Inhibitory Effects of Oolong Tea Polyphenols on Pancreatic Lipase in Vitro

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  • Masaaki Nakai
    Institute for Health Care Science and Suntory Institute for Bioorganic Research, Suntory, Ltd., 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan, Faculty of Bioresources, Gifu University, 1-1 Yanagido, Gifu-shi, Gifu 501-11, Japan, and Faculty of Agriculture, Kagoshima University, Korimoto 1-21-24, Kagoshima 890, Japan
  • Yuko Fukui
    Institute for Health Care Science and Suntory Institute for Bioorganic Research, Suntory, Ltd., 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan, Faculty of Bioresources, Gifu University, 1-1 Yanagido, Gifu-shi, Gifu 501-11, Japan, and Faculty of Agriculture, Kagoshima University, Korimoto 1-21-24, Kagoshima 890, Japan
  • Sumio Asami
    Institute for Health Care Science and Suntory Institute for Bioorganic Research, Suntory, Ltd., 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan, Faculty of Bioresources, Gifu University, 1-1 Yanagido, Gifu-shi, Gifu 501-11, Japan, and Faculty of Agriculture, Kagoshima University, Korimoto 1-21-24, Kagoshima 890, Japan
  • Yoshiko Toyoda-Ono
    Institute for Health Care Science and Suntory Institute for Bioorganic Research, Suntory, Ltd., 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan, Faculty of Bioresources, Gifu University, 1-1 Yanagido, Gifu-shi, Gifu 501-11, Japan, and Faculty of Agriculture, Kagoshima University, Korimoto 1-21-24, Kagoshima 890, Japan
  • Takashi Iwashita
    Institute for Health Care Science and Suntory Institute for Bioorganic Research, Suntory, Ltd., 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan, Faculty of Bioresources, Gifu University, 1-1 Yanagido, Gifu-shi, Gifu 501-11, Japan, and Faculty of Agriculture, Kagoshima University, Korimoto 1-21-24, Kagoshima 890, Japan
  • Hiroshi Shibata
    Institute for Health Care Science and Suntory Institute for Bioorganic Research, Suntory, Ltd., 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan, Faculty of Bioresources, Gifu University, 1-1 Yanagido, Gifu-shi, Gifu 501-11, Japan, and Faculty of Agriculture, Kagoshima University, Korimoto 1-21-24, Kagoshima 890, Japan
  • Tohru Mitsunaga
    Institute for Health Care Science and Suntory Institute for Bioorganic Research, Suntory, Ltd., 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan, Faculty of Bioresources, Gifu University, 1-1 Yanagido, Gifu-shi, Gifu 501-11, Japan, and Faculty of Agriculture, Kagoshima University, Korimoto 1-21-24, Kagoshima 890, Japan
  • Fumio Hashimoto
    Institute for Health Care Science and Suntory Institute for Bioorganic Research, Suntory, Ltd., 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan, Faculty of Bioresources, Gifu University, 1-1 Yanagido, Gifu-shi, Gifu 501-11, Japan, and Faculty of Agriculture, Kagoshima University, Korimoto 1-21-24, Kagoshima 890, Japan
  • Yoshinobu Kiso
    Institute for Health Care Science and Suntory Institute for Bioorganic Research, Suntory, Ltd., 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan, Faculty of Bioresources, Gifu University, 1-1 Yanagido, Gifu-shi, Gifu 501-11, Japan, and Faculty of Agriculture, Kagoshima University, Korimoto 1-21-24, Kagoshima 890, Japan

説明

Fifty-four polyphenols isolated from tea leaves were evaluated for their inhibitory activities against pancreatic lipase, the key enzyme of lipid absorption in the gut. (-)-Epigallocatechin 3-O-gallate (EGCG), which is one of major polyphenols in green tea, showed lipase inhibition with an IC50 of 0.349 microM. Moreover, flavan-3-ol digallate esters, such as (-)-epigallocatechin-3,5-digallate, showed higher activities of inhibition on lipase with an IC50 of 0.098 microM. On the other hand, nonesterified flavan-3-ols, such as (+)-catechin, (-)-epicatechin, (+)-gallocatechin, and (-)-epigallocatechin, showed zero and/or the lowest activities against pancreatic lipase (IC5020 microM). These data suggested that the presence of galloyl moieties within the structure was required for enhancement of pancreatic lipase inhibition. It is well-known that flavan-3-ols are polymerized by polyphenol oxidase and/or heating in a manufacturing process of oolong tea. Oolonghomobisflavans A and B and oolongtheanin 3'-O-gallate, which are typical in oolong tea leaves, showed strong inhibitory activities with IC50 values of 0.048, 0.108, and 0.068 microM, respectively, even higher than that of EGCG. The oolong tea polymerized polyphenols (OTPP) were prepared for the assay from oolong tea extract, from which the preparation effectively subtracted the zero and/or less-active monomeric flavan-3-ols by preparative high-performance liquid chromatography. The weight-average molecular weight (Mw) and number-average molecular-weight (Mn) values of OTPP were 2017 and 903, respectively, by using gel permeation choromatography. OTPP showed a 5-fold stronger inhibition against pancreatic lipase (IC50 = 0.28 microg/mL) by comparison with that of the tannase-treated OTPP (IC50 = 1.38 microg/mL). These data suggested that the presence of galloyl moieties within their chemical structures and/or the polymerization of flavan-3-ols were required for enhancement of pancreatic lipase inhibition.

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