Dictamine Stimulates Cystic Fibrosis Transmembrane Conductance Regulator Cl-Transport  

作　　者：LIU Jun LIU Li-dan WANG Su-mei XU Li-na YU Bo LIN Sen 

机构地区：[1]Biopharmaceutical Center, Liaoning Normal University, Dalian 116029, P. R. China [2]The Second Clinical Medical School, Jilin University, Changchun 130021, P. R. China

出　　处：《Chemical Research in Chinese Universities》2007年第5期554-557,共4页高等学校化学研究（英文版）

基　　金：Supported by the National Natural Science Foundation of China(Nos.30470405and30570864).

摘　　要：Dictamine is a furoquinoline alkaloid isolated from Dictamus dasycarpus Turcz.In the present study,we found that dictamine is able to stimulate the chloride transport activity of wild-type and ΔF508 mutant CFTR.The activity is cAMP-dependent and can be completely reversed by specific CFTR inhibitor CFTRinh-172.In addition,dictamine can further increase the chloride transport activity when CFTR is maximally activated by the combination of cAMP stimulators forskolin（FSK）and IBMX,suggesting direct interaction of dictamine with CFTR.Dictamine may be useful for probing CFTR channel gating mechanisms and used as a lead compound to develop the pharmacological therapy of CFTR-related diseases such as idiopathic chronic pancreatitis and keratoconjunctivitis sicca and cystic fibrosis.Dictamine is a furoquinoline alkaloid isolated from Dictamus dasycarpus Turcz.In the present study,we found that dictamine is able to stimulate the chloride transport activity of wild-type and ΔF508 mutant CFTR.The activity is cAMP-dependent and can be completely reversed by specific CFTR inhibitor CFTRinh-172.In addition,dictamine can further increase the chloride transport activity when CFTR is maximally activated by the combination of cAMP stimulators forskolin（FSK）and IBMX,suggesting direct interaction of dictamine with CFTR.Dictamine may be useful for probing CFTR channel gating mechanisms and used as a lead compound to develop the pharmacological therapy of CFTR-related diseases such as idiopathic chronic pancreatitis and keratoconjunctivitis sicca and cystic fibrosis.

关 键 词：Cystic fibrosis CFI＇R Dictamine ACTIVATOR 

分 类 号：R58[医药卫生—内分泌]