Abstract
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.
Highlights
The sensation of pain is extremely essential in serving as a warning sign to the nervous and defense systems for the purpose of minimising further tissue damage in the body
Our research group had recently synthesised a series of 2-benzoyl-6-benzylidenecyclohexanone analogues, which is a novel family of diarylpentanoids, formed by integrating the α,β-unsaturated β-diketone and cyclohexanone moieties
It’s worth to highlight that the highest dose of BBHC (3.0 mg/kg) showed better suppression in nociceptive activity as compared to acetylsalicylic acid (ASA) and morphine
Summary
The sensation of pain is extremely essential in serving as a warning sign to the nervous and defense systems for the purpose of minimising further tissue damage in the body. Our research group had recently synthesised a series of 2-benzoyl-6-benzylidenecyclohexanone analogues, which is a novel family of diarylpentanoids, formed by integrating the α,β-unsaturated β-diketone and cyclohexanone moieties. Among these 2-benzoyl-6-benzylidenecyclohexanone analogues, a newly synthesised compound called 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol (BBHC). The in vitro study strongly suggested BBHC as a potent NO inhibitor, with I C50 value of 15.2 μM as compared to other analogues of diarylpentanoids[4] Based on these supportive findings, the objectives of the present study were to examine the antinociceptive activities and the potential mechanism of action in BBHC-induced antinociception via chemical- and thermal-induced nociception murine models
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