Abstract

Ilex paraguariensis A. St. Hil. (Aquifoliaceae), popularly known as “yerba mate,” has great economic and social significance for the population of Southern Latin America. This study was conducted (1) to investigate the phytochemical composition of four different standardized extracts, (2) to investigate its free radical scavenging properties, and (3) to investigate the anti-inflammatory action of I. paraguariensis and its major chemical markers. The chemical profile was achieved by Folin-Ciocalteu, by LC/DAD, and by LC/MS assays, while the antioxidant and anti-inflammatory properties were investigated, respectively, by DPPH assay and by inhibition of nitric oxide (Griess reaction) and TNF-α (ELISA). Our results demonstrated that the IA (aqueous infusion extract) showed higher amounts of total phenolic contents (266.62 ± 10.85 mg CAE·g−1 DE), the highest amounts of all six chemical markers (theobromine, 5-O-caffeoylquinic acid, 4-O-caffeoylquinic acid, 3-O-caffeoylquinic acid, caffeine, and rutin), and stronger antioxidant activity (EC50 = 54.4 ± 5.14 μg · mL−1). The IA extract also showed the lowest inhibition of NOx secretion (50.10 ± 8.97%) as well as inhibition of TNF-α (83.33 ± 4.01%). Regarding the chemical markers, all compounds showed strong inhibition of NOx secretion, especially theobromine, which was 200x more potent than dexamethasone. Furthermore, TNF-α secretion was also significantly decreased by THEO at 0.033 μM (22.15 ± 6.49%), NCA at 1.97 μM (27.46 ± 3.98%), CCA at 0.35 μM (39.76 ± 5.73%), CGA at 0.56 μM (23.58 ± 5.79%), CAF at 0.52 μM (26.45 ± 5.34%), and RUT at 0.16 μM (40.18 ± 3.70%). Our results suggest that I. paraguariensis and its major chemical markers have strong free radical scavenging properties as well as showed important anti-inflammatory activity and that these compounds in a plant extract may work based on several different mechanisms synergistically, resulting in moderating the immune system.

Highlights

  • Inflammation usually occurs as a protective event to rid the organism of harmful stimuli

  • In order to evaluate the importance of each compound on anti-inflammatory profile of the in the aqueous extract (IA) extract, we evaluated the effect of these compounds on the nitric oxide (NOx) levels at the concentration present in the original extract (IA extract at 3 μg·mL-1)

  • The analysis showed that all extracts have similar Total Phenolic Content (TPC), except for TES extract, which showed lower TPC (p < 0:05) than all the other preparations

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Summary

Introduction

Inflammation usually occurs as a protective event to rid the organism of harmful stimuli. Inflammation may happen in response to processes such as tissue injury, cell death, cancer, ischemia, and degeneration, leading to the activation of intracellular pathways and triggering the kinase cascades and nuclear transcription factors, such as MAPKs and NFκB [1, 2]. The development of anti-inflammatory drugs has improved the treatment of several diseases, other inflammatory pathologies such as asthma, atherosclerosis, and sepsis have not shown adequate response to current. Free radicals are related to diseases associated with elevated inflammatory signaling. Atherosclerosis, diabetes, and Alzheimer’s are related with an altered redox balance. The investigation of new anti-inflammatory and free radical scavenging agents remains relevant [5, 6]

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