The GABAergic System and Endocannabinoids in Epilepsy and Seizures: What Can We Expect from Plant Oils?

Oliveira, Fábio Rodrigues de; Silva, Nágila Monteiro da; Hamoy, Moisés; Crespo-López, María Elena; Ferreira, Irlon M.; Silva, Edilene O.; Macchi, Barbarella de Matos; Nascimento, José Luiz Martins do

doi:10.3390/molecules27113595

Cited by 4 publications

(2 citation statements)

References 115 publications

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“…This unprovoked seizure has affected approximately 65 million people globally [3] and 80 % of the cases in developing countries. Intracerebral hemorrhage, genetic and developmental abnormalities, brain injuries, stroke, drug abuse, infections, brain tumors, psychological and social morbidities are the main causes of epilepsy [4] . The onset of epilepsy occurs most frequently in elderly people and children.…”

Section: Introductionmentioning

confidence: 99%

“…Intracerebral hemorrhage, genetic and developmental abnormalities, brain injuries, stroke, drug abuse, infections, brain tumors, psychological and social morbidities are the main causes of epilepsy. [4] The onset of epilepsy occurs most frequently in elderly people and children. Anticonvulsants/ antiepileptics are a diverse class of therapeutic drugs that work through various mechanisms to reduce the frequency of epileptic seizures.…”

Section: Introductionmentioning

confidence: 99%

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Exploring the Novel Anticonvulsant Phytochemicals from Glycyrrhiza glabra: An In Silico Approach

Salaria,

NN,

2023

ChemistrySelect

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Computational methods like molecular docking, pharmacokinetic study, molecular dynamic (MD) simulation and Molecular Mechanics‐Poisson‐Boltzmann Surface Area (MM‐PBSA) were used to investigate the ability of Glycyrrhiza glabra phytoconstituents to modulate the activity of GABA‐A receptor. The docking studies suggested that both Kanzonol U and Glabrol, have shown superior binding abilities, as evident by their binding energies of −11.8 and −11.4 kcal/mol, respectively, as compared to diazepam (−10.0 kcal/mol), which is an allosteric modulator of GABA‐A. Only nine constituents were identified as the blood‐brain barrier permeants in the SwissADME investigation, with binding energy≤−10.0 kcal/mol. The docking results were further strengthened by MD simulation which showed that the Kanzonol U and Glabrol complex displayed good conformational stability with an average RMSD of 0.20 nm. Additionally, MM‐PBSA outcomes revealed that these phytochemicals as the most potent GABA‐A modulators. All these investigations suggest that the phytochemicals Kanzonol U and Glabrol may produce a promising antiepileptic effect.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Exploring the Novel Anticonvulsant Phytochemicals from Glycyrrhiza glabra: An In Silico Approach

Salaria,

NN,

2023

ChemistrySelect

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Virtual Screening-Based Drug Development for the Treatment of Nervous System Diseases

Zhao

et al. 2023

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The incidence rate of nervous system diseases is increasing in recent years. Nerve injury or neurodegenerative diseases usually cause neuronal loss and neuronal circuit damage, which seriously affect motor nerve and autonomic nervous function. Therefore, a safe and effective treatment is needed. As traditional drug research becomes slower and more expensive, it is vital to enlist the help of cutting-edge technology. Virtual screening (VS) is an attractive option for the identification and development of promising new compounds with high efficiency and low cost. With the assistance of computer-aided drug design (CADD), VS is becoming more and more popular in new drug development and research. In recent years, it has become a reality to transform non-neuronal cells into functional neurons through small molecular compounds, which provides a broader application prospect than transcription factor-mediated neuronal reprogramming. This review mainly summarizes related theory and technology of VS and the drug research and development using VS technology in nervous system diseases in recent years, and focuses more on the potential application of VS technology in neuronal reprogramming, thus facilitating new drug design for both prevention and treatment of nervous system diseases.

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Lippia origanoides essential oil possesses anticonvulsant effect in pentylenetetrazol-induced seizures in rats: a behavioral, electroencephalographic, and electromyographic study

Bastos de Araújo,

Gurgel do Amaral,

Maia da Fonseca

et al. 2023

Front. Pharmacol.

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Epilepsy is a neuronal disorder characterized by abnormal excitability of the brain, leading to seizures. Only around 66% of the epileptic patients respond adequately to treatment with existing conventional anticonvulsants, making it necessary to investigate new antiepileptic drugs. The growing research into natural products and their pharmacological properties has become increasingly promising, particularly in the study of essential oils, which are already widely used in popular culture for treating various diseases. The present study evaluated the anticonvulsant effects of Lippia origanoides essential oil (LOEO) (100 mg/kg i. p.) compared to diazepam (DZP) (5 mg/kg i. p.), and the combined administration of these two substances to control convulsions induced by pentylenetetrazol (PTZ) (60 mg/kg i. p.). This evaluation was carried out using 108 male Wistar rats, which were divided into two experiments. Experiment 1–Behavioral assessment: The animals were divided into 4 groups (n = 9): (I) saline solution + PTZ, (II) DZP + PTZ, (III) LOEO + PTZ, (IV) LOEO + DZP + PTZ. The convulsive behavior was induced 30 min after the administration of the tested anticonvulsant drugs, and the observation period lasted 30 min. Experiment 2- Electrocorticographic evaluation: The animals were divided into 8 groups (n = 9): (I) saline solution; (II) LOEO; (III) DZP; (IV) LOEO + DZP; (V) saline + PTZ, (VI) DZP + PTZ (VII) LOEO + PTZ, (VIII) LOEO + DZP + PTZ. PTZ was administered 30 min after LOEO and DZP treatments and electrocorticographic activity was assessed for 15 min. For the control groups, electromyographic recordings were performed in the 10th intercostal space to assess respiratory rate. The results demonstrated that Lippia origanoides essential oil increased the latency time for the appearance of isolated clonic seizures without loss of the postural reflex. The animals had a more intense decrease in respiratory rate when combined with LOEO + DZP. EEG recordings showed a reduction in firing amplitude in the LOEO-treated groups. The combining treatment with diazepam resulted in increased anticonvulsant effects. Therefore, treatment with Lippia origanoides essential oil was effective in controlling seizures, and its combination with diazepam may represent a future option for the treatment of difficult-to-control seizures.

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The GABAergic System and Endocannabinoids in Epilepsy and Seizures: What Can We Expect from Plant Oils?

Cited by 4 publications

References 115 publications

Exploring the Novel Anticonvulsant Phytochemicals from Glycyrrhiza glabra: An In Silico Approach

Exploring the Novel Anticonvulsant Phytochemicals from Glycyrrhiza glabra: An In Silico Approach

Virtual Screening-Based Drug Development for the Treatment of Nervous System Diseases

Lippia origanoides essential oil possesses anticonvulsant effect in pentylenetetrazol-induced seizures in rats: a behavioral, electroencephalographic, and electromyographic study

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