Inhibition of dipeptidyl peptidase activity by flavonol glycosides of guava (Psidium guajava L.): A key to the beneficial effects of guava in type II diabetes mellitus
Inhibition of dipeptidyl peptidase activity by flavonol glycosides of guava (Psidium guajava L.): A key to the beneficial effects of guava in type II diabetes mellitus
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DOI：
10.1016/j.fitote.2013.05.015
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发表时间：
2013-09-01
期刊：
影响因子：
3.4
通讯作者：
Krennhuber, Klaus
中科院分区：
文献类型：
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作者：
Eidenberger, Thomas;Selg, Manuel;Krennhuber, Klaus
基于民间医学的传统应用，已在体外对番石榴（Psidium guajava L.）叶提取物以及主要黄酮醇苷成分对二肽基肽酶IV（DP - IV，一种血糖稳态的关键酶）的作用进行了研究。从干燥的番石榴叶粉末制备了一种乙醇提取物，发现其中含有七种主要的黄酮醇苷，通过半制备高效液相色谱法对其进行分离并单独测试。结果表明，番石榴叶乙醇提取物对DP - IV具有剂量依赖性抑制作用，测试溶液中的半数抑制浓度（IC50）为380μg/ml。单个黄酮醇苷也对DP - IV有剂量依赖性抑制作用，效果差异可达10倍，总体效果相当于番石榴总提取物效果的100%。在Caco - 2上皮细胞（一种胃肠道吸收模型）中，单个黄酮醇苷在37℃下60分钟内的回收率为可吸收量的2.3 - 5.3%。（c）2013爱思唯尔有限公司。版权所有。
Based on the traditional use in popular medicine, the effect of extracts from Psidium guajava L. leaves and of the main flavonol-glycoside components on dipeptidyl-peptidase IV (DP-IV), a key enzyme of blood glucose homoeostasis, has been investigated in-vitro. An ethanolic extract was prepared from dried, powdered leaves of guava and was found to contain seven main flavonol-glycosides, which were isolated by semipreparative HPLC and tested individually. The ethanolic guava leave extract was shown to exert a dose-dependent inhibition of DP-IV, with an IC50 of 380 mu g/ml test assay solution. Also the individual flavonol-glycosides inhibited DP-IV dose-dependently, with variations of the effects by a factor of 10, and an overall effect accounting for 100% of that observed for the total guava extract. The recovery of individual flavonol-glycosides in CaCo-2 epithelial cells, a model of gastrointestinal tract absorption, amounted to 2.3-5.3% of the amount available for absorption over 60 min at 37 degrees C. (c) 2013 Elsevier B.V. All rights reserved.