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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.

DOI:10.1016/j.phymed.2014.09.007
PMID:25636873
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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1
In vitro anti-hyperglycemic activity of 4-hydroxyisoleucine derivatives.4-羟基异亮氨酸衍生物的体外抗高血糖活性。
Phytomedicine. 2015 Jan 15;22(1):66-70. doi: 10.1016/j.phymed.2014.09.007. Epub 2014 Dec 9.
2
Non-insulin dependent anti-diabetic activity of (2S, 3R, 4S) 4-hydroxyisoleucine of fenugreek (Trigonella foenum graecum) in streptozotocin-induced type I diabetic rats.(2S,3R,4S)4-羟基异亮氨酸的非胰岛素依赖型抗糖尿病活性 ,来源于葫芦巴(Trigonella foenum graecum),在链脲佐菌素诱导的 I 型糖尿病大鼠中。
Phytomedicine. 2012 May 15;19(7):571-4. doi: 10.1016/j.phymed.2012.01.004. Epub 2012 Mar 6.
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Antihyperglycaemic effect of an unusual amino acid (4-hydroxyisoleucine) in C57BL/KsJ-db/db mice.在 C57BL/KsJ-db/db 小鼠中一种不寻常的氨基酸(4-羟基异亮氨酸)的降血糖作用。
Nat Prod Res. 2010 Feb;24(3):258-65. doi: 10.1080/14786410902836693.
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The effect of fenugreek 4-hydroxyisoleucine on liver function biomarkers and glucose in diabetic and fructose-fed rats.胡芦巴4-羟基异亮氨酸对糖尿病和喂食果糖大鼠肝功能生物标志物及血糖的影响。
Phytother Res. 2009 Jan;23(1):61-4. doi: 10.1002/ptr.2557.
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4-Hydroxyisoleucine stimulates glucose uptake by increasing surface GLUT4 level in skeletal muscle cells via phosphatidylinositol-3-kinase-dependent pathway.4-羟基异亮氨酸通过增加骨骼肌细胞表面 GLUT4 水平,经由磷脂酰肌醇-3-激酶依赖途径刺激葡萄糖摄取。
Eur J Nutr. 2012 Oct;51(7):893-8. doi: 10.1007/s00394-012-0374-9. Epub 2012 May 19.
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4-Hydroxyisoleucine ameliorates fatty acid-induced insulin resistance and inflammatory response in skeletal muscle cells.4-羟基异亮氨酸改善脂肪酸诱导的骨骼肌细胞胰岛素抵抗和炎症反应。
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Trigonella foenum-graecum Seed Extract, 4-Hydroxyisoleucine, and Metformin Stimulate Proximal Insulin Signaling and Increase Expression of Glycogenic Enzymes and GLUT2 in HepG2 Cells.胡芦巴籽提取物、4-羟基异亮氨酸和二甲双胍刺激HepG2细胞中的近端胰岛素信号传导并增加糖原生成酶和GLUT2的表达。
Metab Syndr Relat Disord. 2016 Mar;14(2):114-20. doi: 10.1089/met.2015.0081. Epub 2016 Feb 2.
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4-Hydroxyisoleucine from Fenugreek (Trigonella foenum-graecum): Effects on Insulin Resistance Associated with Obesity.胡芦巴中提取的4-羟基异亮氨酸:对与肥胖相关的胰岛素抵抗的影响。
Molecules. 2016 Nov 22;21(11):1596. doi: 10.3390/molecules21111596.
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4-hydroxyisoleucine an unusual amino acid as antidyslipidemic and antihyperglycemic agent.4-羟基异亮氨酸,一种不同寻常的氨基酸,作为抗血脂异常和抗高血糖药物。
Bioorg Med Chem Lett. 2006 Jan 15;16(2):293-6. doi: 10.1016/j.bmcl.2005.10.003. Epub 2005 Oct 21.
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The addition of fenugreek extract (Trigonella foenum-graecum) to glucose feeding increases muscle glycogen resynthesis after exercise.在葡萄糖喂养中添加胡芦巴提取物(葫芦巴)可增加运动后肌肉糖原的再合成。
Amino Acids. 2005 Feb;28(1):71-6. doi: 10.1007/s00726-004-0143-z. Epub 2004 Dec 2.

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