印防己毒素通过TaALMT1描绘了苹果酸和γ-氨基丁酸的不同转运构型。
Picrotoxin Delineates Different Transport Configurations for Malate and γ Aminobutyric Acid through TaALMT1.
作者信息
Ramesh Sunita A, Long Yu, Dashtbani-Roozbehani Abolfazl, Gilliham Matthew, Brown Melissa H, Tyerman Stephen D
机构信息
Biological Sciences, College of Science and Engineering, Flinders University, Bedford Park, SA 5042, Australia.
ARC Centre of Excellence in Plant Energy Biology, Department of Plant Science, School of Agriculture, Food and Wine, Waite Research Institute, The University of Adelaide, Waite Campus, Glen Osmond, SA 5064, Australia.
出版信息
Biology (Basel). 2022 Aug 2;11(8):1162. doi: 10.3390/biology11081162.
Plant-derived pharmacological agents have been used extensively to dissect the structure-function relationships of mammalian GABA receptors and ion channels. Picrotoxin is a non-competitive antagonist of mammalian GABA receptors. Here, we report that picrotoxin inhibits the anion (malate) efflux mediated by wheat () ALMT1 but has no effect on GABA transport. The EC for inhibition was 0.14 nM and 0.18 nM when the ALMTs were expressed in tobacco BY2 cells and in oocytes, respectively. Patch clamping of the oocyte plasma membrane expressing wheat ALMT1 showed that picrotoxin inhibited malate currents from both sides of the membrane. These results demonstrate that picrotoxin inhibits anion efflux effectively and can be used as a new inhibitor to study the ion fluxes mediated by ALMT proteins that allow either GABA or anion transport.
植物源药理剂已被广泛用于剖析哺乳动物γ-氨基丁酸（GABA）受体和离子通道的结构-功能关系。印防己毒素是哺乳动物GABA受体的非竞争性拮抗剂。在此，我们报告印防己毒素抑制小麦（）苹果酸转运蛋白1（ALMT1）介导的阴离子（苹果酸）外流，但对GABA转运没有影响。当ALMTs分别在烟草BY2细胞和非洲爪蟾卵母细胞中表达时，抑制作用的半数有效浓度（EC）分别为0.14 nM和0.18 nM。对表达小麦ALMT1的卵母细胞质膜进行膜片钳记录显示，印防己毒素从膜的两侧抑制苹果酸电流。这些结果表明，印防己毒素能有效抑制阴离子外流，可作为一种新的抑制剂用于研究由允许GABA或阴离子转运的ALMT蛋白介导的离子通量。
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