Shajib Md Shafiullah, Rashid Ridwan B, Ming Long C, Islam Shanta, Sarker Md Moklesur R, Nahar Lutfun, Sarker Satyajit D, Datta Bidyut K, Rashid Mohammad A
Department of Pharmacy, Stamford University Bangladesh, Dhaka, Bangladesh.
Department of Pharmacy, State University of Bangladesh, Dhaka, Bangladesh.
Front Pharmacol. 2018 Feb 20;9:85. doi: 10.3389/fphar.2018.00085. eCollection 2018.
Polymethoxylavones (PMFs) are known to exhibit significant anti-inflammatory and neuroprotective properties. , an annual Bangladeshi herb, is rich in polymethoxyflavones that possess significant analgesic and anxiolytic activities. The present study aimed to determine the antinociceptive and neuropharmacological activities of polyoxygenated flavonoids namely- 3,3',5,6,7,8-hexamethoxy-4',5'-methylenedioxyflavone (), 3,3',4',5',5,6,7,8-octamethoxyflavone (exoticin) (), 6,7,4',5'-dimethylenedioxy-3,5,3'-trimethoxyflavone (), and 3,3',4',5,5',8-hexamethoxy-6,7-methylenedioxyflavone (), isolated and identified from . Antinociceptive activity was assessed using the acetic-acid induced writhing, hot plate, tail immersion, formalin and carrageenan-induced paw edema tests, whereas neuropharmacological effects were evaluated in the hole cross, open field and elevated plus maze test. Oral treatment of compounds , , and (12.5-25 mg/kg b.w.) exhibited dose-dependent and significant ( < 0.01) antinociceptive activity in the acetic-acid, formalin, carrageenan, and thermal (hot plate)-induced pain models. The association of ATP-sensitive K channel and opioid systems in their antinociceptive effect was obvious from the antagonist effect of glibenclamide and naloxone, respectively. These findings suggested central and peripheral antinociceptive activities of the compounds. Compound , , and (12.5 mg/kg b.w.) demonstrated significant ( < 0.05) anxiolytic-like activity in the elevated plus-maze test, while the involvement of GABA receptor in the action of compound and was evident from the reversal effects of flumazenil. In addition, compounds and (12.5-25 mg/kg b.w) exhibited anxiolytic activity without altering the locomotor responses. The present study suggested that the polymethoxyflavones () from could be considered as suitable candidates for the development of analgesic and anxiolytic agents.
多甲氧基黄酮(PMFs)具有显著的抗炎和神经保护特性。[植物名称]是一种一年生的孟加拉草药,富含具有显著镇痛和解焦虑活性的多甲氧基黄酮。本研究旨在确定从[植物名称]中分离鉴定出的多氧化黄酮类化合物,即3,3',5,6,7,8 - 六甲氧基 - 4',5'-亚甲二氧基黄酮([化合物名称1])、3,3',4',5',5,6,7,8 - 八甲氧基黄酮(异紫铆因)([化合物名称2])、6,7,4',5'-二甲烯二氧基 - 3,5,3'-三甲氧基黄酮([化合物名称3])和3,3',4',5,5',8 - 六甲氧基 - 6,7 - 亚甲二氧基黄酮([化合物名称4])的抗伤害感受和神经药理学活性。使用乙酸诱导扭体、热板、尾浸、福尔马林和角叉菜胶诱导的爪肿胀试验评估抗伤害感受活性,而在洞板、旷场和高架十字迷宫试验中评估神经药理学作用。化合物[化合物名称1]、[化合物名称2]和[化合物名称3](12.5 - 25 mg/kg体重)口服给药在乙酸、福尔马林、角叉菜胶和热(热板)诱导的疼痛模型中表现出剂量依赖性且显著(P < 0.01)的抗伤害感受活性。格列本脲和纳洛酮的拮抗作用分别表明ATP敏感性钾通道和阿片样物质系统在其抗伤害感受作用中的关联。这些发现提示了这些化合物的中枢和外周抗伤害感受活性。化合物[化合物名称1]、[化合物名称2]和[化合物名称3](12.5 mg/kg体重)在高架十字迷宫试验中表现出显著(P < 0.05)的抗焦虑样活性,而氟马西尼的逆转作用表明GABA受体参与了化合物[化合物名称1]和[化合物名称2]的作用。此外,化合物[化合物名称1]和[化合物名称2](12.5 - 25 mg/kg体重)表现出抗焦虑活性且不改变运动反应。本研究表明,来自[植物名称]的多甲氧基黄酮(PMFs)可被视为开发镇痛和解焦虑药物的合适候选物。