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4-羟基异亮氨酸衍生物的体外抗高血糖活性。

In vitro anti-hyperglycemic activity of 4-hydroxyisoleucine derivatives.

作者信息

Korthikunta Venkateswarlu, Pandey Jyotsana, Singh Rohit, Srivastava Rohit, Srivastava Arvind K, Tamrakar Akhilesh K, Tadigoppula Narender

机构信息

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, UP 226 031, India.

Biochemistry Division, CSIR-Central Drug Research Institute, Lucknow, UP 226 031, India.

出版信息

Phytomedicine. 2015 Jan 15;22(1):66-70. doi: 10.1016/j.phymed.2014.09.007. Epub 2014 Dec 9.

Abstract

The nonproteinogenic amino acid, 4-hydroxyisoleucine (1) has been isolated in large quantities from the fenugreek (T. foenum-graecum) seeds. Few novel derivatives (3-11 and 13-18) were prepared from the naturally occurring 4-hydroxyisoleucine (1) and screened for their in vitro glucose uptake stimulatory effect in L-6 skeletal muscle cells. The derivatives 6, 7, 8, 10 and 11 exhibited better glucose uptake stimulatory activity than parent compound, 4-hydroxyisoleucine at 5 and 10µM concentrations and compounds 7 and 11 enhanced translocation of insulin sensitive glucose transporters-4 in skeletal muscle cells.

摘要

非蛋白质氨基酸4-羟基异亮氨酸(1)已从胡芦巴(T. foenum - graecum)种子中大量分离出来。从天然存在的4-羟基异亮氨酸(1)制备了几种新型衍生物(3 - 11和13 - 18),并在L - 6骨骼肌细胞中筛选它们的体外葡萄糖摄取刺激作用。在5和10µM浓度下,衍生物6、7、8、10和11表现出比母体化合物4-羟基异亮氨酸更好的葡萄糖摄取刺激活性,并且化合物7和11增强了骨骼肌细胞中胰岛素敏感性葡萄糖转运蛋白-4的易位。

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