中国药理学通报2024，Vol.40Issue(4)：695-700,6.DOI:10.12360/CPB202311084
邻苯二甲酸二异丁酯——新型的ANO2通道开放剂
DIBP as a novel ligand for ANO2 channel activating
摘要
Abstract
Aim To screen specific ligand for ANO2 to provide structural information of lead compounds for the development of new drugs targeting ANO2.Meth-ods ANO2 overexpressed HEK293 cell line was con-structed using liposome transfection,and the specific ligand of ANO2 was screened by confocal microscopy and patch-clamp technique.Results Under the record-ing conditions of transmembrane depolarized potential 100 mV and 1 μmol·L-1 calcium pipette solution,ANO2-mediated chloride current Idensity was 14.67± 2.87 pA/pF before DIBP administration and was 28.75±4.05 pA/pF after DIBP administration,which showed significant statistical difference.The results of calcium fluorescence imaging experiment showed that DIBP had no regulated effect on the cytoplasm calcium signaling.When using 0 μmol·L-1 calcium pipette solution,DIBP could not direct activate ANO2 chan-nel.Conclusions DIBP enhances the conductance of the opening ANO2 channel through direct action.As a novel ANO2 channel agonist,DIBP provides structural information for the development of ANO2-targeting drugs and provides strong theoretical basis for the study of the toxicological effects of other phthalates.关键词
邻苯二甲酸二异丁酯/ANO2/配体/过表达/先导化合物/电流密度/白介素-8Key words
DIBP/ANO2/ligand/overexpression/lead compound/Idensity/IL-8分类
医药卫生引用本文复制引用
郑晓恬,白立川,王惠杰,吴琼..邻苯二甲酸二异丁酯——新型的ANO2通道开放剂[J].中国药理学通报,2024,40(4):695-700,6.基金项目
国家自然科学基金项目(No 820028215) （No 820028215）
辽宁省自然基金指导计划项目(No 20180551125) （No 20180551125）
