Clarified Açaí (Euterpe oleracea) Juice as an Anticonvulsant Agent: In Vitro Mechanistic Study of GABAergic Targets.

Gabriela P F Arrifano,Mathieu P Lichtenstein,Maria Elena Crespo-López,Hervé Rogez,Marcelo Farina,Cristina Suñol,José Carlos Tavares Carvalho,José Rogério Souza-Monteiro

doi:10.1155/2018/2678089

Abstract

Seizures affect about 50 million people around the world. Approximately 30% of seizures are refractory to the current pharmacological arsenal, so, the pursuit of new therapeutic alternatives is essential. Clarified Euterpe oleracea (EO) juice showed anticonvulsant properties similar to diazepam in an in vivo model with pentylenetetrazol, a GABAA receptor blocker. This study investigated the effects of EO on the main GABAergic targets for anticonvulsant drugs, analyzing the effect on the GABA receptor's benzodiazepine and picrotoxinin binding sites and the GABA uptake. Primary cultures of cortical neurons and astrocytes were treated with EO (0–25%) for up to 90 min. [3H]Flunitrazepam and [3H]TBOB binding, [3H]GABA uptake, cell viability, and morphology were assayed. Nonlethal concentrations of EO increased agonist binding and decreased antagonist binding in cortical neurons. Low concentrations significantly inhibited GABA uptake, especially in astrocytes, suggesting an accumulation of endogenous GABA in the synaptic cleft. The results demonstrate, for the first time, that EO can improve GABAergic neurotransmission via interactions with GABAA receptor and modulation of GABA uptake. Understanding these molecular mechanisms will help in the treatment of seizures and epilepsy, especially in developing countries where geographic isolation and low purchasing power are the main barriers to access to adequate treatment.

Highlights

Seizures are deleterious consequences of serious insults to the brain and primary manifestations in epilepsy, affecting more than 50 million people worldwide [1]
Treatment with Euterpe oleracea (EO) significantly decreased [3H]TBOB binding of the GABAA receptor in cortical neurons treated with ≥25% EO (Figure 1)
Figure 1: [3H]TBOB binding in cultures of cortical neurons treated with clarified Euterpe oleracea (EO) juice

Summary

Introduction

Seizures are deleterious consequences of serious insults to the brain (e.g., trauma and stroke) and primary manifestations in epilepsy, affecting more than 50 million people worldwide [1]. 80% of all epileptic patients live in low-income or developing countries, and approximately 75% of these patients do not get adequate treatment [1]. Açaí is the fruit of a common palm found in the eastern Amazonian floodplains, and its juice is highly consumed in Oxidative Medicine and Cellular Longevity northern Brazil (up to 1 l/day per person) [3]. It is available at the international market as a growing economic value (e.g., in 2011, açaí generated an estimated monetary movement of US$ 700,000 in Brazil) [4]

Methods

Results

Conclusion