Natural Compound 20(S)-Protopanaxadiol Activates Cystic Fibrosis Transmembrane Conductance Regulator Chloride Channel

Chem. J. Chinese Universities

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Natural Compound 20(S)-Protopanaxadiol Activates Cystic Fibrosis Transmembrane Conductance Regulator Chloride Channel

LIU Jun^1,2, NA Wan-Li³, XIN Wei-Hong³, LIU Li-Dan⁴, YU Bo¹, MA Tong-Hui¹, YANG Hong¹*

1. Membrane Channel Research Laboratory, Northest Normal University, Changchun 130024, China;
2. The Second Affiliated Hospital, Jilin Uniniversity, Changchun 130041, China;
3. Sino-Japanese Union Hospital, Jilin University, Changchun 130031, China;
4. Nursing College, Jilin Uniniversity, Changchun 130021, China

Received:2007-06-11 Revised:1900-01-01 Online:2008-04-10 Published:2008-04-10
Contact: YANG Hong

Abstract

Abstract: In the present study, we identified a natural compound 20(S)-protopanaxadiol as an effective CFTR chloride channel activator by screening of 386 single compounds from Chinese medicinal herbs by cell-based fluorescent assay. The CFTR-stimulating activity was confirmed by an Ussing chamber short-circuit current assay. The activation is rapid, reversible and cAMP-dependent. The compound does not elevate cellular cAMP level, implying that it worked in a direct binding way. 20(S)-Protopanaxadiol can also restore the impaired chloride conductance of ΔF508 mutant CFTR. In our study a new natural compound was identified that may be useful for probing CFTR channel gating mechanisms and as a leading compound to develop pharmacological therapy of CFTR-related disease such as cystic fibrosis, idiopathic chronic pancreatitis, keratoconjunctivitis sicca and habitual constipation.

Key words: Cystic fibrosis, CFTR chloride channel, Mutation, Natural products, Activator

CLC Number:

O657
Q73

TrendMD:

LIU Jun^1,2, NA Wan-Li³, XIN Wei-Hong³, LIU Li-Dan⁴, YU Bo¹, MA Tong-Hui¹, YANG Hong¹*. Natural Compound 20(S)-Protopanaxadiol Activates Cystic Fibrosis Transmembrane Conductance Regulator Chloride Channel[J]. Chem. J. Chinese Universities, doi: .

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Natural Compound 20(S)-Protopanaxadiol Activates Cystic Fibrosis Transmembrane Conductance Regulator Chloride Channel

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