Activation of CFTR-mediated Cl- Transport by Magnolin |
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Authors: | JIN Ling-ling LIU Xin SUN Yan LIN Sen ZHOU Na XU Li-na YU BO HOU Shu-guang YANG Hong |
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Institution: | [1]Liaoning Province Key Laboratory of Biotechnology and Drug Discovery, Liaoning Normal University,Dalian 116029, P. R. China [2]China-Japan Union Hospital, Jilin University, Changchun 130033,P R. China [3]Qianwei Affiliate Hospital, Jilin University, Changchun 130021, P. R. China |
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Abstract: | Magnolin is a herbal compound from Magnolia biondii Pamp.It possesses numerous biological activities.Cystic fibrosis transmembrane conductance regulator(CFTR)is all epithelial chloride channel that plays a key role in the fluid secretion of various exocrine organs.In the present study,the activation of CFTR-mediated chloride transport by magnolin is indentified and characterized.In CFTR stably trailsfected FRT cells.magnolin increases CFTR Cl- currents in a concentration-dependent manner.The activation of magnolin on CFTR is rapid,reversible,and cAMP-dependent.Magnolin does not elevate cellular cAMP level.indicating that it activates CFTR by direct binding and interaction with CFTR protein.Magnolin selectively activates wildtype CFTR rather than mutant CFTIL Magnolin may present a novel class of therapeutic lead compound for the treatment of diseases associated with reduced CFTR function such as keratoconjunctivitis sicca,idiopathic chronic pancreatiti,and chromc constipation. |
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Keywords: | Cystic fibrosis CFTR Mutation Magnolin Activator |
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