首页> 外国专利> INHIBITION OF ALDOSE REDUCTASE BY NATURAL COMPOUNDS (AGNUSIDE, EUPALITIN- 3-O-GALACTOSIDE, PICROSIDE II AND 7-O-METHYLWOGONIN) TO TREAT DIABETIC RETINOPATHY

INHIBITION OF ALDOSE REDUCTASE BY NATURAL COMPOUNDS (AGNUSIDE, EUPALITIN- 3-O-GALACTOSIDE, PICROSIDE II AND 7-O-METHYLWOGONIN) TO TREAT DIABETIC RETINOPATHY

机译:天然化合物(葡糖苷,三联体3-O-半乳糖苷,去甲壳素II和7-O-甲基卵磷脂)抑制醛糖还原酶治疗糖尿病的视网膜病变

摘要

Identification of specific Aldose reductase inhibitors (ARTs) has gained importance in research since most of the tested ARIs were withdrawn due to adverse side effects, mainly due to the nonspecific binding of the ARIs to the Aldoketo reductase (AKR) superfamily proteins, having a high rate of structural similarity to Aldose reductase (ALR2). The phytpcompounds, Agnuside, Picroside II, Eupalitin-3-O-Galactoside and 7-O-Methylwogonin showed potent inhibition of human ALR2 in diabetic lens and ARPE-19 cell line. The Phytocompounds, Agnuside and Eupalitin-3-O-Galactoside inhibited human lens ALR2 with IC50 values lower than the drug Epalrestat (98 nM). Agnuside had the lowest IC50 of 22.4 nM followed by Eupalitin-3-O-Galactoside having an IC50 of 27.3 nM in inhibiting Human ALR2. 7-O-Methylwogonin had an IC50 of 108 nM, and Picroside II had an IC50 of 130 nM in inhibiting ALR2.
机译:特定醛糖还原酶抑制剂(ARTs)的鉴定在研究中已变得越来越重要,因为大多数测试的ARIs由于不良副作用而被撤回,这主要是由于ARIs与醛糖还原酶(AKR)超家族蛋白的非特异性结合,具有很高的与醛糖还原酶(ALR2)的结构相似率。肌醇六磷酸化合物,Agnuside,Picroside II,Eupalitin-3-O-Galactoside和7-O-Methylwogonin在糖尿病晶状体和ARPE-19细胞系中显示出对人ALR2的有效抑制作用。植物化合物,阿糖核苷和Eupalitin-3-O-半乳糖苷抑制人晶状体ALR2,IC50值低于药物Epalrestat(98 nM)。在抑制人ALR2方面,Agnuside的最低IC50为22.4 nM,其次为Eupalitin-3-O-半乳糖苷,IC50为27.3 nM。 7-O-甲基wogonin抑制ALR2的IC50为108 nM,而Picroside II的IC50为130 nM。

著录项

  • 公开/公告号IN2015CH04993A

    专利类型

  • 公开/公告日2017-06-30

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN4993/CHE/2015

  • 发明设计人 ANGELINE JULIUS;

    申请日2015-09-18

  • 分类号C07K16/24;A61K39/395;

  • 国家 IN

  • 入库时间 2022-08-21 13:38:45

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