羟基积雪草酸的镇痛活性及其作用机制研究
Anti-nociceptive effect and mechanism of madecassic acid
白溪山 1邓超锐 1李育晓 1李红锐 1李艳红 1黄相中1
作者信息
- 1. 云南民族大学民族医药学院民族药资源化学国家民委-教育部重点实验室,昆明 650504
- 折叠
摘要
目前对积雪草的功效成分研究主要集中在三萜皂苷类成分,对其他成分的药理活性研究较少.本研究采用小鼠醋酸扭体实验、热板法实验和福尔马林实验,对羟基积雪草酸的镇痛活性进行探究.实验分为对照组、阳性药阿司匹林组和低(10 mg/kg)、中(20 mg/kg)、高(40 mg/kg)剂量的羟基积雪草酸(MA)组.同时,还采用阿片受体阻断实验,辣椒素和谷氨酸诱导的小鼠舔爪实验,对其镇痛机制进行研究.结果显示:MA在醋酸扭体实验和福尔马林实验的Ⅱ阶段表现出显著的镇痛活性;在醋酸扭体实验和福尔马林实验中,MA的镇痛活性没有被纳洛酮明显减弱;中、高剂量的MA均能有效地减轻由辣椒素所引起的疼痛,抑制率分别为 29.5%和 64.4%,还能有效地缩减由谷氨酸所引起的舔爪时间,抑制率分别为 30.9%和56.1%.研究结果表明:MA可通过作用于外周神经系统发挥较好的镇痛作用;该化合物产生的镇痛活性可能涉及谷氨酸能系统和TRPV1的调节,但不涉及阿片能系统.
Abstract
To date,the investigation of the functional composition of Centella asiatica(L.)Urban has been mainly focused on the triterpenoid saponins,with little research on the other compositions.The acetic acid-induced writhing,Eddy's hot plate and formalin tests were employed to investigate the anti-nociceptive effects of madecassic acid(MA).The experiment was divided into normal control group,acetylsalicylic acid(ASA)group,and the MA groups of low(10 mg/kg),medium(20 mg/kg)and high(40 mg/kg)dosage.Meanwhile,the anti-nociceptive effect of MA on the acetic acid and formalin-induced nociceptive models in the absence and presence of NAL(naloxone hydrochloride)was evaluated.To have an insight into the anti-nociceptive mechanisms of MA,the capsaicin-and glutamate-induced paw licking tests were also employed to evaluate the involvement of the vanilloid and glutamatergic systems,respectively.Results showed that MA exhibited good anti-nociceptive activity in the acetic acid-induced writhing test and the second phase of formalin test;the anti-nociceptive effect of MA in both the acetic acid and formalin-induced nociception was not effectively removed by NAL;MA(20 mg/kg and 40 mg/kg)effectively reduced the duration of biting/licking the capsaicin-injected paw with inhibition rates of 29.5%and 64.4%,respectively;MA(20 mg/kg and 40 mg/kg)distinctly shortened the time spent in biting/licking the glutamate-injected paw by 30.9%and 56.1%,respectively.In summary,MA induces significant peripheral anti-nociceptive effect,and the anti-nociceptive activities probably involve the modulation of glutamatergic systems and vanilloid systems(TRPV1)instead of the opioidergic system.
关键词
羟基积雪草酸/镇痛/TRPV1/谷氨酸能系统Key words
madecassic acid/analgesia/transient receptor potential vanilloid-1(TRPV1)/glutamatergic systems引用本文复制引用
基金项目
国家自然科学基金(81960783)
云南省科技重大专项(202102AA100018)
云南省基础研究计划重点项目(202201AS070012)
云南省基础研究计划青年项目(202201AU070045)
出版年
2024
国家科技期刊平台
NSTL
万方数据