Attenuation of stress-induced gastrointestinal motility disorder by gentiopicroside, from Gentiana macrophylla Pall.
OBJECTIVE
The current study was designed to explore the mechanism of the prokinetic activity of Gentiopicroside (Ge), from Gentiana macrophylla Pall which is widely used to strengthen gastric motility in clinic.


METHODS
Gastrointestinal motility disorder rats were induced by stress stimulation and the rats were treated with Ge. The functions of gastric emptying and intestinal propelling were measured after blood was obtained to assay the levels of plasmatic motilin (MTL), vasoactive intestinal peptide (VIP), somatostatin (SST), gastrin (GAS), neurotensin (NT) and substance of P (SP). The expressions of MTL receptor (MTLR), VIP receptor 2 (VIPR2) and SST receptor 2 (SSTR2) were measured also. In addition, an isolated guinea pig ileum was applied to evaluate the influences of Ge on M-R, H1-R, 5-HT4-R and D-R in vitro.


RESULTS
Ge increased gastric emptying and intestinal propelling obviously. It also decreased the level of SST and increased GAS in plasma significantly. Moreover, it promoted the expressions of MTLR in gastric antrum, duodenum, jejunum and ileum, and restrained the expression of VIPR2 in duodenum. Piboserod and loratadine had no obvious restrain to Ge' exciting ileum effect and Ge also didn't affect dopamine paralyzing ileum. However, Ge failed to improve the hypofunction of guinea pigs ileums pre-treated with atropine sulfate.


CONCLUSIONS
The mechanisms of Ge' prokinetic effect were associated with modulating the levels of SST and GAS in plasma, raising the expressions of MTLR in gastric antrum, duodenum, ileum and jejunum, reducing the expression of VIPR2 in duodenum and activating M-R.
Jiangsu Key Laboratory for Pharmacology and Safety Evaluation of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, PR China; School of Food Science, Nanjing Xiaozhuang University, Nanjing 211171, PR China.
Ming
M
Ruan
Jiangsu Key Laboratory for Pharmacology and Safety Evaluation of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, PR China. Electronic address: nzyyubin@163.com.
Bin
B
Yu
Jiangsu Key Laboratory for Pharmacology and Safety Evaluation of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, PR China.
Li
L
Xu
Jiangsu Key Laboratory for Pharmacology and Safety Evaluation of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, PR China.
Liang
L
Zhang
Jiangsu Key Laboratory for Pharmacology and Safety Evaluation of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, PR China.
Jun
J
Long
Guiyang Medical University, Guiyang 550004, PR China. Electronic address: shenxiangchun@126.com.
Xiangchun
X
Shen
D000818:Animals; D005260:Female; D005755:Gastrins / Q000097:blood; D005767:Gastrointestinal Diseases / Q000188:drug therapy; D005769:Gastrointestinal Motility / Q000187:drug effects*; D030012:Gentiana / Q000737:chemistry*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D057888:Iridoid Glucosides / Q000494:pharmacology*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D051239:Receptors, Vasoactive Intestinal Peptide, Type II / Q000378:metabolism; D013004:Somatostatin / Q000097:blood
D005755:Gastrins; D057888:Iridoid Glucosides; D051239:Receptors, Vasoactive Intestinal Peptide, Type II; C495511:Vipr2 protein, rat; C012997:gentiopicroside; D013004:Somatostatin
Gastrointestinal hormones; Gastrointestinal prokinetic effect; Gentiopicroside; Gentiopicroside (PubChem CID: 88708); Muscarinic acetylcholine receptor agonist