Abstract

BackgroundTieghemella heckelii stem bark is used in African traditional medicine to treat inflammatory pain conditions. However, these biological actions of the plant have not been proven. This study investigates the phytochemical composition and the mechanisms of analgesic and anti-inflammatory actions of the hydroethanolic stem bark extract of T. heckelii (THBE). Methods Phytochemical composition of THBE was investigated using qualitative and quantitative phytochemical analyses. Anti-inflammatory activity was evaluated using the carrageenan-induced paw oedema assay. Analgesic activity was evaluated using hot plate and acetic acid-induced writhing assays. Mechanism of analgesic action was determined using pharmacological antagonist such as naloxone, atropine, flumazenil, nifedipine, or ketamine. Test agents were administered orally as follows: Tween 80 (5%) (control), diclofenac sodium (DS) 10/tramadol 9 mg/kg (standard), or THBE 10, 100, and 450 mg/kg. Glutathione peroxidase (GPx), superoxide dismutase (SOD), and lipid peroxidation levels were also measured. Results THBE which contained 58.45% saponins, 229.04 ± 0.049 GAE mg/g phenolic compounds,and 0.482 ± 0.0028 QE mg/g flavonoids produced (p < 0.5) anti-inflammatory effect of 56.22% and analgesia of 330 ± 72% and 50.4% in the hot plate and writhing assays, respectively, at 10 mg/kg and inhibited oxidative stress by GPx and SOD elevation in rats during inflammation. Ketamine significantly blocked the analgesia of THBE, indicating NMDA receptor-dependent analgesic action. Whereas, naloxone, atropine, nifedipine, and flumazenil could not antagonize the analgesic action of THBE. Conclusion These results show that THBE produced potent anti-inflammatory effect via disruption of oxidative stress and also generated NMDA receptor-dependent analgesia.

Highlights

  • Pain is a protective mechanism which warns the body against possible or actual tissue damage when there is a noxious stimulus, physical injury, inflammatory state, or disease. e most prevalent cause for which people seek medical treatment is acute pain which manifests in various forms such as headache, gastrointestinal, musculoskeletal, or chest pains in addition to pain due to injuries, e.g., sprains, lacerations, and fractures [1, 2]

  • Yield and Nature of the Extract. e 70% hydroethanolic extract of the 200 g dried stem bark of T. heckelii produced 43.76 g of reddish brown hygroscopic solid which translated into a yield of 21.88% w/w

  • Toxicity or Safety of THBE Administration in Acute Conditions. e extract administered at 2500 mg/kg p.o. did not produce any observable sign of toxicity such as change in motor activity, eye color, salivation, lachrymation, coma, or eventual death within the 14 days observation period in female SDR rats

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Summary

Introduction

Pain is a protective mechanism which warns the body against possible or actual tissue damage when there is a noxious stimulus, physical injury, inflammatory state, or disease. e most prevalent cause for which people seek medical treatment is acute pain which manifests in various forms such as headache, gastrointestinal, musculoskeletal, or chest pains in addition to pain due to injuries, e.g., sprains, lacerations, and fractures [1, 2]. E young bud is employed against snake bites, and the stem bark is used to treat blennorrhoea and toothache [8] Few biological activities such as antibacterial, cytotoxicity, and anti-HIV inhibitory effects of the plant have been reported [9, 10]. Is study, sought to investigate the mechanism of analgesic and anti-inflammatory actions of the standardized hydroethanolic stem bark extract of T. heckelii. Tieghemella heckelii stem bark is used in African traditional medicine to treat inflammatory pain conditions These biological actions of the plant have not been proven. Is study investigates the phytochemical composition and the mechanisms of analgesic and anti-inflammatory actions of the hydroethanolic stem bark extract of T. heckelii (THBE). Conclusion. ese results show that THBE produced potent anti-inflammatory effect via disruption of oxidative stress and generated NMDA receptor-dependent analgesia

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