Anticonvulsant effect of Rhynchophylline involved in the inhibition of persistent sodium current and NMDA receptor current in the pilocarpine rat model of temporal lobe epilepsy

Shao, Hui; Yang, Yang; Mi, Ze; Zhu, Guoqi; Qi, Aiping; Ji, Wei-gang; Zhu, Zhi-ru

doi:10.1016/j.neuroscience.2016.09.029

Cited by 32 publications

(28 citation statements)

References 58 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Alkaloids are defined by the presence of a heterocyclic nitrogen atom, and have been increasingly attracting pharmaceutical researchers to develop therapeutic agents as lead compounds [1][2][3]. Indole alkaloids are characterized by the presence of a structural moiety of indole, and have been extensively studied as they possess important biological properties such as antihypertension [4], antihistamine [5], anticonvulsant [6], anti-leishmanial [7], antidiabetic [8], anti-HIV-1, anti-inflammatory [9], anticancer [10], and antibacterial activities [11]. They are present in several plant families as secondary metabolites, including the Strychnaceae, Apocynaceae, Rutaceae, and Rubiaceae [10].…”

Section: Introductionmentioning

confidence: 99%

Novel Deep Eutectic Solvent Based on Levulinic Acid and 1,4-Butanediol as an Extraction Media for Bioactive Alkaloid Rutaecarpine

Sun

Liu

et al. 2019

Processes

View full text Add to dashboard Cite

Deep eutectic solvents (DESs) are increasingly receiving interest as a new type of green and sustainable alternative to hazardous organic solvents. In this work, a novel DES based on levulinic acid (La) and 1,4-butanediol (Buta) as an extraction media was developed for extracting the bioactive alkaloid rutaecarpine from the unripe fruits of Tetradium ruticarpum. 24 different DESs consisting of choline chloride, betaine, sugar alcohols, organic acids, amides, and sugars were prepared and tailored to test their extraction efficiency. After initial screening, a hydrophilic DES composed of La and Buta with 1:0.5 molar ratio containing 25% water was tailored for the highest extraction efficiency, followed by the optimizations of molar ratio and water content. The interaction between the molecules of La-Buta DES was investigated by nuclear magnetic resonance spectroscopy in order to confirm its deep eutectic supermolecular structure feature. The extraction conditions were optimized by single-factor experiments, including extraction temperature, extraction time, and solid-liquid ratio. The developed La-Buta DES extraction procedure was successfully applied for the analysis of rutaecarpine in Chinese patent medicines containing the unripe fruits of T. ruticarpum. The excellent property of La-Buta DES indicated its potential as a promising green solvent instead of conventional organic solvent for the extraction of rutaecarpine from the unripe fruits of T. ruticarpum, and that it can used as a sustainable and safe extraction media for other applications.

show abstract

Section: Introductionmentioning

confidence: 99%

Novel Deep Eutectic Solvent Based on Levulinic Acid and 1,4-Butanediol as an Extraction Media for Bioactive Alkaloid Rutaecarpine

Sun

Liu

et al. 2019

Processes

View full text Add to dashboard Cite

show abstract

“…The dried stem and hook of Uncaria rhynchophylla , named as Gou-teng or Cat’s Claw, have a variety of uses in traditional herbal medicine including the treating of convulsions, numbness and hypertension ( Zhou and Zhou, 2010 ; Ng et al, 2015 ; Shao et al, 2016 ), and in treating head ailments such as headache and dizziness. Meanwhile, Uncaria rhynchophylla is also commercially sold as a health food product.…”

Section: Introductionmentioning

confidence: 99%

Neuroprotection Against MPP+-Induced Cytotoxicity Through the Activation of PI3-K/Akt/GSK3β/MEF2D Signaling Pathway by Rhynchophylline, the Major Tetracyclic Oxindole Alkaloid Isolated From Uncaria rhynchophylla

Mak

Zuo

et al. 2018

Front. Pharmacol.

