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Original Article

Korean J Physiol Pharmacol 2017; 21(6): 609-616

Published online November 1, 2017 https://doi.org/10.4196/kjpp.2017.21.6.609

Copyright © The Korean Journal of Physiology & Pharmacology.

Ardipusilloside-I stimulates gastrointestinal motility and phosphorylation of smooth muscle myosin by myosin light chain kinase

Zhili Xu1,#, Hanye Liang1,#, Mingbo Zhang1, Xiaojun Tao1, Deqiang Dou1, Liping Hu2,*, and Tingguo Kang1,*

1College of Pharmacy, Liaoning University of Traditional Chinese Medicine, Liaoning 116600, 2College of Information Science & Technology, Liaoning University of Traditional Chinese Medicine, Liaoning 110847, PR China

This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/4.0) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.


Ardipusilloside-I is a natural triterpenoid saponin, which was isolated from Ardisia pusilla A. DC. The aim of the study was to evaluate the stimulation of ardipusilloside-I on gastrointestinal motility in vitro and in vivo. The experiment of smooth muscle contraction directly monitored the contractions of the isolated jejunal segment (IJS) in different contractile states, and the effects of ardipusilloside-I on myosin were measured in the presence of Ca2+-calmodulin using the activities of 20 kDa myosin light chain (MLC20) phosphorylation and myosin Mg2+-ATPase. The effects of ardipusilloside-I on gastro emptying and intestinal transit in constipation-predominant rats were observed, and the MLCK expression in jejuna of constipated rats was determined by western blot. The results showed that, ardipusilloside-I increased the contractility of IJS in a dose-dependent manner and reversed the low contractile state (LCS) of IJS induced by low Ca2+, adrenaline, and atropine respectively. There were synergistic effects on contractivity of IJS between ardipusilloside-I and ACh, high Ca2+, and histamine, respectively. Ardipusilloside-I could stimulate the phosphorylation of MLC20 and Mg2+-ATPase activities of Ca2+-dependent phosphorylated myosin. Ardipusilloside-I also stimulated the gastric emptying and intestinal transit in normal and constipated rats in vivo, respectively, and increased the MLCK expression in the jejuna of constipation-predominant rats. Briefly, the findings demonstrated that ardipusilloside-I could effectively excite gastrointestinal motility in vitro and in vivo.

Keywords: Ardipusilloside-I, Gastrointestinal motility, Myosin light chain kinase, Myosin Mg2+-ATPase