Antinociceptive activities of a novel diarylpentanoid analogue, 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol, and its possible mechanisms of action in mice

A novel synthetic compound from the 2-benzoyl-6-benzylidenecyclohexanone analogue, namely 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol (BBHC), showed pronounced nitric oxide inhibition in IFN-γ/LPS-induced RAW 264.7 cells. Based on this previous finding, our present study aimed to inves...

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Main Authors: Ong, Hui Ming, Ahmad Azmi, Ahmad Farhan, Sze, Wei Leong, Abas, Faridah, Perimal, Enoch Kumar, Omar Farouk, Ahmad Akira, Ahmad Israf, Daud, Sulaiman, Mohd Roslan
Format: Article
Published: Nature Research 2021
Online Access:http://psasir.upm.edu.my/id/eprint/95923/
https://www.nature.com/articles/s41598-021-02961-1
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spelling my.upm.eprints.959232023-03-22T03:07:03Z http://psasir.upm.edu.my/id/eprint/95923/ Antinociceptive activities of a novel diarylpentanoid analogue, 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol, and its possible mechanisms of action in mice Ong, Hui Ming Ahmad Azmi, Ahmad Farhan Sze, Wei Leong Abas, Faridah Perimal, Enoch Kumar Omar Farouk, Ahmad Akira Ahmad Israf, Daud Sulaiman, Mohd Roslan A novel synthetic compound from the 2-benzoyl-6-benzylidenecyclohexanone analogue, namely 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol (BBHC), showed pronounced nitric oxide inhibition in IFN-γ/LPS-induced RAW 264.7 cells. Based on this previous finding, our present study aimed to investigate the antinociceptive effects of BBHC via chemical and thermal stimuli in vivo. The investigation of the antinociceptive activity of BBHC (0.1, 0.3, 1.0 and 3.0 mg/kg, i.p.) was initiated with 3 preliminary screening tests, then BBHC was subjected to investigate its possible involvement with excitatory neurotransmitters and opioid receptors. The potential acute toxicity of BBHC administration was also studied. Administration of BBHC significantly inhibited acetic acid-induced abdominal constrictions, formalin-induced paw licking activity and developed notable increment in the latency time. BBHC’s ability to suppress capsaicin- and glutamate-induced paw licking activities, as well as to antagonise the effect of naloxone, had indicated the possible involvement of its antinociception with TRPV1, glutamate and opioid receptors, respectively. The antinociceptive activities of BBHC was not related to any sedative action and no evidence of acute toxic effect was detected. The present study showed that BBHC possessed significant peripheral and central antinociceptive activities via chemical- and thermal-induced nociceptive murine models without any locomotor alteration and acute toxicity. Nature Research 2021 Article PeerReviewed Ong, Hui Ming and Ahmad Azmi, Ahmad Farhan and Sze, Wei Leong and Abas, Faridah and Perimal, Enoch Kumar and Omar Farouk, Ahmad Akira and Ahmad Israf, Daud and Sulaiman, Mohd Roslan (2021) Antinociceptive activities of a novel diarylpentanoid analogue, 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol, and its possible mechanisms of action in mice. Scientific Reports, 11. art. no. 24121. pp. 1-10. ISSN 2045-2322 https://www.nature.com/articles/s41598-021-02961-1 10.1038/s41598-021-02961-1
institution Universiti Putra Malaysia
building UPM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Putra Malaysia
content_source UPM Institutional Repository
url_provider http://psasir.upm.edu.my/
description A novel synthetic compound from the 2-benzoyl-6-benzylidenecyclohexanone analogue, namely 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol (BBHC), showed pronounced nitric oxide inhibition in IFN-γ/LPS-induced RAW 264.7 cells. Based on this previous finding, our present study aimed to investigate the antinociceptive effects of BBHC via chemical and thermal stimuli in vivo. The investigation of the antinociceptive activity of BBHC (0.1, 0.3, 1.0 and 3.0 mg/kg, i.p.) was initiated with 3 preliminary screening tests, then BBHC was subjected to investigate its possible involvement with excitatory neurotransmitters and opioid receptors. The potential acute toxicity of BBHC administration was also studied. Administration of BBHC significantly inhibited acetic acid-induced abdominal constrictions, formalin-induced paw licking activity and developed notable increment in the latency time. BBHC’s ability to suppress capsaicin- and glutamate-induced paw licking activities, as well as to antagonise the effect of naloxone, had indicated the possible involvement of its antinociception with TRPV1, glutamate and opioid receptors, respectively. The antinociceptive activities of BBHC was not related to any sedative action and no evidence of acute toxic effect was detected. The present study showed that BBHC possessed significant peripheral and central antinociceptive activities via chemical- and thermal-induced nociceptive murine models without any locomotor alteration and acute toxicity.
format Article
author Ong, Hui Ming
Ahmad Azmi, Ahmad Farhan
Sze, Wei Leong
Abas, Faridah
Perimal, Enoch Kumar
Omar Farouk, Ahmad Akira
Ahmad Israf, Daud
Sulaiman, Mohd Roslan
spellingShingle Ong, Hui Ming
Ahmad Azmi, Ahmad Farhan
Sze, Wei Leong
Abas, Faridah
Perimal, Enoch Kumar
Omar Farouk, Ahmad Akira
Ahmad Israf, Daud
Sulaiman, Mohd Roslan
Antinociceptive activities of a novel diarylpentanoid analogue, 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol, and its possible mechanisms of action in mice
author_facet Ong, Hui Ming
Ahmad Azmi, Ahmad Farhan
Sze, Wei Leong
Abas, Faridah
Perimal, Enoch Kumar
Omar Farouk, Ahmad Akira
Ahmad Israf, Daud
Sulaiman, Mohd Roslan
author_sort Ong, Hui Ming
title Antinociceptive activities of a novel diarylpentanoid analogue, 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol, and its possible mechanisms of action in mice
title_short Antinociceptive activities of a novel diarylpentanoid analogue, 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol, and its possible mechanisms of action in mice
title_full Antinociceptive activities of a novel diarylpentanoid analogue, 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol, and its possible mechanisms of action in mice
title_fullStr Antinociceptive activities of a novel diarylpentanoid analogue, 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol, and its possible mechanisms of action in mice
title_full_unstemmed Antinociceptive activities of a novel diarylpentanoid analogue, 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol, and its possible mechanisms of action in mice
title_sort antinociceptive activities of a novel diarylpentanoid analogue, 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol, and its possible mechanisms of action in mice
publisher Nature Research
publishDate 2021
url http://psasir.upm.edu.my/id/eprint/95923/
https://www.nature.com/articles/s41598-021-02961-1
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