Atividade antioxidante do extrato de lúpulo e afinidade de seus alfa ácidos ao receptor GABAA: implicações no tratamento da epilepsia

Abstract

Epilepsy is an extremely common neurological condition, affecting approximately 50 million people worldwide. It is characterized by recurrent episodes of epileptic seizures and is responsible for significant morbidity and mortality. The treatment of epilepsy mainly involves the use of antiepileptic drugs, which can help control epileptic seizures and improve the quality of life of those suffering from the condition. However, a significant proportion of this population is refractory to existing treatments, making it important to carry out studies to identify new drugs with antiepileptic action that are safe and effective. In this sense, hops, a plant from the Cannabacea family, known for its use in brewing beer, is also used as a herbal medicine to treat anxiety and sleep disorders. In addition, pre-clinical trials have already demonstrated the effects of hops on other pathological conditions affecting the central nervous system, such as Alzheimer's and depression. Therefore, the objectives of this work were to obtain an extract of hops, characterize the alpha-acid fraction of the extract using the Nuclear Magnetic Resonance technique, evaluate its antioxidant activities in vitro, the content of total phenolic compounds and their binding affinity with the GABAA receptor. Initially, the hop extract was prepared using the solvent hexane, which was analyzed using Nuclear Magnetic Resonance equipment. It was possible to identify three alpha acids in the extract, humulone, cohumulone and adhumulone. The extract showed significant antioxidant activity in the DPPH, ABTS+ radical cation capture, phosphomolybdenum and reducing power methods, as well as a high content of total phenolic compounds. In the in silico analysis, using the molecular docking tool, it was possible to observe the link between the alpha acids identified in the extract and the GABAA receptor. It is noteworthy that humulone had the best docking score among the alpha acids evaluated. We conclude that the hop extract developed in this study stands out for its significant antioxidant activity and high concentration of alpha acids. In addition, our results predict that alpha acids bind to the GABAA receptor, which suggests that hops have great potential for use in the treatment of epilepsy.