Characteristics of evodiamine-exerted stimulatory effects on rat jejunal contractility

• Published in: Natural product research Vol. 29; no. 4; pp. 388 - 391
• Main Authors: Xiong, Yong-Jian, Chen, Da-Peng, Peng, Jin-Yong, Wang, Jing-Yu, Lv, Bo-Chao, Liu, Fang-Fei, Lin, Yuan
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 16.02.2015
• Subjects: acetylcholine; Animals; antagonists; atropine; calcium; Calcium - metabolism; Calcium Channel Blockers - pharmacology; cholinergic nervous; Evodia rutaecarpa; evodiamine; Gastrointestinal Motility - drug effects; jejunal contractility; jejunum; Jejunum - drug effects; Molecular Structure; Muscle Contraction - drug effects; myosin; Myosins - metabolism; neurons; Nifedipine - pharmacology; Phosphorylation; Quinazolines - pharmacology; Rats; receptor protein-tyrosine kinase; smooth muscle; stimulatory effects; tetrodotoxin; Tetrodotoxin - pharmacology; Evodia rutaecarpa; cholinergic nervous; evodiamine; stimulatory effects; Ca2; jejunal contractility
• ISSN: 1478-6419; 1478-6427; 1478-6427
• DOI: 10.1080/14786419.2014.947485

This study was designed to characterise the effects of evodiamine on intestinal contractility and reveal the correlated mechanisms. Evodiamine (2.5-80.0 μM) increased normal jejunal contractility and jejunal hypocontractility established under a variety of experimental conditions. Evodiamine-exerted stimulatory effects were blocked by the L-type Ca 2+ channel blocker nifedipine or abolished in the Ca 2+ -free assay condition. The stimulatory effects of evodiamine on jejunal contractility were partially blocked in the presence of neurotoxin tetrodotoxin or endogenous acetylcholine synthesis blocker hemicholinium-3 or muscarinic receptor antagonist atropine, respectively. Evodiamine-exerted stimulatory effects were blocked by c-kit receptor tyrosine kinase inhibitor imatinib. Evodiamine increased myosin phosphorylation in jejunal smooth muscle of constipation-prominent rats. These results showed that evodiamine-exerted stimulatory effects on jejunal segments are Ca 2+ -dependent, need the presence of interstitial cell of Cajal, requirement of cholinergic neuron and correlate with increased myosin phosphorylation, implicating the potential value of evodiamine in relieving hypo-motility disorders.