Benzodiazepine agonist-type activity of raubasine, a rauwolfia serpentina alkaloid

Charvéron, M.; Assié, Marie Bernadette; Stenger, A.; Briley, Mike

doi:10.1016/0014-2999(84)90718-0

Cited by 14 publications

(6 citation statements)

References 17 publications

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“…Apart from diterpenoid Aconitum alkaloids, there are many other kinds of alkaloids that have been reported with antiepileptic or anticonvulsant activities, including isoquinoline alkaloids such as berberine, montanine, and tetrahydropalmatine; indole alkaloids such as ibogaine, piperidine alkaloids such as piperine, amide alkaloids such as piplartine, tetracyclic oxindole alkaloids such as rhynchophylline and isorhynchophylline, aporphine alkaloids such as nantenine, erythrine byproducts such as erysothrine, (+)‐erythravine and (+)‐11‐α‐hydroxy‐erythravine, as well as raubasine . Anticonvulsant activities of the above‐mentioned alkaloids have been investigated in one or more of the models including pentylenetetrazole (PTZ), maximal electroshock (MES), kainic acid (KA), and bicuculline, pilocarpine, or N ‐methyl‐ d ‐aspartate (NMDA)–induced convulsions.…”

Section: Medicinal Compounds With Antiepileptic/anticonvulsant Activimentioning

confidence: 99%

“…Piperine, which significantly increased latencies to first convulsion and to death, as well as percentage of survival in pilocarpine‐induced convulsive mice, showed effects on inhibitory amino acids and on the GABAergic system . Raubasine attenuated PTZ‐ and bicuculline‐induced convulsions in mice; this may well be due to its benzodiazepine agonist–type activity . Furthermore, anticonvulsant activity of ibogaine has been studied both in vitro through voltage clamp recording, and in vivo using MES‐ and NMDA‐induced models.…”

Section: Medicinal Compounds With Antiepileptic/anticonvulsant Activimentioning

confidence: 99%

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Medicinal compounds with antiepileptic/anticonvulsant activities

et al. 2013

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SUMMARYObjective: Epilepsy is a serious neural disease that affects around 50 million people all over the world. Although for the majority patients with epilepsy, seizures are well controlled by currently available antiepileptic drugs (AEDs), there are still >30% of patients suffered from medically refractory epilepsy and approximately 30-40% of all epileptic patients affected by numerous side effects and seizure resistance to the current AEDs. Therefore, many researchers try to develop novel approaches to treat epilepsy, for example, to discover new antiepileptic constituents from herbal medicines. Although there are already several reviews on phytotherapy in epilepsy, most of them placed emphasis on the plant crude extracts or their isolated fractions, not pure active compounds derived from herbal medicines. This article aims to review components in herbal medicines that have shown antiepileptic or anticonvulsant properties. Methods: We searched online databases and identified articles using the preset searching syntax and inclusion criteria. The active medicinal compounds that have shown anticonvulsant or antiepileptic activity were included and classified according to structural types. Results: We have reviewed herein the active constituents including alkaloids, flavonoids, terpenoids, saponins, and coumarins. The screening models, the seizures-inducing factors and response, the effective dose, the potential mechanisms, as well as the structure-activity relationships in some of these active components have also been discussed. Significance: The in vitro and in vivo experimental data reviewed in this paper would supply the basic science evidence for research and development of novel AEDs from medicinal plants.

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Section: Medicinal Compounds With Antiepileptic/anticonvulsant Activimentioning

confidence: 99%

Section: Medicinal Compounds With Antiepileptic/anticonvulsant Activimentioning

confidence: 99%

Medicinal compounds with antiepileptic/anticonvulsant activities

et al. 2013

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“…Both of these compounds have shown anticonvulsant activity through neurotransmitter modulation [ 30 , 31 ]. Another compound, the Raubasine reduced bicuculline as well as PTZ induced convulsions into the mice; it might be due to its interacting activity with benzodiazepine [ 32 ]. Safranal is another monoterpene aldehyde of Crocus sativus L; it also showed inhibitory effect toward the PTZ induced convulsions in mice through an interaction with GABAA benzodiazepine receptor complex [ 33 , 34 ].…”

Section: Discussionmentioning

confidence: 99%

In silico inhibition of GABARAP activity using antiepileptic medicinal derived compounds

et al. 2015

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Epilepsy is a neurological disorder affecting more than 50 million people worldwide. It can be controlled by antiepileptic drugs (AEDs) but more than 30% patients are still resistant to AEDs. To overcome this problem, researchers are trying to develop novel approaches to treat epilepsy including the use of herbal medicines. The γ-amino butyric acid type-A receptor associated protein (GABARAP) is ubiquitin-like modifier implicated in the intracellular trafficking of GABAAR. An in silico mutation was created at 116 amino acid position G116A, and an in silico study was carried out to identify the potential binding inhibitors (with antiepileptic properties) against the active sites of GABARAP. Five different plant derived compounds namely (a) Aconitine (b) Berberine (c) Montanine (d) Raubasine (e) Safranal were selected, and their quantitative structure-activity relationships (QSAR) have been conducted to search the inhibitory activity of the selected compounds. The results have shown maximum number of hydrogen bond (H-bond) interactions of Raubasine with highest interaction energy among all of the five compounds. So, Raubasine could be the best fit ligand of GABARAP but in vitro, and in vivo studies are necessary for further confirmation.

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“…Another component of Rauvolfia, raubasine, is a benzodiazepine receptor agonist. 19 Due to these actions, Rauvolfia is a valuable therapeutic tool in treating individuals with stress and anxiety disorders.…”

Section: Rauvolfia Serpentina and Rauvolfia Vomitoriamentioning

confidence: 99%

The Calming Actions of Anemone Pulsatilla, Nepeta, and Rauvolfia

Stansbury¹,

Saunders²,

Winston³

2013

j restorat med

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Pulsatilla, Nepeta, and Rauvolfia are important therapeutic agents with nervecalming effects. Although not as strong as anxiolytic drugs, these herbal remedies are gentle and safe treatments for anxiety and insomnia. They can improve sleep, reduce mood swings and irritability, and moderate the stress-induced 'fight-or-flight' state. Theoretical concerns regarding adverse combination with alcohol or other psychoactive drugs have not been confirmed by clinical or scientific studies. The onset of depression must be monitored carefully when prescribing Rauvolfia to predisposed patients; however, this side effect does not appear to occur as commonly or severely as previously cited in the literature.

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Benzodiazepine agonist-type activity of raubasine, a rauwolfia serpentina alkaloid

Cited by 14 publications

References 17 publications

Medicinal compounds with antiepileptic/anticonvulsant activities

Medicinal compounds with antiepileptic/anticonvulsant activities

In silico inhibition of GABARAP activity using antiepileptic medicinal derived compounds

The Calming Actions of Anemone Pulsatilla, Nepeta, and Rauvolfia

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