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 |
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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. |
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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. 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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.</description><subject>Acetic acid</subject><subject>Acids</subject><subject>Analgesics - pharmacology</subject><subject>Analgesics - therapeutic use</subject><subject>Animals</subject><subject>antinociceptive activity</subject><subject>Blood-brain barrier</subject><subject>Caffeic acid</subject><subject>Cannabinoid CB1 receptors</subject><subject>cannabinoid receptor 1 (CB1)</subject><subject>Cannabinoids - pharmacology</subject><subject>Cannabinoids - therapeutic use</subject><subject>Computational neuroscience</subject><subject>Ethanol</subject><subject>Exploratory behavior</subject><subject>Gallic acid</subject><subject>High-performance liquid chromatography</subject><subject>Hypnotics and Sedatives - pharmacology</subject><subject>Hypnotics and Sedatives - therapeutic use</subject><subject>Kaempferol</subject><subject>Liquid chromatography</subject><subject>Locomotor activity</subject><subject>Male</subject><subject>Mice</subject><subject>molecular docking</subject><subject>Pain</subject><subject>Pain perception</subject><subject>Phenols</subject><subject>Phenols - pharmacology</subject><subject>Phenols - therapeutic use</subject><subject>Plant Extracts - chemistry</subject><subject>Quercetin</subject><subject>Receptors</subject><subject>Sleep</subject><subject>Vanillic acid</subject><subject>Vernonia</subject><subject>Vernonia - chemistry</subject><subject>Vernonia patula</subject><issn>0951-418X</issn><issn>1099-1573</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><sourceid>24P</sourceid><sourceid>WIN</sourceid><sourceid>EIF</sourceid><recordid>eNp10V1rFDEUBuAgFrtWwV8gAW-8mTYfM8nkshS_oGCRKt4NmeSETZlNxiRj2d_hHzazWxWEXh0CD29O8iL0ipJzSgi7mEs6F70UT9CGEqUa2kn-FG2I6mjT0v77KXqe8x0hRDHSPkOnnFPWUtFu0K_LUHyIxhuYi_8JWAeLM1h9PJg6fNnj6PA3SCEGr_GsyzLpA5wTWG8O1IcCafUx5JX7kvG8hRAnb7CJuzkuwWZ878sWly1go0PQY73aW1z2M2CKE6xLxPQCnTg9ZXj5MM_Q1_fvbq8-NtefP3y6urxuDO-5aEaleqpAEe6Yk9LWN0nSy55xJp1go6SWgRKuU6R11EigvRsZCBid0NZSfobeHnPnFH8skMuw89nANOkAcckDaztRf09xUemb_-hdXFKo21WlWCeEouJfoEkx5wRumJPf6bQfKBnWooZa1LAWVenrh8Bl3IH9C_80U0FzBPd-gv2jQcPN7ZdD4G_pCJ8U</recordid><startdate>202102</startdate><enddate>202102</enddate><creator>Siraj, Md Afjalus</creator><creator>Howlader, Md Sariful Islam</creator><creator>Rahaman, Md Sohanur</creator><creator>Shilpi, Jamil A.</creator><creator>Seidel, Veronique</creator><general>John Wiley & Sons, Ltd</general><general>Wiley Subscription Services, Inc</general><scope>24P</scope><scope>WIN</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7TM</scope><scope>8FD</scope><scope>FR3</scope><scope>K9.</scope><scope>P64</scope><scope>RC3</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0003-3880-5261</orcidid><orcidid>https://orcid.org/0000-0001-8159-1698</orcidid></search><sort><creationdate>202102</creationdate><title>Antinociceptive and sedative activity of Vernonia patula and predictive interactions of its phenolic compounds with the cannabinoid type 1 receptor</title><author>Siraj, Md Afjalus ; 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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.</abstract><cop>Chichester, UK</cop><pub>John Wiley & Sons, Ltd</pub><pmid>33124164</pmid><doi>10.1002/ptr.6876</doi><tpages>11</tpages><orcidid>https://orcid.org/0000-0003-3880-5261</orcidid><orcidid>https://orcid.org/0000-0001-8159-1698</orcidid><oa>free_for_read</oa></addata></record> |
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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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