Abstract

The commencement of the presented project was by screening of natural compounds extracted from neuroactive endogenous medicinal plants. Explicitly, ferutinin (Ferula hermonis L.), thymoquinone (Nigella sativa L.), eugenol (Syzygium aromaticum L.) and 6-gingerol (Zingiber officinale L.) were tested for their protective effect against neurodegeneration utilizing Glycine receptors (GlyRs) in vivo model. None of these compounds were reported before to modulate the in vivo GlyRs. GlyRs are inhibitory key mediators of synaptic signaling in spinal cord, brain stem, and higher central nervous system regions. Neurodegeneration may cause alteration of the GlyRs causing strychnine-like convulsions and stiffness. Modulation of GlyRs in vivo was studied in a mouse model of strychnine toxicity. Ferutinin revealed to be potent modulators to GlyR; with potential anticonvulsant properties in low doses. Thymoquinone, eugenol and 6-gingerol when given together with strychnine, in low concentrations reduce strychnine toxicity by reversing strychnine toxicity in mice. It could be concluded that all compounds under investigation could be used as sedatives in low doses. In order to fight against neurodegenerative diseases is to improve body antioxidant, the compounds under investigation provided to be good sources for antioxidant potential. In brief, ferutinin, thymoquinone, eugenol and 6-gingerol suggested being novel GlyR modulators, good phytochemicals, pharmacological tool and a dose sensitive drug to treat stiffness, convulsions and prophylactic agents to guard against neurodegenerative disorders.

Highlights

  • The use of endogenous natural products with therapeutic properties is as ancient as human civilization and, for a long time, plant products were the main sources of drugs [1]

  • In an attempt to find potential neuroprotective agents from plants against neurodegeneration, we examined whether a number of natural products of endogenous herbal medicines may exhibit protective efficacy on the in vivo Glycine receptors (GlyRs)

  • The protective effects of these compounds against neurodegeneration were mainly investigated in this study using in vivo behavioral studies on mice and radical scavenging activity on DPPH

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Summary

Introduction

The use of endogenous natural products with therapeutic properties is as ancient as human civilization and, for a long time, plant products were the main sources of drugs [1]. In an attempt to find potential neuroprotective agents from plants against neurodegeneration, we examined whether a number of natural products of endogenous herbal medicines may exhibit protective efficacy on the in vivo GlyRs. The selection of the natural compounds under investigation was based on screening of many neuroactive compounds, utilizing preliminary electrophysiological studies using patch-clamp. The choice of quinone and phenolic compounds under investigation was based on their preliminary modulatory effects in the in vitro homomeric α1 GlyR transfected on HEK 293 cells. There is increasing evidence for many potential benefits through quinone and phenolic compounds mediated regulation of cellular processes such as inflammation and neuroactivity [2]. Inductive or signaling properties of quinones and phenolics may occur at concentrations much lower than required for effective radical scavenging [2]. Quinones and phenolics demonstrate numerous biological and pharmacological effects, including antiinflammatory, and anticarcinogenic [3,4,5]

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