几种强心苷类成分的镇痛活性

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(P0.05,P0.01),也能使醋酸所致小鼠扭体次数减少(P0.05,P0.01);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(P0.05,P0.01)。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。

Analgesic Activity of Several Cardiac Glycosides

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.