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Isolation of Stimulants of Gastrointestinal Motility in Beer
Author(s) -
Yokoo Yoshiaki,
Fujii Wataru,
Hori Hisako,
Nagao Koji,
Suwa Yoshihide,
Taniyama Kohtaro,
Tsuji Kuniro,
Yoshida Toshiyuki,
Nukaya Haruo
Publication year - 2004
Publication title -
alcoholism: clinical and experimental research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.267
H-Index - 153
eISSN - 1530-0277
pISSN - 0145-6008
DOI - 10.1111/j.1530-0277.2004.tb03230.x
Subject(s) - muscarinic acetylcholine receptor , motility , congener , gastric emptying , chemistry , biological activity , receptor , pharmacology , ileum , muscarinic acetylcholine receptor m3 , endocrinology , biochemistry , chromatography , in vitro , stomach , biology , genetics
Background: Among various alcoholic beverages, it has reported that beer has a potent activity to stimulate gastric emptying. Our previous studies showed that beer congener stimulated gastrointestinal motility by directly stimulating muscarinic M 3 receptor, present in smooth muscles of the gastrointestinal tract. However, active components that account for the action have yet to be identified. We attempted to isolate the stimulant(s) of gastrointestinal motility in beer. Methods: Beer congener was prepared from beer and used to separate and purify active components by a series of liquid chromatography using affinity to muscarinic M 3 receptor as an index. Gastrointestinal motility‐stimulating activity was evaluated using a test for activity that causes contraction of longitudinal muscles in guinea pig ileum and a test for gastric emptying activity in mice. Results: The active components (compounds A and B) were purified and isolated from beer by four liquid chromatography steps. The IC 50 values of two active isolates to muscarinic M 3 receptor were 0.65 × 10 −6 g/ml and 2.30 × 10 −6 g/ml, respectively. The concentrations of compounds A and B contained in beer were sufficient to explain most of the muscarinic M 3 receptor binding activity of beer. The active fraction that contained both compounds A and B (which was 10 times as active as beer congener in muscarinic M 3 receptor binding activity) dose‐dependently contracted the longitudinal muscles of guinea pig ileum with an activity that was 20 times as potent as that of beer congener. The same active fraction significantly stimulated gastric emptying in mice with an activity 20 times as potent as that of beer congener. Conclusions: Two active components (compounds A and B) were isolated as gastrointestinal motility stimulants (muscarinic M 3 agonists) in beer. These results suggest that the two isolated active components are the active entities of the gastrointestinal motility‐stimulating effect of beer.