Prenylated Flavonoids from Epimedium koreanum Nakai and their Human Neutrophil Elastase Inhibitory Effects

被引：6
作者：
Lee, Soo Min [1 ]
Song, Yeong Hun [1 ]
Uddin, Zia [1 ]
Ban, Yeong Jun [1 ]
Park, Ki Hun [1 ]
机构：
[1] Gyeongsang Natl Univ, Grad Sch, IALS, Div Appl Life Sci,Plus BK21, Jinju 660701, South Korea
来源：
RECORDS OF NATURAL PRODUCTS | 2017年 / 11卷 / 06期
关键词：
Epimedium Koreanum Nakai; Epimedokoreanin B; Human neutrophil elastase; Prenylated flavonoids;
D O I：
10.25135/rnp.66.17.05.090
中图分类号：
Q94 [植物学];
学科分类号：
071001 ;
摘要：
Human neutrophil elastase (HNE) has been linked to immune system functions, including inflammation, as well as the development of skin wrinkles, suggesting that HNE inhibitors have many practical applications. In this study, the methanol extract of Epimedium koreanum Nakai contained potent HNE inhibitory flavonoids (1–4) with IC50 values of 6.06–125.80 μM. Prenyl groups within these flavonoids were critical for the inhibitory effects. For example, epimedokoreanin B (1) (IC50= 6.06 μM) showed 6-fold higher efficacy than that of its parent luteolin (IC50 = 36.01 μM). A similar trend was observed for compound 2 (IC50= 6.28 μM) and its parent, apigenin (IC50= 37.94 μM). Lineweaver–Burk plots showed that the compounds exhibit mixed-type inhibition. In a detailed kinetic study, compound 1 was assigned to mixed type I and exhibited the greatest binding to the free enzyme (KI= 11.7 μM, KIS= 40.9 μM). © 2017 ACG Publications. All rights reserved.
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收藏
页码：514 / 520
页数：16
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