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标题：Enzymatically Modified Isoquercitrin, α-Oligoglucosyl Quercetin 3-O-Glucoside, Is Absorbed More Easily than Other Quercetin Glycosides or Aglycone after Oral Administration in Rats
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作者：Toshiaki Makino ; Ryosuke Shimizu ; Misaki Kanemaru 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2009
卷号：32
期号：12
页码：2034-2040
DOI：10.1248/bpb.32.2034
出版社：The Pharmaceutical Society of Japan
摘要：Quercetin, a flavonol contained in various vegetables and herbal medicines, has various biological activities including anti-cancer, anti-allergic and anti-oxidative activities. However, low oral bioavailability of quercetin due to insolubility in water has limited its use as a food additive or dietary supplement. Since the water solubility is enhanced by glycosyl conjugation, in the present study, we evaluated the bioavailability of several quercetin glycosides with different sugar moieties in rats. Quercetin, quercetin-3- O -rutinoside (rutin), and quercetin-3- O -glucoside (isoquercitrin, IQC) in suspension, and quercetin-3- O -maltoside (Q3M), quercetin-3- O -gentiobioside (Q3G), α-monoglucosyl rutin (αMR), α-oligoglucosyl rutin (αOR), and enzymatically modified isoquercitrin (α-oligoglucosyl isoquercitrin, EMIQ) dissolved in water, were orally administered to rats under anesthesia. Bioavailability ( F value) was calculated from the concentrations of total quercetin in plasma from 0 to 12 h after the administration. F value of quercetin was 2.0%, and those of IQC, Q3M and EMIQ were 12%, 30%, and 35%, respectively. Although Q3G, αMR and αOR have high water solubility, their F values were low (3.0%, 4.1%, 1.8%, respectively). In the in vitro study, the homogenate of rat intestinal epithelium rapidly hydrolyzed IQC, Q3M and EMIQ to quercetin, and αMR and αOR to rutin. However, it could not hydrolyze Q3G or rutin to quercetin. Elongation of α-linkage of glucose moiety in IQC enhances the bioavailability of quercetin, and intestinal epithelial enzymes such as lactase-phrolizin hydrolase or mucosal maltase-glucoamylase would play important roles in the hydrolysis and absorption of these flavonol glycosides.
关键词：enzymatically modified isoquercitrin;quercetin;rutin;bioavailability;lactase-phlorizin hydrolase