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http://dx.doi.org/10.4062/biomolther.2010.18.4.442

The Inhibitory Effect of Eupatilin on the Intestinal Contraction Induced by Carbachol  

Je, Hyun-Dong (Department of Pharmacology, College of Pharmacy, Catholic University of Daegu)
Lee, Jong-Min (Department of Pharmacology, College of Pharmacy, Catholic University of Daegu)
La, Hyen-Oh (Department of Pharmacology, College of Medicine, The Catholic University of Korea)
Publication Information
Biomolecules & Therapeutics / v.18, no.4, 2010 , pp. 442-447 More about this Journal
Abstract
This study was conducted to determine whether treatment with the anti-inflammatory eupatilin influences intestinal smooth muscle contraction stimulated by carbachol and, if so, to investigate the related mechanism. Denuded ileal or colonic muscles from Sprague-Dawley rats were used for the study and measurements of isometric contractions were obtained using a computerized data acquisition system; this data was also combined with results from molecular experiments. Eupatilin from Artemisia asiatica Nakai significantly decreased carbachol-induced contractions in both ileal and colonic muscles. Interestingly, eupatilin decreased carbachol-induced phosphorylation of ERK1/2 more significantly than that of MYPT1 at Thr855 in ileal and colonic muscles. However, eupatilin significantly decreased phosphorylation of MYPT1 at Thr855, but only in ileal muscle. Therefore, thin filament regulation, including MEK inactivation and related phospho-ERK1/2 decrease, is mainly involved in the eupatilin-induced decrease of intestinal contraction induced by carbachol. In conclusion, this study provides the evidence and a possible related mechanism concerning the inhibitory effect of the flavonoid as an antispasmodic on the agonist-induced contractions in rat ileum and colonic muscles.
Keywords
Colon; ERK; Eupatilin; Ileum; MYPT1; Smooth muscle;
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