Fractionation of a herbal antidiarrheal medicine reveals Eugenol as an inhibitor of Ca2+-activated Cl- channel TMEM16A

Zhen Yao, Wan Namkung, Eun A. Ko, Jinhong Park, Lukmanee Tradtrantip, A. S. Verkman

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Abstract

The Ca2+-activated Cl- channel TMEM16A is involved in epithelial fluid secretion, smooth muscle contraction and neurosensory signaling. We identified a Thai herbal antidiarrheal formulation that inhibited TMEM16A Cl- conductance. C18-reversed-phase HPLC fractionation of the herbal formulation revealed >98% of TMEM16A inhibition activity in one out of approximately 20 distinct peaks. The purified, active compound was identified as eugenol (4-allyl-2-methoxyphenol), the major component of clove oil. Eugenol fully inhibited TMEM16A Cl- conductance with single-site IC50~150 μM. Eugenol inhibition of TMEM16A in interstitial cells of Cajal produced strong inhibition of intestinal contraction in mouse ileal segments. TMEM16A Cl- channel inhibition adds to the list of eugenol molecular targets and may account for some of its biological activities.

Original languageEnglish
Article numbere38030
JournalPloS one
Volume7
Issue number5
DOIs
Publication statusPublished - 2012 May 30

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All Science Journal Classification (ASJC) codes

  • Biochemistry, Genetics and Molecular Biology(all)
  • Agricultural and Biological Sciences(all)
  • General

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