Li Chun-Li, Zhang Jing-Hai, Yang Bao-Feng, Jiao Jun-Dong, Wang Ling, Wu Chun-Fu
Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Regul Pept. 2006 Jan 15;133(1-3):74-81. doi: 10.1016/j.regpep.2005.09.022. Epub 2005 Oct 17.
A new recombinant neurotoxic polypeptide ANEPIII (BmK ANEPIII) derived from Scorpion peptide, which was demonstrated with antineuroexcitation properties in animal models, was examined for its action on K+ currents in primary cultured rat hippocampal and cortical neurons using the patch clamp technique in the whole-cell configuration. The delayed rectifier K+ current (I(k)) was inhibited by externally applied recombinant BmK ANEPIII, while the transient A-current (I(A)) remained virtually unaffected. BmK ANEPIII 3 microM, reduced the delayed rectifier current by 28.2% and 23.6% in cultured rat hippocampal and cortical neurons, respectively. The concentration of half-maximal block was 155.1 nM for hippocampal neurons and 227.2 nM for cortical neurons, respectively. These results suggest that BmK ANEPIII affect K+ currents, which may lead to a reduction in neuronal excitability.
一种源自蝎肽的新型重组神经毒性多肽ANEPIII（东亚钳蝎ANEPIII），在动物模型中已证实具有抗神经兴奋特性，本研究采用全细胞模式的膜片钳技术，检测其对原代培养的大鼠海马和皮层神经元钾离子电流的作用。外源性应用重组东亚钳蝎ANEPIII可抑制延迟整流钾电流（I(k)），而瞬时A电流（I(A)）几乎不受影响。3 microM的东亚钳蝎ANEPIII分别使培养的大鼠海马和皮层神经元的延迟整流电流降低了28.2%和23.6%。海马神经元和皮层神经元的半数最大阻断浓度分别为155.1 nM和227.2 nM。这些结果表明，东亚钳蝎ANEPIII影响钾离子电流，这可能导致神经元兴奋性降低。
