Biochemical and electrophysiological characterization of two sea anemone type 1 potassium toxins from a geographically distant population of Bunodosoma caissarum.

Biochemical and electrophysiological characterization of two sea anemone type 1 potassium toxins from a geographically distant population of Bunodosoma caissarum.
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DOI:
10.3390/md11030655
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发表时间:
2013-03-06
期刊:
影响因子:
5.4
通讯作者:
Tytgat J
Tytgat J
中科院分区:
医学2区
文献类型:
--
作者:
Orts DJ;Peigneur S;Madio B;Cassoli JS;Montandon GG;Pimenta AM;Bicudo JE;Freitas JC;Zaharenko AJ;Tytgat J

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海葵毒素是研究电压门控钾通道(KV)药理学和结构功能的重要工具。这些神经毒素根据其结构和作用方式可分为四种不同类型。本研究首次从巴西圣彼得和圣保罗群岛的白蛇蛇毒中分离纯化了两种毒素。序列比对和系统发育分析表明BcsTx 1和BcsTx 2是海葵1型钾通道毒素的最新成员。通过对KV通道的12种不同亚型(KV1.1-KV1.6; KV2.1; KV3.1; KV4.2; KV4.3; hERG和Shaker IR)进行广泛的电生理学筛选,对其进行功能表征。与rKv1.6、hKv1.3、Shaker IR和rKv1.1相比,BcsTx 1对rKv1.2显示出高亲和力,而与hKv1.3、rKv1.1、Shaker IR和rKv1.2相比,Bcstx 2有效地阻断了rKv1.6。此外,我们还首次报道了两个地理上遥远的海葵种群之间的毒液成分和生物活性比较。
Sea anemone (Cnidaria, Anthozoa) venom is an important source of bioactive compounds used as tools to study the pharmacology and structure-function of voltage-gated K+ channels (KV). These neurotoxins can be divided into four different types, according to their structure and mode of action. In this work, for the first time, two toxins were purified from the venom of Bunodosoma caissarum population from Saint Peter and Saint Paul Archipelago, Brazil. Sequence alignment and phylogenetic analysis reveals that BcsTx1 and BcsTx2 are the newest members of the sea anemone type 1 potassium channel toxins. Their functional characterization was performed by means of a wide electrophysiological screening on 12 different subtypes of KV channels (KV1.1–KV1.6; KV2.1; KV3.1; KV4.2; KV4.3; hERG and Shaker IR). BcsTx1 shows a high affinity for rKv1.2 over rKv1.6, hKv1.3, Shaker IR and rKv1.1, while Bcstx2 potently blocked rKv1.6 over hKv1.3, rKv1.1, Shaker IR and rKv1.2. Furthermore, we also report for the first time a venom composition and biological activity comparison between two geographically distant populations of sea anemones.
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