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2″,4″-O-二乙酰槲皮苷,一种从红背酸脚杆中提取的新型晚期糖基化终产物形成抑制剂和醛糖还原酶抑制剂。

2″,4″-O-diacetylquercitrin, a novel advanced glycation end-product formation and aldose reductase inhibitor from Melastoma sanguineum.

作者信息

Lee Ik-Soo, Kim Il Soon, Lee Yun Mi, Lee Youngseop, Kim Joo-Hwan, Kim Jin Sook

机构信息

KM-Based Herbal Drug Research Group, Herbal Medicine Research Division, Korea Institute of Oriental Medicine.

出版信息

Chem Pharm Bull (Tokyo). 2013;61(6):662-5. doi: 10.1248/cpb.c12-00877.

DOI:10.1248/cpb.c12-00877
PMID:23727780
Abstract

A new flavonoid, 2,″4″-O-diacetylquercitrin (1), along with six known flavonoids (2-7) were isolated from the aerial parts of Melastoma sanguineum. The structure of the new flavonoid was established by extensive spectroscopic studies and chemical evidence. The inhibitory effects of isolated compounds (1-7) on advanced glycation end-products (AGEs) formation and rat lens aldose reductase (RLAR) in vitro were examined. Of the tested compounds, compound 1 was the strongest inhibitor of AGEs, with an IC50 of 11.46±0.44 µm. In the RLAR assay, all tested compounds exhibited greater inhibitory effects on RLAR than that of a positive control, 3,3-tetramethyleneglutaric acid (IC50=28.8±1.5 µm); compound 1 exhibited the strongest RLAR-inhibitory activity, with an IC50 of 0.077±0.003 µm.

摘要

从毛稔地上部分分离得到一种新的黄酮类化合物2,″4″-O-二乙酰槲皮苷(1)以及六种已知的黄酮类化合物(2 - 7)。通过广泛的光谱研究和化学证据确定了该新黄酮类化合物的结构。考察了分离得到的化合物(1 - 7)对晚期糖基化终产物(AGEs)形成和大鼠晶状体醛糖还原酶(RLAR)的体外抑制作用。在所测试的化合物中,化合物1是AGEs的最强抑制剂,IC50为11.46±0.44μm。在RLAR测定中,所有测试化合物对RLAR的抑制作用均强于阳性对照3,3 - 四亚甲基戊二酸(IC50 = 28.8±1.5μm);化合物1表现出最强的RLAR抑制活性,IC50为0.077±0.003μm。

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