Department of Veterinary Preclinical Sciences, Faculty of Veterinary Medicine, Universiti Putra Malaysia, Serdang 43400, Selangor, Malaysia.
Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang 43400, Selangor, Malaysia.
Molecules. 2018 Aug 21;23(9):2099. 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.
姜黄根茎中提取的姜黄素类化合物已被报道具有镇痛、抗氧化和抗炎活性。我们评估了 5-(3,4-二羟基苯基)-3-羟基-1-(2-羟基苯基)戊-2,4-二烯-1-酮 (),一种新型合成姜黄素类似物,在 0.1、0.3、1 和 3 mg/kg(腹腔内)时,通过化学和热疼痛模型的外周和中枢镇痛活性。通过辣椒素和谷氨酸诱导的爪舔试验评估了对香草素和谷氨酸能系统的影响。结果表明, ()显著(<0.05)减弱了 0.8%乙酸注射引起的扭体反应。此外,1 和 3 mg/kg 的 ()显著(<0.05)减少了 2.5%福马林试验的两个阶段中每只小鼠舔爪的时间,并增加了热板上小鼠的反应潜伏期。然而,在后一种情况下,非选择性阿片受体拮抗剂纳洛酮并不能逆转这种作用。尽管如此,()以剂量反应的方式降低了辣椒素和谷氨酸诱导的爪舔试验中小鼠的舔舐潜伏期。总之,()表现出优异的外周和中枢镇痛活性,可能是通过减轻合成和/或释放促炎介质,以及调节香草素和谷氨酸能系统,而对阿片能系统没有明显影响。