Gelfuso

Reis

Aguiar

et al. 2020

European Journal of Pharmacology

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Erythrinian alkaloids ((+)-erythravine and (+)-11-α-hydroxy-erythravine) have been pointed as the main responsible agents for the anticonvulsant and anxiolytic properties of Erythrina mulungu Mart ex Benth. The present work provides a new set of information about the mode of action of these alkaloids by the use of a complementary approach of neurochemical and electrophysiological assays. We propose here that the antiepileptic and anxiolytic properties exhibited by both alkaloids appear not to be related to the inhibition of glutamate binding or GABA uptake, or even to the increase of glutamate uptake or GABA binding, as investiga ted here by the use of rat cortical synaptosomes. Similarly, and even in a high concentration, (+)erythravine and (+)-11-α-hydroxy-erythravine did not modulate the main sodium and potassium channel isoforms checked by the use of voltage-clamp studies on Xenopus laevis oocytes. However, unlike (+)-11-α-hydroxy-erythravine, which presented a little effect, it was possible to observe that the (+)-erythravine alkaloid produced a significant inhibitory modulation on α4β2, α4β4 and α7 isoforms of nicotinic acetylcholine receptors also checked by the use of voltage-clamp studies, which could explain at least partially its anxiolytic and anticonvuls a nt properties. Since (+)-11-α-hydroxy-erythravine and erythravine modulated nicotinic acetylcholine receptors to different extents, it is possible to reinforce that small differe nces between the chemical structure of these alkaloids can affect the selectivity and affinity of targetligand interactions, conferring distinct potency and/or pharmacological properties to them, as previously suggested by differential experimental comparison between different erythrinia n alkaloids.

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The protective effect of inhibiting mitochondrial fission on the juvenile rat brain following PTZ kindling through inhibiting the BCL2L13/LC3 mitophagy pathway

et al. 2022

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Neuroprotective effects and improvement of learning and memory elicited by erythravine and 11α-hydroxy-erythravine against the pilocarpine model of epilepsy

Cited by 4 publications

References 50 publications

Insights into the Role of Erythrina corallodendron L. in Alzheimer's Disease: in Vitro and in Silico Approach

Insights into the Role of Erythrina corallodendron L. in Alzheimer's Disease: in Vitro and in Silico Approach

New insights in the mode of action of (+)-erythravine and (+)-11α-hydroxy-erythravine alkaloids

The protective effect of inhibiting mitochondrial fission on the juvenile rat brain following PTZ kindling through inhibiting the BCL2L13/LC3 mitophagy pathway

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