Analgesic Effect of 5-(3,4-Dihydroxyphenyl)-3-hydroxy-1-(2-hydroxyphenyl)penta-2,4-dien-1-one in Experimental Animal Models of Nociception

• Published in: Molecules (Basel, Switzerland) Switzerland), 2018-08, Vol.23 (9), p.2099
• Main Authors: Kamarudin, Nadhirah, Hisamuddin, Nadia, Ong, Hui Ming, Ahmad Azmi, Ahmad Farhan, Leong, Sze Wei, Abas, Faridah, Sulaiman, Mohd Roslan, Shaik Mossadeq, Wan Mastura
• Format: Article
• Language: English
• Subjects: 5-(3,4-dihydroxyphenyl)-3-hydroxy-1-(2-hydroxyphenyl)penta-2,4-dien-1-one; Adrenergic receptors; Analgesics; Analgesics - chemistry; Analgesics - pharmacology; Animal models; Animals; Antidepressants; antinociceptive; Behavior, Animal - drug effects; Bioavailability; Biological properties; Cannabinoid receptors; Disease Models, Animal; Drug dosages; Experiments; glutamatergic; Male; Mice; Molecular Structure; Motor Activity - drug effects; Narcotics; Natural products; Nociception - drug effects; Nociceptive Pain - drug therapy; Nociceptive Pain - etiology; Nonsteroidal anti-inflammatory drugs; opioid; Opioid receptors; Organic chemistry; Pain; Pain perception; Plant Extracts - chemistry; Plant Extracts - pharmacology; Rotarod Performance Test; Serotonin; Serotonin S1 receptors; Substance abuse treatment; Tricyclic antidepressants; turmeric; vanilloid
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules23092099

Curcuminoids derived from turmeric rhizome have been reported to exhibit antinociceptive, antioxidant and anti-inflammatory activities. We evaluated the peripheral and central antinociceptive activities of 5-(3,4-dihydroxyphenyl)-3-hydroxy-1-(2-hydroxyphenyl)penta-2,4-dien-1-one ( ), a novel synthetic curcuminoid analogue at 0.1, 0.3, 1 and 3 mg/kg (intraperitoneal), through chemical and thermal models of nociception. The effects of on the vanilloid and glutamatergic systems were evaluated through the capsaicin- and glutamate-induced paw licking tests. Results showed that significantly ( < 0.05) attenuated the writhing response produced by the 0.8% acetic acid injection. In addition, 1 and 3 mg/kg of significantly ( < 0.05) reduced the licking time spent by each mouse in both phases of the 2.5% formalin test and increased the response latency of mice on the hot-plate. However, the effect produced in the latter was not reversed by naloxone, a non-selective opioid receptor antagonist. Despite this, decreased the licking latency of mice in the capsaicin- and glutamate-induced paw licking tests in a dose response manner. In conclusion, showed excellent peripheral and central antinociceptive activities possibly by attenuation of the synthesis and/or release of pro-inflammatory mediators in addition to modulation of the vanilloid and glutamatergic systems without an apparent effect on the opioidergic system.