Oligomeric procyanidins in apple polyphenol are main active components for inhibition of pancreatic lipase and triglyceride absorption.
Inhibitory effects of apple polyphenol extract (AP) and procyanidin contained in AP on in vitro pancreatic lipase activity and in vivo triglyceride absorption in mice and humans were examined. AP and procyanidin considerably inhibited in vitro pancreatic lipase activity. However, polyphenols, except for procyanidin, in AP (i.e., catechins, chalcones, and phenol carboxylic acids) showed weak inhibitory activities on pancreatic lipase. Procyanidins separated by normal-phase chromatography according to the degree of polymerization were also examined. Inhibitory effects of procyanidins increased according to the degree of polymerization from dimer to pentamer. On the other hand, pentamer or greater procyanidins showed maximal inhibitory effects on pancreatic lipase. These results suggested that with respect to in vitro pancreatic lipase inhibition, the degree of polymerization was an important factor and oligomeric procyanidin mainly contributed. Next, we performed a triglyceride tolerance test in mice and humans. Simultaneous ingestion of AP and triglyceride significantly inhibited an increase of plasma triglyceride levels in both models. These results suggested that the oligomeric procyanidins contained in AP inhibited triglyceride absorption by inhibiting pancreatic lipase activity in mice and humans.
Sugiyama
Hiroshi
H
Fundamental Research Laboratory, Asahi Breweries Limited, I-21, Midori 1-chome, Moriya-shi, Ibaraki 302-0106, Japan. hiroshi.sugiyama@asahibeer.co.jp
Akazome
Yoko
Y
Shoji
Toshihiko
T
Yamaguchi
Atsuko
A
Yasue
Masaaki
M
Kanda
Tomomasa
T
Ohtake
Yasuyuki
Y
D000328:Adult; D000818:Animals; D044946:Biflavonoids / Q000737:chemistry / Q000494:pharmacology*; D002392:Catechin / Q000737:chemistry / Q000494:pharmacology*; D018592:Cross-Over Studies; D004311:Double-Blind Method; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects; D008049:Lipase / Q000037:antagonists & inhibitors*; D008297:Male; D027845:Malus / Q000737:chemistry*; D010636:Phenols / Q000737:chemistry / Q000494:pharmacology; D059808:Polyphenols; D044945:Proanthocyanidins / Q000737:chemistry / Q000494:pharmacology*; D014280:Triglycerides / Q000097:blood* / Q000493:pharmacokinetics
D044946:Biflavonoids; D004791:Enzyme Inhibitors; D005419:Flavonoids; D010636:Phenols; D059808:Polyphenols; D044945:Proanthocyanidins; D014280:Triglycerides; C017674:procyanidin; D002392:Catechin; D008049:Lipase