摘要
为了从海南产桶形芋螺(Conus betulins Linnaeus)的毒液中发现作用于烟碱型乙酰胆碱受体(nAChRs)不同亚型的天然毒素,本研究利用高效液相色谱法,从桶形芋螺的毒液中分离和纯化了天然毒素组分,并以非洲爪蟾卵母细胞表达的nAChRs各种亚型为药靶,采用双电极电压钳电生理技术,筛选了作用于nAChRs不同亚型的天然芋螺毒素组分.结果显示:通过分离和纯化方法,从桶形芋螺的毒液中获得了16个天然毒素组分,此后测定了每个组分对nAChRs各个亚型的阻断活性,同时发现组分CBL-2,CBL-3和CBL-4对肌肉型(α1β1δε)nAChR具有强阻断活性;组分CBL-12对α4β2 nAChR亚型有阻断作用;组分CBL-4和CBL-5对α3β2 nAChR亚型有阻断作用.由此认为:这5个天然毒素组分分别对α3β2,α4β2和α1β1δεnAChR这三种亚型有阻断活性,特别是其能阻断α4β2 nAChR亚型的活性,在此之前还未发现α4β2 nAChR亚型的特异阻断剂.
To obtain the native toxins from the venom of Conus betulinus L. from Hainan,which act on different subtypes of nicotinic acetylcholine receptors（nAChRs）,in the study,the high performance liquid chromatography method was used to isolate and purify the native toxin factions from C. betulinus L. crude venom,Various subtypes of nAChRs expressed in Xenopus oocytes were used as drug targets. Electrophysiology technology of two-electrode voltage clamp was used to screen the toxin fraction on different nAChR subtypes. The results indicated that 16 natural toxin fractions were obtained from C. betulinus L. venom,CBL-2,CBL-3,and CBL-4,had strong blocking effect on α1β1δε nAChR,CBL-4 and CBL-5 were potent to block α3β2 nAChR,CBL-12 had inhibition effects on α4β2 nAChR. So,The five toxin fractions were observed to be active on α3β2,α4β2,and α1β1δε nAChR subtypes,respectively. Especially,it was the first report about the special antagonist of theα4β2 nAChR subtype CBL-12.
作者
黄艺
付双玉
朱晓鹏
长孙东亭
罗素兰
Huang Yi1,2, Fu Shuangyu1 , Zhu Xiaopeng1 , Zhangsun Dongting1 , Luo Sulan1(1. Key Laboratory of Tropical Biological Resources of Ministry of Education, Key Lab for Mm＇ine Drug of Haikou, Haikou 570228, China; 2. College of Tropical Agriculture and Forestry, Hainan University, Haikou 570228, China)
出处
《海南大学学报（自然科学版）》
CAS
2018年第2期124-132,共9页
Natural Science Journal of Hainan University
基金
国家自然科学基金重点国际合作项目(81420108028)
国家自然科学基金(31760249)
长江学者和创新团队发展计划(IRT-15R15)
海南省高等学校科学研究项目(Hnky2017-16)
关键词
桶形芋螺毒液
天然芋螺毒素
烟碱型乙酰胆碱受体
电生理技术
Conus betulinus L. venom
native conotoxins
nicotinic acetylcholine receptor
electrophysiologytechnology
