Department of Pharmacology, Mamata Medical College, Rotarynagar, Khammam, Telangana, 507002, India.
Department of Pharmacology, Faculty of Medicine, Texila American University, Georgetown, Guyana.
Inflammopharmacology. 2019 Dec;27(6):1155-1167. doi: 10.1007/s10787-019-00579-4. Epub 2019 Mar 8.
Previous reports suggest flavonoids as potent analgesic compounds. Based on these observations, the present study investigated the antinociceptive action of flavonol, 3', 4'-dimethoxy flavonol, 6, 3'-dimethoxy flavonol, 7, 2'-dimethoxy flavonol, and 7, 3'-dimethoxy flavonol and the possible mechanisms involved in these effects. The antinociceptive effect of the investigated compounds in doses of 25, 50, 100, and 200 mg/kg was evaluated in male Swiss albino mice using the acetic acid test, formalin-induced nociception, and hot water tail immersion test. The role of opioid, tryptaminergic, adrenergic, dopaminergic, GABAergic, and K channels in producing the antinociceptive effect was also studied using appropriate interacting agents. Treatment with flavonol and dimethoxy flavonols resulted in a significant reduction in the number of abdominal constrictions in the acetic acid test, a significant inhibition of the paw-licking/biting response time in both the phases of formalin nociception and also a significant increase in mean reaction time in the hot water tail immersion test. These observations revealed the antinociceptive effect of dimethoxy flavonols. The role of opioid, serotonergic (5HT), and dopaminergic system was identified in the antinociceptive effect of flavonol and all dimethoxy derivatives investigated. In addition, the role of GABAergic, K channel, and α-2 adrenergic mechanisms were also observed in the antinociceptive action of some of the investigated compounds. The present study identified the antinociceptive effect of flavonol and dimethoxy flavonols in mice acting through different neuronal pathways.
先前的报告表明,类黄酮是一种有效的镇痛化合物。基于这些观察结果,本研究调查了黄酮醇、3',4'-二甲氧基黄酮醇、6,3'-二甲氧基黄酮醇、7,2'-二甲氧基黄酮醇和 7,3'-二甲氧基黄酮醇的镇痛作用及其可能涉及的机制。在雄性瑞士白化小鼠中,使用醋酸试验、甲醛诱导的疼痛和热水尾巴浸入试验,评估了研究化合物在 25、50、100 和 200mg/kg 剂量下的镇痛作用。还使用适当的相互作用剂研究了阿片样物质、色胺能、肾上腺素能、多巴胺能、GABA 能和 K 通道在产生镇痛作用中的作用。黄酮醇和二甲氧基黄酮醇的治疗导致醋酸试验中腹部收缩次数显著减少,甲醛疼痛的两个阶段中舔足/咬足反应时间显著抑制,以及热水尾巴浸入试验中平均反应时间显著增加。这些观察结果揭示了二甲氧基黄酮醇的镇痛作用。阿片样物质、5-羟色胺(5HT)和多巴胺能系统在黄酮醇和所有研究的二甲氧基衍生物的镇痛作用中发挥了作用。此外,还观察到 GABA 能、K 通道和α-2 肾上腺素能机制在一些研究化合物的镇痛作用中发挥作用。本研究确定了黄酮醇和二甲氧基黄酮醇在小鼠中的镇痛作用,这些作用通过不同的神经元途径发挥。