【摘要】 目的:探讨了华蟾毒精、远华蟾毒精、沙蟾毒精和杠柳苷4种强心苷类成分的镇痛作用及华蟾毒精的镇痛作用机制。方法:昆明种小鼠按要求分为空白组,阿司匹林阳性组(200 mg·kg-1),各受试化合物高、中、低剂量组,采用小鼠热板法和醋酸扭体法观察4种强心苷类化合物的镇痛作用;通过注射盐酸纳洛酮(2 mg·kg-1)和外周阿片受体阻断剂(纳洛酮四价盐衍生物,NAL-M,20 mg·kg-1)初步研究华蟾毒精的镇痛作用机制。结果:与空白组比较,华蟾毒精、远华蟾毒精、沙蟾毒精和杠柳苷均能提高热板所致小鼠舔足的痛阈(P<0.05,P<0.01),也能使醋酸所致小鼠扭体次数减少(P<0.05,P<0.01);ip纳洛酮和NAL-M后,均能拮抗华蟾毒精对热板所致小鼠痛阈值的提高作用(P<0.05,P<0.01)。结论:华蟾毒精、远华蟾毒精、沙蟾毒精和杠柳苷均具有镇痛作用,且华蟾毒精的镇痛作用与外周阿片受体有一定的关联。更多还原

【Abstract】 Objective: To investigate the analgesic activity of four cardiac glycosides-cinobufagin,telocinobufagin,arenobufagin and periplocin and the analgesic mechanism of cinobufagin. Method: According to the requirements,the KM mice were divided into the blank group,the asprin positive group( 200 mg·kg- 1),and groups of high,medium and low dose of test compounds. The analgesic effects of the four cardiac glycosides in mice were observed by the hot-plate test and acetic acid writhing methods. Moreover,the potential analgesic mechanism of cinobufagin was preliminarily investigated by injecting naloxone hydrochloride( 2 mg·kg- 1) and peripheral opioid receptor antagonist naloxone methiodide( NAL-M,20 mg·kg- 1). Result: Compared with the blank group,all of the four cardiac glycosides can increase the pain threshold of paw-licking induced by hot plate( P < 0. 05,P < 0. 01) and decrease the number of writhing induced by acetic acid in mice( P < 0. 05,P <0. 01). The intraperitoneal injection with naloxone hydrochloride and NAL-M can antagonize the increase in the pain threshold of paw-licking induced by hot plate( P < 0. 05, P < 0. 01). Conclusion: Cinobufagin,telocinobufagin,arenobufagin and periplocin have the analgesic effect,and the analgesic effect of cinobufagin may be correlated with the peripheral opioid receptor.更多还原