Natural compound paeonol activates cystic fibrosis transmembrane conductance regulator chloride channel

Abstract

Abstract: AIM: To study the activation of paeonol on CFTR Cl^- channel depending on 3', 5' - cAMP. METHODS: A cell-based fluorescence assay was used to determine CFTR-mediated iodide influx rate. RESULTS: Paeonol increased CFTR-mediate iodide influx in a dose-dependent way. The activation was rapid, reversible and cAMP-dependent. Paeonol had additive effect with FSK IBMX mixture and showed different sensitivity to ΔF508-CFTR and G551DCFTR, implied it worked through a direct binding mechanism. CONCLUSION: The study suggests that CFTR may be a therapeutic drug target of anti-hypertension Chinese Herbs. Paeonol may be useful as a leading compound to develop pharmacological therapy of anti-hypertension drugs.

Key words: paeonol, cystic fibrosis transmembrane conductance regulator, hypertension, chlorine transport, activator

CLC Number:

Q73
R965.2

HOU Ting-ting, GE Hong, SUN Juan-juan, YU Bo, YANG Hong. Natural compound paeonol activates cystic fibrosis transmembrane conductance regulator chloride channel[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2008, 13(11): 1208-1219.

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