Antinociceptive and sedative activity of Vernonia patula and predictive interactions of its phenolic compounds with the cannabinoid type 1 receptor

When tested in the acetic acid‐induced writhing and formalin‐induced paw‐licking tests, the ethanol extract of Vernonia patula (VP) aerial parts showed significant antinociceptive activity. In neuropharmacological tests, it also significantly delayed the onset of sleep, increased the duration of sle...

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Veröffentlicht in:Phytotherapy research 2021-02, Vol.35 (2), p.1069-1079
Hauptverfasser: Siraj, Md Afjalus, Howlader, Md Sariful Islam, Rahaman, Md Sohanur, Shilpi, Jamil A., Seidel, Veronique
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container_issue 2
container_start_page 1069
container_title Phytotherapy research
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creator Siraj, Md Afjalus
Howlader, Md Sariful Islam
Rahaman, Md Sohanur
Shilpi, Jamil A.
Seidel, Veronique
description When tested in the acetic acid‐induced writhing and formalin‐induced paw‐licking tests, the ethanol extract of Vernonia patula (VP) aerial parts showed significant antinociceptive activity. In neuropharmacological tests, it also significantly delayed the onset of sleep, increased the duration of sleeping time, and significantly reduced the locomotor activity and exploratory behaviour of mice. Five phenolic compounds, namely gallic acid, vanillic acid, caffeic acid, quercetin and kaempferol, were detected in VP following HPLC‐DAD analysis. The presence of these phenolic compounds in VP provides some support for the observed antinociceptive and sedative effects. A computational study was performed to predict the binding affinity of gallic acid, vanillic acid, caffeic acid, quercetin and kaempferol towards the cannabinoid type 1 (CB1) receptor. Caffeic and vanillic acid showed the highest probable ligand efficiency indices towards the CB1 target. Vanillic acid displayed the best blood–brain barrier penetration prediction score. These findings provide some evidence for the traditional use of VP to treat pain.
doi_str_mv 10.1002/ptr.6876
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subjects Acetic acid
Acids
Analgesics - pharmacology
Analgesics - therapeutic use
Animals
antinociceptive activity
Blood-brain barrier
Caffeic acid
Cannabinoid CB1 receptors
cannabinoid receptor 1 (CB1)
Cannabinoids - pharmacology
Cannabinoids - therapeutic use
Computational neuroscience
Ethanol
Exploratory behavior
Gallic acid
High-performance liquid chromatography
Hypnotics and Sedatives - pharmacology
Hypnotics and Sedatives - therapeutic use
Kaempferol
Liquid chromatography
Locomotor activity
Male
Mice
molecular docking
Pain
Pain perception
Phenols
Phenols - pharmacology
Phenols - therapeutic use
Plant Extracts - chemistry
Quercetin
Receptors
Sleep
Vanillic acid
Vernonia
Vernonia - chemistry
Vernonia patula
title Antinociceptive and sedative activity of Vernonia patula and predictive interactions of its phenolic compounds with the cannabinoid type 1 receptor
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