The fungal neurotoxin lolitrem B inhibits the function of human large conductance calcium-activated potassium channels

被引：39
作者：
Dalziel, JE
Finch, SC
Dunlop, J
机构：
[1] AgResearch, Biomembrane Grp, Grassland Res Ctr, Palmerston North 5301, New Zealand
[2] AgResearch, Ruakura Res Ctr, Hamilton, New Zealand
来源：
TOXICOLOGY LETTERS | 2005年 / 155卷 / 03期
关键词：
BK channel; lolitrem; endophyte; indole diterpene; Neotyphodium lolii;
D O I：
10.1016/j.toxlet.2004.11.011
中图分类号：
R99 [毒物学（毒理学）];
学科分类号：
100405 ;
摘要：
The effects of the mycotoxin lolitrem B on the function of hSlo large conductance calcium-activated potassium channels expressed in HEK293 cells have been investigated using inside-out membrane patches. Lolitrem B potently inhibited hSlo potassium currents activated by depolarising voltage pulses in the presence of 10 muM free calcium. At a concentration of 100 nM, lolitrem B rapidly and completely inhibited outward potassium currents. The concentration that produced half-maximal inhibition was 3.7 nM, indicating a high apparent affinity for hSlo channels. This is the first time that a molecular site of action has been identified for a compound of the lolitrem structural class of indole diterpene and identifies a novel BK channel blocker. (C) 2004 Elsevier Ireland Ltd. All rights reserved.
引用
收藏
页码：421 / 426
页数：6
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