Elucidation of the effect of polyphenols on the inhibition of intestinal cholesterol transport and for their clinical applications

2014 Fiscal Year Final Research Report

• Project/Area Number: 24500969
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Eating habits, studies on eating habits
• Research Institution: The University of Tokyo
• Principal Investigator: KOBAYASHI Shoko 東京大学, 農学生命科学研究科, 准教授 (90348144)
• Co-Investigator(Kenkyū-buntansha): ISHIMARU Yoshiro 東京大学, 大学院農学生命科学研究科, 特任准教授 (10451840)
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: コレステロールトランスポーター / ルテオリン / ケルセチン

Outline of Final Research Achievements

Niemann-pick C1-Like 1 (NPC1L1) mediates cholesterol absorption, and ezetimibe is a potent NPC1L1 inhibitor applicable for medication of hypercholesterolemia. Epidemiological studies demonstrated that consumption of polyphenols correlates with a decreased risk for atherosclerosis, and we hypothesized that polyphenols inhibit intestinal transport of cholesterol. We elucidated the kinetic parameters of intestinal cholesterol absorption using Caco-2 cells and screened 34 polyphenols. Luteolin and quercetin inhibited cholesterol absorption by Caco-2 cells and human embryonic kidney 293T cells expressing NPC1L1. Serum cholesterol levels significantly decreased more in rats fed both cholesterol and luteolin (or quercetin), than in those observed in the cholesterol feeding group. These results suggest that luteolin and quercetin reduce high blood cholesterol levels by specifically inhibiting intestinal cholesterol absorption mediated by NPC1L1.

Free Research Field

食生活学