Abstract

Aspidosperma pyrifolium is used in traditional medicine to treat inflammatory disorders. The aim of the study was to perform phytochemical characterization and evaluate the anti-inflammatory, anti-nociceptive and acute toxicity effects of the total alkaloid fraction (TAF-Ap) from stem barks. Two monoterpenic indole alkaloids were isolated by high performance liquid chromatography coupled with mass spectrometry (HPLC-MS) and the structural elucidation was performed using 1D and 2D NMR analysis. As for toxicity, no animals died at 50 mg kg−1 and this concentration presented mild sedation and forced breathing within the first 24 h. The lethal dose capable of killing 50% of the animals (LD50) was estimated to be 160 mg kg−1. In the pharmacological tests, the models used were 1% carrageenan-induced paw edema and peritonitis, 1% formalin-induced nociception and 1% acetic acid-induced abdominal writhing in Swiss mice. The study made it possible to isolate 15-methoxyaspidospermine and 15-methoxypyrifolidine, corroborating the results of pharmacological assays, which showed anti-inflammatory and analgesic potential, especially at 30 mg kg−1 (p < 0.001). Thus, the species was shown to be a promising source of active substances, with special attention paid to its toxicological potential.

Highlights

  • Inflammation is an immune defense mechanism that the body uses to fight bacteria, viruses and other pathogens [1,2]

  • The results presented suggest that TAF‐Ap exerts a central and peripheral effect against pain and inflammation, which corroborates data from another study [6], in which the 100 mg kg−1 dose of the aqueous extract of the seeds from A. pyrifolium showed a decrease in late phase licking time similar to that

  • Two monoterpenic indole alkaloids were isolated from the total alkaloid fraction

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Summary

Introduction

Inflammation is an immune defense mechanism that the body uses to fight bacteria, viruses and other pathogens [1,2]. In these processes, a variety of chemical mediators are released from damaged tissue, including excitatory amino acids, hydrogen ions, peptides, lipids, and cytokines, all of which underlie inflammation and pain [3]. Non-steroidal anti-inflammatory drugs, such as aspirin, as well as steroidal antiinflammatory drugs, such as dexamethasone, have been widely used to fight inflammation, but there is clinical evidence that these drugs are capable of causing adverse effects, including gastrointestinal disorders. Its wood is used in the manufacture of furniture, due to its excellent quality [5,6,7]; in traditional medicine, the extract of its leaves and bark is used for its anti-inflammatory and analgesic properties [7,8,9]

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