View full text Add to dashboard Cite

Rhynchophylline is a major tetracyclic oxindole alkaloid in Uncaria rhynchophylla, which has been extensively used as traditional herb medicine for the prevention of convulsions and hypertension. However, there is still little evidence about the neuroprotective effects of rhynchophylline for Parkinson’s disease (PD), a neurodegenerative condition currently without any effective cure. In this present study, the neuroprotective molecular mechanisms of rhynchophylline were investigated in a cellular model associated with PD. It is shown that rhynchophylline (10–50 μM) greatly prevented neurotoxicity caused by 1-methyl-4-phenylpyridinium ion (MPP+) in primary cerebellar granule neurons, as evidenced by the promotion of cell viability as well as the reversal of dysregulated protein expression of Bax/Bcl-2 ratio. Very encouragingly, we found that rhynchophylline markedly enhanced the activity of the transcription factor myocyte enhancer factor 2D (MEF2D) at both basal and pathological conditions using luciferase reporter gene assay, and reversed the inhibition of MEF2D caused by MPP+. Additionally, pharmacological inhibition of PI3-Kinase or short hairpin RNA-mediated gene down-regulation of MEF2D abrogated the protection provided by rhynchophylline. Furthermore, Western blot analysis revealed that rhynchophylline could potentiate PI3-K/Akt to attenuate GSK3β (the MEF2D inhibitor) in response to MPP+ insult. In conclusion, rhynchophylline inhibits MPP+-triggered neurotoxicity by stimulating MEF2D via activating PI3-K/Akt/GSK3β cascade. Rhynchophylline is served as a novel MEF2D enhancer and might be a potential candidate for further preclinical study in the prevention of PD.

show abstract

“…Positive results in either model suggest that the test compound, or its metabolite crossed the blood–brain barrier and exerted its effect in the central nervous system [ 1 ]. In this review, all experiments consisted initially of phenotypic screens in rodents using predominantly PTZ [ 6 , 13 , 18 , 19 , 21 , 22 , 24 , 25 , 27 , 28 ], MES [ 20 , 22 , 24 ] and pilocarpine [ 16 , 23 , 26 , 32 ] seizure models. A few researchers dared to test their extracts in more than one phenotypic screening models [ 13 , 20 , 22 , 24 ].…”

Section: Discussionmentioning

confidence: 99%

Recent Advances in Antiepileptic Herbal Medicine

Manchishi

2017

View full text Add to dashboard Cite

Background:Epilepsy is one of the most common neurological disorders worldwide, with about 80 percent of cases thought to be in developing nations where it is mostly linked to superstition. The limited supply, high cost as well as low efficacy and adverse side effects of antiepileptic drugs (AEDs) is a matter of major concern. Herbal medicine has always been traditionally part of treatment of epilepsy. Herbal medicines are generally well tolerated, with fewer side effects.Method:To highlight some herbal extracts that have been studied for their anticonvulsant activity in animal models, literature search from PubMed and Science Direct, was performed. The keywords for the search consisted of combinations of the following terms: Herbal antiepileptic and/or anticonvulsant, botanicals + epilepsy. Literature published in the last five years was considered.Results:Eighteen (18) anticonvulsant herbal agents are reported and discussed. Experiments mostly consisted of phenotypic screens in rodents, with little diversity in screening methods. In most experiments, the tested extracts prolonged the time to onset of seizures and decreased their duration. Most experimenters implicate potentiation of GABAergic activity as the mode of action of the extracts, even though some experimenters did not fully characterise the bioactive chemical composition of their extracts.Conclusion:Potential herbal remedies have shown positive results in animal models. It remains unclear how many make it into clinical trials and eventually making part of the AED list. More rigorous research, applying strict research methodology with uniform herbal combinations, as well as clinical studies are urgently needed.

show abstract

Anticonvulsant effect of Rhynchophylline involved in the inhibition of persistent sodium current and NMDA receptor current in the pilocarpine rat model of temporal lobe epilepsy

Cited by 32 publications

References 58 publications

Novel Deep Eutectic Solvent Based on Levulinic Acid and 1,4-Butanediol as an Extraction Media for Bioactive Alkaloid Rutaecarpine

Novel Deep Eutectic Solvent Based on Levulinic Acid and 1,4-Butanediol as an Extraction Media for Bioactive Alkaloid Rutaecarpine

Neuroprotection Against MPP+-Induced Cytotoxicity Through the Activation of PI3-K/Akt/GSK3β/MEF2D Signaling Pathway by Rhynchophylline, the Major Tetracyclic Oxindole Alkaloid Isolated From Uncaria rhynchophylla

Recent Advances in Antiepileptic Herbal Medicine

Contact Info

Product

Resources

About