摘要
目的研究常用的中药止疼药蜈蚣、三七和川芎对NaV1.7离子通道的抑制作用(疼痛的抑制)和NaV1.5离子通道的影响(心脏安全性进行评估)。方法采用超蒸水和95%的乙醇对药物进行提取。NaV1.7离子通道,NaV1.5离子通道和hERG离子通道分别在HEK293细胞中稳定表达,然后使用全细胞膜片钳技术,研究药物分别对这些通道的作用。同时,采用动物行为学实验测试了药物的镇痛作用。结果在本研究中,蜈蚣的水提取物(50μg/ml)、三七的水提取物(150μg/ml)、川芎的水提取物(250μg/ml)对NaV1.7离子通道的抑制作用分别为(22.65±2.78)%、(4.52±0.02)%和(15.49±1.95)%;川芎醇提取物、三七醇提取物、蜈蚣的醇提取物(50μg/ml)对NaV1.7离子通道抑制作用分别为(38.35±5.15)%、(39.80±17.52)%和(91.67±4.16)%。NaV1.7离子通道和NaV1.5离子通道的蜈蚣乙醇提取物抑制作用呈剂量依赖性,NaV1.7和NaV1.5离子通道抑制的IC50值分别为(0.30±0.09)μg/ml和(0.27±0.02)μg/ml。此外,蜈蚣乙醇提取物对hERG通道的抑制作用较弱,IC50值为(16.47±6.96)μg/ml。在动物行为实验中,蜈蚣的水提取物(15 mg/ml)与曲马多显示出相似的镇痛作用。结论通过膜片钳技术和行为学实验发现:这三种中药止痛成份易溶于乙醇,不易溶解于水;蜈蚣醇提取物在这些药物提取物中对抑制疼痛效果最好。但是当使用蜈蚣药酒时,应注意其心脏安全性的影响。
Objective In the present study,we try to evaluate the inhibition effects on NaV1.7 ion channel(inhibit of pain)and influence on NaV1.5 ion channel(the cardiac safety)of traditional Chinese analgesic medicine Centipede,Panax notoginseng and Ligusticum wallichii.Methods Here,drugs were heat-extracted by distilled water and 95%alcohol.Then,using whole-cell patch-clamp technique,we investigated the effects of these drugs on hNaV1.7,hNaV1.5 and hERG channels that are stably expressed in HEK 293 cells,respectively.Also,animal behavioral experiment was used to test the analgesic effects.Results In this study,the hNaV1.7 inhibition effects of centipede water extract(CWE)(50μg/mL),Panax notoginseng water extract(PNWE)(150μg/mL),Ligusticum wallichii water extract(LWWE)(250μg/ml)and centipedealcohol extract(CAE)(50μg/ml),Panax notoginseng alcohol extract(PNAE)(50μg/ml),Ligusticum chuanxiong alcohol extract(LCAE)(50μg/mL)were(22.65±2.78)%,(4.52±0.02)%,(15.49±1.95)%and(91.67±4.16)%,(39.80±17.52)%,(38.35±5.15)%.The CAE inhibition effects on hNaV1.7 and hNaV1.5 are dose-dependent and the calculated IC50 value is(0.30±0.09)ug/ml and(0.27±0.02)μg/ml for hNaV1.7 and hNaV1.5,respectively.Also,the CAE had weaker inhibition effect on hERG channels with IC50 value(16.47±6.96)μg/ml.In the animal behavioral experiment,CAE(15 mg/ml)shown similar analgesic effects with tramadol.Conclusions Through patch clamp and behavioral experiment,we find that these drugs are easy to dissolve in alcohol.Centipede alcohol extracts might have the best effect to alleviate pain sensation in these drug extracts.But when using medicinal liquor of centipede,the cardiac safety should be noticed.
作者
申小年
周爱民
赵忠
Shen Xiaonian;Zhou Aimin;Zhao Zhong(Anhui college of traditional Chinese medicine,Wuhu,Anhui,241000,China)
出处
《齐齐哈尔医学院学报》
2021年第18期1565-1569,共5页
Journal of Qiqihar Medical University
基金
安徽高校自然科学研究重点项目计划(KJ2016A421)。
关键词
蜈蚣
三七
川芎
镇痛药
NaV1.7离子通道
Centipede
Panax notoginseng
Ligusticum wallichii
Painkillers
NaV1.7 ion channel
