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一种富含厚朴酚的厚朴树皮提取物具有类似抗焦虑的活性,并通过调节CB1受体发挥神经保护作用。

A honokiol-enriched Magnolia officinalis Rehder & E.H. Wilson. bark extract possesses anxiolytic-like activity with neuroprotective effect through the modulation of CB1 receptor.

作者信息

Borgonetti Vittoria, Governa Paolo, Manetti Fabrizio, Miraldi Elisabetta, Biagi Marco, Galeotti Nicoletta

机构信息

Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Section of Pharmacology, University of Florence, Florence, Italy.

Department of Biotechnology, Chemistry and Pharmacy - Department of Excellence 2018-2022, University of Siena Siena, Italy.

出版信息

J Pharm Pharmacol. 2021 Aug 12;73(9):1161-1168. doi: 10.1093/jpp/rgab067.

Abstract

OBJECTIVES

The exposure of neurons to an excessive excitatory stimulation induces the alteration of the normal neuronal function. Mood disorders are among the first signs of alterations in the central nervous system function. Magnolia officinalis bark extract has been extensively used in the traditional medicine systems of several countries, showing several pharmacological activities. Honokiol, the main constituent of M. officinalis, is a GABA modulator and a CB1 agonist, which is deeply investigated for its role in modulating mood disorders.

METHODS

Thus, we evaluated the possible neuroprotective effect of a standardized M. officinalis bark extract (MOE), enriched in honokiol, and its effect on animal mood behavioural tests and in an in vitro model of excitotoxicity.

KEY FINDINGS

MOE showed neuroprotective effect using SH-SY5Y cells, by normalizing brain-derived neurotrophic factor release. Then, we tested the effect of MOE in different behavioural tests evaluating anxiety and depression and we observed a selective anxiolytic-like effect. Finally, we confirmed the involvement of CB1 in the final effect of MOE by the co-administration of the CB1 antagonist, AM251.

CONCLUSION

These results suggest that MOE could be considered an effective and safe anxiolytic candidate with neuroprotective activity.

摘要

目的

神经元暴露于过度的兴奋性刺激会导致正常神经元功能的改变。情绪障碍是中枢神经系统功能改变的首批迹象之一。厚朴树皮提取物已在多个国家的传统医学体系中广泛使用,具有多种药理活性。厚朴酚是厚朴的主要成分,是一种γ-氨基丁酸(GABA)调节剂和大麻素1(CB1)受体激动剂,其在调节情绪障碍中的作用已得到深入研究。

方法

因此,我们评估了一种富含厚朴酚的标准化厚朴树皮提取物(MOE)可能的神经保护作用,及其对动物情绪行为测试和兴奋性毒性体外模型的影响。

主要发现

MOE通过使脑源性神经营养因子释放正常化,在SH-SY5Y细胞中显示出神经保护作用。然后,我们在评估焦虑和抑郁的不同行为测试中测试了MOE的作用,观察到了选择性抗焦虑样作用。最后,通过共同给予CB1拮抗剂AM251,我们证实了CB1参与了MOE的最终作用。

结论

这些结果表明,MOE可被认为是一种具有神经保护活性的有效且安全的抗焦虑候选物。

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