Antiepileptic activity and potential mechanism of full-spectrum hemp extract

IF 6.3 3区 综合性期刊 Q1 Multidisciplinary Fundamental Research Pub Date : 2025-01-01 DOI:10.1016/j.fmre.2024.11.002
Zengliang Jin , Zhuo Huang
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Abstract

Epilepsy is the fourth most common neuropsychiatric disorder. Although the approval of Epidiolex has ignited hope for patients, there is still a large gap in the field of anti-seizure research. The effect and underlying mechanism of full-spectrum hemp extract (HE) remains unclear. Here this study investigated the anti-seizure effect of HE on seizure models. The results showed that HE significantly reduced seizure susceptibility and prolonged seizure latency with better pharmacokinetic performance compared to CBD. This article then further explored the anti-seizure active components and their possible mechanism in HE. The results indicated that cannabichromene (CBC) and cannabinol (CBN) were involved in the anti-seizure process, especially CBC showed a strong allosteric enhancement effects on CBD binding site of the GABAA receptor, which implied that the GABAA receptor seemed to be the primary anti-epileptic target of HE. This article not only presents the great potential of HE as a candidate for new anti-epileptic drugs with less psychoactive, but also provides a valuable contribution to subsequent mechanism research and drug development on epilepsy.Abstract: Epilepsy is the fourth most coneuropsychiatric disorder. Although the approval of Epidiolex has ignited hope for patients, there is still a large gap in the field of anti-seizure research. The effect and underlying mechanism of full-spectrum hemp extract remains unclear. Here this study investigated the anti-seizure effect of HE on seizure models. The results showed that HE significantly reduced seizure susceptibility and prolonged seizure latency with better pharmacokinetic performance compared to CBD. This article then further explored the anti-seizure active components and their possible mechanism in HE. The results indicated that cannabichromene and cannabinol were involved in the anti-seizure process, especially CBC showed a strong allosteric enhancement effects on CBD binding site of the GABAA receptor, which implied that the GABAA receptor seemed to be the primary anti-epileptic target of HE. This article not only presents the great potential of HE as a candidate for new anti-epileptic drugs with less psychoactive, but also provides a valuable contribution to subsequent mechanism research and drug development on epilepsy.
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全谱大麻提取物的抗癫痫活性及其潜在机制
癫痫是第四大最常见的神经精神疾病。虽然Epidiolex的获批点燃了患者的希望,但在抗癫痫研究领域仍存在较大差距。全谱大麻提取物(HE)的作用和作用机制尚不清楚。本研究探讨HE对癫痫模型的抗癫痫作用。结果表明,与CBD相比,HE显著降低了癫痫发作的易感性,延长了癫痫发作潜伏期,并具有更好的药代动力学性能。本文进一步探讨了HE抗癫痫活性成分及其可能的作用机制。结果表明,大麻红素(CBC)和大麻酚(CBN)参与了抗癫痫过程,特别是CBC对GABAA受体的CBD结合位点表现出较强的变构增强作用,暗示GABAA受体可能是HE抗癫痫的主要靶点。本文不仅展示了HE作为一种精神活性较低的新型抗癫痫药物的巨大潜力,而且为后续癫痫的机制研究和药物开发提供了宝贵的贡献。摘要:癫痫是第四大神经精神障碍。虽然Epidiolex的获批点燃了患者的希望,但在抗癫痫研究领域仍存在较大差距。全谱大麻提取物的作用和作用机制尚不清楚。本研究探讨HE对癫痫模型的抗癫痫作用。结果表明,与CBD相比,HE显著降低了癫痫发作的易感性,延长了癫痫发作潜伏期,并具有更好的药代动力学性能。本文进一步探讨了HE抗癫痫活性成分及其可能的作用机制。结果表明,大麻红素和大麻酚参与了抗癫痫过程,特别是CBC对GABAA受体的CBD结合位点表现出较强的变抗增强作用,提示GABAA受体可能是HE抗癫痫的主要靶点。本文不仅展示了HE作为一种精神活性较低的新型抗癫痫药物的巨大潜力,而且为后续癫痫的机制研究和药物开发提供了宝贵的贡献。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Fundamental Research
Fundamental Research Multidisciplinary-Multidisciplinary
CiteScore
4.00
自引率
1.60%
发文量
294
审稿时长
79 days
期刊介绍:
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