Kushenol A and 8-prenylkaempferol, tyrosinase inhibitors, derived from Sophora flavescens

被引：37

作者：

Kim, Jang Hoon ^{[1
]}

Cho, In Sook ^{[2
]}

So, Yang Kang ^{[1
]}

Kim, Hyeong-Hwan ^{[2
]}

Kim, Young Ho ^{[3
]}

机构：

[1] Korea Atom Energy Res Inst, Adv Radiat Technol Inst, Jeongeup, South Korea

[2] RDA, Natl Inst Hort & Herbal Sci, Dept Hort & Crop Environm, Wonju 55365, South Korea

[3] Chungnam Natl Univ, Coll Pharm, Daejeon 34134, South Korea

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2018年 / 33卷 / 01期

基金：

新加坡国家研究基金会;

关键词：

Sophora flavescens; Fabaceae; tyrosinase inhibitor; molecular docking; antioxidant; OXIDATIVE STRESS; FLAVONOIDS; ROOTS; CELLS; AIT; ACID;

D O I：

10.1080/14756366.2018.1477776

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Tyrosinase is known for an enzyme that plays a key role in producing the initial precursor of melanin biosynthesis. Inhibition of the catalytic reaction of this enzyme led to some advantage such as skin-whitening and anti-insect agents. To find a natural compound with inhibitory activity towards tyrosinase, the five flavonoids of kushenol A (1), 8-prenylkaempferol (2), kushenol C (3), formononetin (4) and 8-prenylnaringenin (5) were isolated by column chromatography from a 95% methanol extract of Sophora flavescens. The ability of these flavonoids to block the conversion of L-tyrosine to L-DOPA by tyrosinase was tested in vitro. Compounds 1 and 2 exhibited potent inhibitory activity, with IC50 values less than 10 mu M. Furthermore, enzyme kinetics and molecular docking analysis revealed the formation of a binary encounter complex between compounds 1-4 and the enzyme. Also, all of the isolated compounds (1-5) were confirmed to possess antioxidant activity.

引用

页码：1048 / 1054

页数：7

共 22 条

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