Department of Pharmacology, Meenakshi Ammal Dental College, Chennai, India.
Pharmacol Biochem Behav. 2010 Jul;96(1):1-6. doi: 10.1016/j.pbb.2010.03.010. Epub 2010 Mar 24.
This study was designed to evaluate the antinociceptive action of four dihydroxy flavone derivatives; 3,3'-dihydroxy flavone, 5,6-dihydroxy flavone, 3,7-dihydroxy flavone and 6,3'-dihydroxy flavone and to investigate the mechanisms involved.
The antinociceptive effect of dihydroxy flavones was investigated in mice employing acetic acid induced abdominal constrictions, formalin-induced nociception, and hot plate assay procedures. The effects following pretreatment with naloxone, yohimbine, ondansetron, haloperidol, bicuculline and glibenclamide were also studied by acetic acid assay to reveal the involvement of opioid, adrenergic, tryptaminergic, dopaminergic, GABAergic or potassium channels respectively in the antinociceptive action of these compounds.
Dihydroxy flavone derivatives significantly reduced the number of abdominal constrictions in acetic acid assay. The paw licking response time during both the early and late phases of formalin-induced nociception was reduced in a dose dependent manner by dihydroxy flavones treatment. A significant increase in reaction time was also evident in hot plate assay after dihydroxy flavones treatment. The antinociceptive effect of dihydroxy flavones in the acetic acid assay was significantly attenuated by pretreatment with either naloxone or bicuculline. However, pretreatment of animals with yohimbine, ondansetron, haloperidol, or glibenclamide did not alter the response.
All the four investigated dihydroxy flavones produced dose related antinociception through mechanisms that involve an interaction with opioid and GABAergic pathways.
本研究旨在评估四种二羟基黄酮衍生物;3,3'-二羟基黄酮、5,6-二羟基黄酮、3,7-二羟基黄酮和 6,3'-二羟基黄酮的镇痛作用,并探讨其涉及的机制。
采用醋酸诱导的腹部收缩、甲醛诱导的疼痛和热板试验程序,在小鼠中研究二羟基黄酮的镇痛作用。还通过醋酸试验研究纳洛酮、育亨宾、昂丹司琼、氟哌啶醇、荷包牡丹碱和格列本脲预处理后的作用,以揭示阿片类、肾上腺素能、色胺能、多巴胺能、GABA 能或钾通道分别参与这些化合物的镇痛作用。
二羟基黄酮衍生物显著减少了醋酸试验中的腹部收缩次数。二羟基黄酮处理后,甲醛诱导的疼痛的早期和晚期阶段的爪舔反应时间呈剂量依赖性减少。二羟基黄酮处理后,热板试验中的反应时间也明显增加。在醋酸试验中,二羟基黄酮的镇痛作用被纳洛酮或荷包牡丹碱预处理显著减弱。然而,育亨宾、昂丹司琼、氟哌啶醇或格列本脲预处理动物不会改变反应。
所有四种研究的二羟基黄酮都通过与阿片类和 GABA 能途径相互作用产生剂量相关的镇痛作用。