Flavan-3-ols Having a γ-Lactam from the Roots of Actinidia arguta Inhibit the Formation of Advanced Glycation End Products in Vitro

Flavan-3-ols Having a γ-Lactam from the Roots of Actinidia arguta Inhibit the Formation of Advanced Glycation End Products in Vitro
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DOI:
10.1248/cpb.57.397
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发表时间:
2009-04-01
影响因子:
1.7
通讯作者:
Kim, Jin Sook
Kim, Jin Sook
中科院分区:
医学4区
文献类型:
--
作者:
Jang, Dae Sik;Lee, Ga Young;Kim, Jin Sook

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从杏叶猕猴桃(Actinidia arguta)根的etoac可溶性提取物中分离得到了6-(2-吡咯烷酮-5-基)-(-)-表儿茶素(1)和8-(2-吡咯烷酮-5-基)-(-)-表儿茶素(2)以及5个已知化合物(-)-表儿茶素(3)、(+)-儿茶素(4)、原花青素B-4(5)、(+)-松脂醇和对羟基苯甲酸。化合物1和2的结构是通过光谱数据解释,特别是通过广泛的一维和二维核磁共振研究阐明的。所有分离株在体外对晚期糖基化终产物(AGEs)形成的抑制活性进行了评估。其中化合物1 ~ 5对AGEs的形成具有明显的抑制作用,IC50值在10.1 ~ 125.2 μ m之间。
Two new flavan-3-ols, 6-(2-pyrrolidinone-5-yl)-(-)-epicatechin (1) and 8-(2-pyrrolidinone-5-yl)-(-)-epicatechin (2), as well as five known compounds, (-)-epicatechin (3), (+)-catechin (4), proanthocyanidin B-4 (5), (+)-pinoresinol, and p-hydroxybenzoic acid, were isolated from an EtOAc-soluble extract of the roots of Actinidia arguta. The structures of compounds 1 and 2 were elucidated by spectroscopic data interpretation, particularly by extensive 1D- and 2D-NMR studies. All the isolates were evaluated in vitro for inhibitory activity on the formation of advanced glycation end products (AGEs). Of these, compounds 1-5 exhibited significant inhibitory activity against AGEs formation with IC50 values ranging from 10.1 to 125.2 mu m.