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Antinociceptive activity of a synthetic curcuminoid analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone, on nociception-induced models in mice.
Basic Clin Pharmacol Toxicol 2012; 110(3):275-82BC

Abstract

This study investigated the potential antinociceptive efficacy of a novel synthetic curcuminoid analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone (BHMC), using chemical- and thermal-induced nociception test models in mice. BHMC (0.03, 0.1, 0.3 and 1.0 mg/kg) administered via intraperitoneal route (i.p.) produced significant dose-related inhibition in the acetic acid-induced abdominal constriction test in mice with an ID(50) of 0.15 (0.13-0.18) mg/kg. It was also demonstrated that BHMC produced significant inhibition in both neurogenic (first phase) and inflammatory phases (second phase) of the formalin-induced paw licking test with an ID(50) of 0.35 (0.27-0.46) mg/kg and 0.07 (0.06-0.08) mg/kg, respectively. Similarly, BHMC also exerted significant increase in the response latency period in the hot-plate test. Moreover, the antinociceptive effect of the BHMC in the formalin-induced paw licking test and the hot-plate test was antagonized by pre-treatment with the non-selective opioid receptor antagonist, naloxone. Together, these results indicate that the compound acts both centrally and peripherally. In addition, administration of BHMC exhibited significant inhibition of the neurogenic nociception induced by intraplantar injections of glutamate and capsaicin with ID(50) of 0.66 (0.41-1.07) mg/kg and 0.42 (0.38-0.51) mg/kg, respectively. Finally, it was also shown that BHMC-induced antinociception was devoid of toxic effects and its antinociceptive effect was associated with neither muscle relaxant nor sedative action. In conclusion, BHMC at all doses investigated did not cause any toxic and sedative effects and produced pronounced central and peripheral antinociceptive activities. The central antinociceptive activity of BHMC was possibly mediated through activation of the opioid system as well as inhibition of the glutamatergic system and TRPV1 receptors, while the peripheral antinociceptive activity was perhaps mediated through inhibition of various inflammatory mediators.

Authors+Show Affiliations

Department of Biomedical Science, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Selangor, Malaysia.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21967232

Citation

Ming-Tatt, Lee, et al. "Antinociceptive Activity of a Synthetic Curcuminoid Analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone, On Nociception-induced Models in Mice." Basic & Clinical Pharmacology & Toxicology, vol. 110, no. 3, 2012, pp. 275-82.
Ming-Tatt L, Khalivulla SI, Akhtar MN, et al. Antinociceptive activity of a synthetic curcuminoid analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone, on nociception-induced models in mice. Basic Clin Pharmacol Toxicol. 2012;110(3):275-82.
Ming-Tatt, L., Khalivulla, S. I., Akhtar, M. N., Mohamad, A. S., Perimal, E. K., Khalid, M. H., ... Sulaiman, M. R. (2012). Antinociceptive activity of a synthetic curcuminoid analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone, on nociception-induced models in mice. Basic & Clinical Pharmacology & Toxicology, 110(3), pp. 275-82. doi:10.1111/j.1742-7843.2011.00804.x.
Ming-Tatt L, et al. Antinociceptive Activity of a Synthetic Curcuminoid Analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone, On Nociception-induced Models in Mice. Basic Clin Pharmacol Toxicol. 2012;110(3):275-82. PubMed PMID: 21967232.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antinociceptive activity of a synthetic curcuminoid analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone, on nociception-induced models in mice. AU - Ming-Tatt,Lee, AU - Khalivulla,Shaik Ibrahim, AU - Akhtar,Muhammad Nadeem, AU - Mohamad,Azam Shah, AU - Perimal,Enoch Kumar, AU - Khalid,Mohamed Hanief, AU - Akira,Ahmad, AU - Lajis,Nordin, AU - Israf,Daud Ahmad, AU - Sulaiman,Mohd Roslan, Y1 - 2011/11/04/ PY - 2011/10/5/entrez PY - 2011/10/5/pubmed PY - 2012/6/15/medline SP - 275 EP - 82 JF - Basic & clinical pharmacology & toxicology JO - Basic Clin. Pharmacol. Toxicol. VL - 110 IS - 3 N2 - This study investigated the potential antinociceptive efficacy of a novel synthetic curcuminoid analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone (BHMC), using chemical- and thermal-induced nociception test models in mice. BHMC (0.03, 0.1, 0.3 and 1.0 mg/kg) administered via intraperitoneal route (i.p.) produced significant dose-related inhibition in the acetic acid-induced abdominal constriction test in mice with an ID(50) of 0.15 (0.13-0.18) mg/kg. It was also demonstrated that BHMC produced significant inhibition in both neurogenic (first phase) and inflammatory phases (second phase) of the formalin-induced paw licking test with an ID(50) of 0.35 (0.27-0.46) mg/kg and 0.07 (0.06-0.08) mg/kg, respectively. Similarly, BHMC also exerted significant increase in the response latency period in the hot-plate test. Moreover, the antinociceptive effect of the BHMC in the formalin-induced paw licking test and the hot-plate test was antagonized by pre-treatment with the non-selective opioid receptor antagonist, naloxone. Together, these results indicate that the compound acts both centrally and peripherally. In addition, administration of BHMC exhibited significant inhibition of the neurogenic nociception induced by intraplantar injections of glutamate and capsaicin with ID(50) of 0.66 (0.41-1.07) mg/kg and 0.42 (0.38-0.51) mg/kg, respectively. Finally, it was also shown that BHMC-induced antinociception was devoid of toxic effects and its antinociceptive effect was associated with neither muscle relaxant nor sedative action. In conclusion, BHMC at all doses investigated did not cause any toxic and sedative effects and produced pronounced central and peripheral antinociceptive activities. The central antinociceptive activity of BHMC was possibly mediated through activation of the opioid system as well as inhibition of the glutamatergic system and TRPV1 receptors, while the peripheral antinociceptive activity was perhaps mediated through inhibition of various inflammatory mediators. SN - 1742-7843 UR - https://www.unboundmedicine.com/medline/citation/21967232/Antinociceptive_activity_of_a_synthetic_curcuminoid_analogue_26_bis__4_hydroxy_3_methoxybenzylidene_cyclohexanone_on_nociception_induced_models_in_mice_ L2 - https://doi.org/10.1111/j.1742-7843.2011.00804.x DB - PRIME DP - Unbound Medicine ER -