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Molecules 2016, 21(8), 1077; doi:10.3390/molecules21081077

Antinociceptive Effect of 3-(2,3-Dimethoxyphenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one in Mice Models of Induced Nociception

1
Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 Serdang, Malaysia
2
Faculty of Pharmaceutical Sciences, UCSI University, 56000 Cheras, Malaysia
3
Laboratory of Natural Products, Institute of Bioscience, Universiti Putra Malaysia, 43400 Serdang, Malaysia
4
Faculty of Industrial Sciences & Technology, University Malaysia Pahang, 26300 Gambang, Malaysia
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 28 June 2016 / Revised: 11 August 2016 / Accepted: 12 August 2016 / Published: 22 August 2016
(This article belongs to the Section Natural Products)
View Full-Text   |   Download PDF [2992 KB, uploaded 22 August 2016]   |  

Abstract

The antinociceptive effects produced by intraperitoneal administration of a novel synthetic chalcone, 3-(2,3-dimethoxyphenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one (DMFP), were investigated in several mouse models of induced nociception. The administration of DMFP (0.1, 0.5, 1.0 and 5.0 mg/kg) produced significant attenuation on the acetic acid-induced abdominal-writhing test. It also produced a significant increase in response latency time in the hot-plate test and a marked reduction in time spent licking the injected paw in both phases of the formalin-induced paw-licking test. In addition, it was also demonstrated that DMFP exhibited significant inhibition of the neurogenic nociceptive response induced by intraplantar injections of capsaicin and glutamate. Moreover, the antinociceptive effect of DMFP in the acetic acid-induced abdominal-writhing test and the hot-plate test was not antagonized by pretreatment with a non-selective opioid receptor antagonist, naloxone. Finally, DMFP did not show any toxic effects and/or mortality in a study of acute toxicity and did not interfere with motor coordination during the Rota-rod test. Our present results show that DMFP exhibits both peripheral and central antinociceptive effects. It was suggested that its peripheral antinociceptive activity is associated with attenuated production and/or release of NO and various pro-inflammatory mediators, while central antinociceptive activity seems to be unrelated to the opioidergic system, but could involve, at least in part, an interaction with the inhibition of capsaicin-sensitive fibers and the glutamatergic system. View Full-Text
Keywords: 3-(2,3-dimethoxyphenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one; chalcone; antinociceptive activity; opioidergic system; TRPV1 receptor; glutamatergic system 3-(2,3-dimethoxyphenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one; chalcone; antinociceptive activity; opioidergic system; TRPV1 receptor; glutamatergic system
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MDPI and ACS Style

Ismail, N.I.; Ming-Tatt, L.; Lajis, N.; Akhtar, M.N.; Akira, A.; Perimal, E.K.; Israf, D.A.; Sulaiman, M.R. Antinociceptive Effect of 3-(2,3-Dimethoxyphenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one in Mice Models of Induced Nociception. Molecules 2016, 21, 1077.

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