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Alcohol and Alcoholism, Vol 34, 161-168, Copyright © 1999 by Medical Council on Alcoholism

ARTICLES

Isolation from beer and structural determination of a potent stimulant of gastrin release

Y Yokoo, H Kohda, A Kusumoto, H Naoki, N Matsumoto, T Amachi, Y Suwa, H Fukazawa, H Ishida, K Tsuji and H Nukaya
Technical Development Department and Health Science Laboratory, Suntory Limited, Shimamoto-Cho, Mishima-Gun, Osaka 618-0001 and 618-8503, Suntory Institute for Bioorganic Research, Shimamoto-Cho, Mishima-Gun, Osaka 618-8503 and School of Pharmaceutical Science, University of Shizuoka, 52-1, Yada, Shizuoka 422-8526, JapanPresent address: Laboratory of Biochemistry, Division of Applied Biosciences, Graduate School of Agriculture, Kyoto University, Kyoto 606-8502, Japan; Corresponding author at: Health Science Laboratory, Suntory Limited, 1-1-1, Wakayamadai, Shimamoto-cho, Mishima-Gun, Osaka 618-8503, Japan

Beer was subjected to five successive chromatographic procedures to isolate the gastrin release-inducing activity, guided by bioassay of the fractions in anaesthetized Donryu rats. The procedures were: (1) hydrophobic interaction chromatography (aqueous effluent with an HP20 column); (2) weak cation-exchanged chromatography (1 M acetic acid eluate with a CM Sephadex C-25 column); (3) gel filtration (methanol eluate with a Sephadex LH-20 column); (4) same as (2); (5) high-performance liquid chromatography (YMC-Pack ODS-AM with 7% acetonitrile-0.01 M HCl). The active component finally isolated had a specific activity 10 000 times higher than that of beer. It was identified by means of mass, 1H- and 13C-nuclear magnetic resonance spectral analyses as N-methyltyramine (NMT). The dose of NMT giving maximal gastrin-releasing activity was 25 g/kg, and the 50% effective dose was 10 g/kg on oral administration to rats. NMT was isolated and identified as a gastrin release inducer in beer. Its concentration in beer is sufficient to account for most of the activity of beer.
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 Drug Metab. Dispos.Home page
T. Kimura, N. Iwasaki, J.-I. Yokoe, S. Haruta, Y. Yokoo, K.-I. Ogawara, and K. Higaki
Analysis and Prediction of Absorption Profile Including Hepatic First-Pass Metabolism of N-Methyltyramine, A Potent Stimulant of Gastrin Release Present in Beer, after Oral Ingestion in Rats by Gastrointestinal-Transit-Absorption Model
Drug Metab. Dispos., May 1, 2000; 28(5): 577 - 581.
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