Natural Compound Curcumin-a Channel Potentiator Rather Than a Corrector of the Defective Intracellul

• 作 者: LIU Xin GUAN Li HE Cheng-yan Z
• 机 构: Membrane Channel Research Laboratory,China-Japan Union Hospital,Liaoning Provincial Key Laboratory o
• 出 处: 高等学校化学研究（英文版）
• 发表日期: 2004年期
• 关键词: Cystic fibrosis CFTR Mutation Natural compound Drug discovery

Cystic fibrosis(CF)is a severe genetic disease caused by the gene mutation of the cystic fibrosis transmembrane conductance regulator(CFTR)chloride channel.The most common point mutation △F508,which leads to impaired intracellular processing and channel gating of CFTR, appears in about 90%CF patients.The natural compound curcumin was reported to correct the processing defect of △F508-CFTR and proposed as a potential therapeutic drug to cure CF.In the present study.we analyzed the efrect of curcumin on △F508-CFTR and demonstrated that curcumin can restore the impaired chloride conductance of △F508 mutant CFTR.The activity is rapid,reversible and cAMP-dependent.However,we couldn't reproduce the previously reported correction of the defective membrane trafficking of △F508-CFTR by curcumin.Therefore,curcumin may not be a superior lead compound for developing anti-CF drugs.