Synthesis and biological activity of trans-tiliroside derivatives as potent anti-diabetic agents.

Synthesis and biological activity of trans-tiliroside derivatives as potent anti-diabetic agents.
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强效抗糖尿病药物反式替利罗苷衍生物的合成及生物活性

DOI:
10.3390/molecules15129174
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发表时间:
2010-12-10
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Duan H
Duan H
中科院分区:
其他
文献类型:
--
作者:
Zhu Y;Zhang Y;Liu Y;Chu H;Duan H

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合成了一系列新的反式替罗苷衍生物。通过红外光谱、核磁共振氢谱和质谱分析确定了化合物的结构。在胰岛素抵抗(IR)HepG 2细胞模型上评价它们的抗糖尿病活性。结果,与阳性对照(二甲双胍)相比,化合物7a、7 c、7 h和反式-替皮苷在IR-HepG 2细胞中表现出显著的葡萄糖消耗增强作用。本研究为进一步设计和发现抗糖尿病药物提供了有益的线索。
A set of novel trans-tiliroside derivatives were synthesized. The structures of the derivatives were identified by their IR, 1H-NMR, and MS spectra analysis. Their anti-diabetic activities were evaluated on the insulin resistant (IR) HepG2 cell model. As a result, compounds 7a, 7c, 7h, and trans-tiliroside exhibited significant glucose consumption-enhancing effects in IR-HepG2 cells compared with the positive control (metformin). This research provides useful clues for further design and discovery of anti-diabetic agents.
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