title: Characteristics of evodiamine-exerted stimulatory effects on rat jejunal contractility.
abstract: 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.
authors.affiliation: a Pharmaceutical College, Dalian Medical University , 9 West Section, Lvshun South Road, Dalian 116044 , P.R. China.
authors.forename: Yong-Jian
authors.initials: YJ
authors.lastname: Xiong
authors.forename: Da-Peng
authors.initials: DP
authors.lastname: Chen
authors.forename: Jin-Yong
authors.initials: JY
authors.lastname: Peng
authors.forename: Jing-Yu
authors.initials: JY
authors.lastname: Wang
authors.forename: Bo-Chao
authors.initials: BC
authors.lastname: Lv
authors.forename: Fang-Fei
authors.initials: FF
authors.lastname: Liu
authors.forename: Yuan
authors.initials: Y
authors.lastname: Lin
mesh_terms: D000818:Animals; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000494:pharmacology; D005769:Gastrointestinal Motility / Q000187:drug effects; D007583:Jejunum / Q000187:drug effects*; D015394:Molecular Structure; D009119:Muscle Contraction / Q000187:drug effects*; D009218:Myosins / Q000378:metabolism; D009543:Nifedipine / Q000494:pharmacology; D010766:Phosphorylation; D011799:Quinazolines / Q000494:pharmacology*; D051381:Rats; D013779:Tetrodotoxin / Q000494:pharmacology
chemical_list: D002121:Calcium Channel Blockers; D011799:Quinazolines; D013779:Tetrodotoxin; C049639:evodiamine; D009218:Myosins; D009543:Nifedipine; D002118:Calcium
keywords: Ca2+; Evodia rutaecarpa; cholinergic nervous; evodiamine; jejunal contractility; stimulatory effects