The inhibitory effect of Prunella vulgaris L. on aldose reductase and protein glycation.

Journal of Biomedicine and Biotechnology Pub Date : 2012-01-01 Epub Date: 2012-10-03 DOI:10.1155/2012/928159

Hong Mei Li, Jin Kyu Kim, Jai Man Jang, Sang Oh Kwon, Cheng Bi Cui, Soon Sung Lim

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引用次数: 16

Abstract

To evaluate the aldose reductase (AR) enzyme inhibitory ability of Prunella vulgaris L. extract, six compounds were isolated and tested for their effects. The components were subjected to in vitro bioassays to investigate their inhibitory assays using rat lens aldose reductase (rAR) and human recombinant AR (rhAR). Among them, caffeic acid ethylene ester showed the potent inhibition, with the IC(50) values of rAR and rhAR at 3.2 ± 0.55 μM and 12.58 ± 0.32 μM, respectively. In the kinetic analyses using Lineweaver-Burk plots of 1/velocity and 1/concentration of substrate, this compound showed noncompetitive inhibition against rhAR. Furthermore, it inhibited galactitol formation in a rat lens incubated with a high concentration of galactose. Also it has antioxidative as well as advanced glycation end products (AGEs) inhibitory effects. As a result, this compound could be offered as a leading compound for further study as a new natural products drug for diabetic complications.

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夏枯草对醛糖还原酶和蛋白糖基化的抑制作用。

为评价夏枯草提取物对醛糖还原酶(AR)酶的抑制作用，分离了6个化合物并进行了实验。采用大鼠晶状体醛糖还原酶(rAR)和人重组醛糖还原酶(rhAR)进行体外生物测定。其中，咖啡酸乙酯对rAR和rhAR具有较强的抑制作用，其IC(50)值分别为3.2±0.55 μM和12.58±0.32 μM。利用Lineweaver-Burk图对底物的1/速度和1/浓度进行动力学分析，发现该化合物对rhAR具有非竞争性抑制作用。此外，它抑制半乳糖在大鼠晶状体中与高浓度半乳糖孵育的形成。此外，它还具有抗氧化和晚期糖基化终产物(AGEs)抑制作用。因此，该化合物作为治疗糖尿病并发症的新型天然产物药物，可作为进一步研究的先导化合物。

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来源期刊

Journal of Biomedicine and Biotechnology 生物-生物工程与应用微生物

自引率

0.00%

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审稿时长

3 months