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 (DHHPD), 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 DHHPD on the vanilloid and glutamatergic systems were evaluated through the capsaicin- and glutamate-induced paw licking tests. Results showed that DHHPD significantly (p < 0.05) attenuated the writhing response produced by the 0.8% acetic acid injection. In addition, 1 and 3 mg/kg of DHHPD significantly (p < 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, DHHPD decreased the licking latency of mice in the capsaicin- and glutamate-induced paw licking tests in a dose response manner. In conclusion, DHHPD 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.

中文翻译：

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5-（3,4-二羟基苯基）-3-羟基-1-（2-羟基苯基）penta-2,4-dien-1-one在伤害性实验动物模型中的镇痛作用。

据报道，姜黄素衍生自姜黄根茎，具有抗伤害感受，抗氧化和消炎的作用。我们评估了新型合成姜黄素类似物5-（3,4-二羟基苯基）-3-羟基-1-（2-羟基苯基）penta-2,4-dien-1-one（DHHPD）的外周和中央镇痛活性通过伤害感受的化学模型和热模型，分别以0.1、0.3、1和3 mg / kg（腹膜内）的剂量给药。DHHPD对辣椒素和谷氨酸能系统的作用是通过辣椒素和谷氨酸诱导的舔舔试验来评估的。结果表明，DHHPD显着（p <0.05）减弱了注射0.8％乙酸产生的扭曲反应。此外，1和3 mg / kg的DHHPD显着（p <0.05）减少了每只小鼠在2个阶段的两个阶段所花费的舔舔时间。5％福尔马林测试并增加了热板上小鼠的反应潜伏期。但是，后者产生的作用并未被非选择性阿片受体拮抗剂纳洛酮逆转。尽管如此，在辣椒素和谷氨酸诱导的爪舔试验中，DHHPD以剂量反应方式减少了小鼠的舔潜伏期。总之，DHHPD可能通过抑制促炎性介质的合成和/或释放，以及调节香草醛和谷氨酸能系统而对外周和中枢镇痛活性无明显作用，而对视皮醇系统没有明显作用。DHHPD以剂量反应方式降低了辣椒素和谷氨酸诱导的爪舔试验中小鼠的舔潜伏期。总之，DHHPD可能通过减弱促炎性介质的合成和/或释放，以及调节类香草酸和谷氨酸能系统，而对视皮醇能系统没有明显作用，因此显示出优异的外周和中枢镇痛活性。DHHPD以剂量反应方式减少了辣椒素和谷氨酸诱导的爪舔试验中小鼠的舔潜伏期。总之，DHHPD可能通过抑制促炎性介质的合成和/或释放，以及调节香草醛和谷氨酸能系统而对外周和中枢镇痛活性无明显作用，而对视皮醇系统没有明显作用。