Scopoletin from the Flower Buds of Magnolia fargesii Inhibits Protein Glycation, Aldose Reductase, and Cataractogenesis Ex Vivo
Scopoletin from the Flower Buds of Magnolia fargesii Inhibits Protein Glycation, Aldose Reductase, and Cataractogenesis Ex Vivo
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DOI：
10.1007/s12272-010-0904-z
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发表时间：
2010-09-01
影响因子：
6.7
通讯作者：
Kim, Jin Sook
中科院分区：
文献类型：
--
作者：
Lee, Jun;Kim, Nan Hee;Kim, Jin Sook
采用色谱分离的方法从厚朴花蕾中分离得到5个已知结构的化合物，分别为东莨菪碱(1)、northalifoline(2)、stigmist -4-en-3-one(3)、tiliroside(4)和oplopanone(5)。通过对光谱数据（包括1D和2d nmr）的解释以及与报道值的比较，确定了1-5的结构。其中化合物1 ~ 3为首次从法氏分枝杆菌中分离得到。所有分离株（1-5）进行体外生物测定，以评估其对晚期糖基化终产物形成和大鼠晶状体醛糖还原酶（RLAR）的抑制活性。化合物1对晚期糖基化终产物的形成具有显著的抑制活性，IC50值为2.93 μ M（氨基胍：961 μ M）；化合物1对RLAR具有显著的抑制活性，IC50值为22.5 μ M（3.3-四亚甲基戊二酸：28.7 μ M）。化合物4对RLAR具有较强的抑制活性（IC50 = 14.9 μ M）。在进一步的离体实验中，复方1可明显抑制木糖诱导的大鼠晶状体白内障的发生。
Five compounds previously known structures, scopoletin (1), northalifoline (2), stigmast-4-en-3-one (3), tiliroside (4), and oplopanone (5) were obtained from the flower buds of Magnolia fargesii using chromatographic separation methods. The structures of 1-5 were identified by the interpretation of their spectroscopic data including 1D- and 2D-NMR as well as by comparison with reported values. Three compounds 1-3 were found from M. fargesii for the first time in this study. All the isolates (1-5) were subjected to in vitro bioassays to evaluate the inhibitory activity on advanced glycation end products formation and rat lens aldose reductase (RLAR). Compound 1 showed a remarkable inhibitory activity on advanced glycation end products formation with IC50 value of 2.93 mu M (aminoguanidine: 961 mu M), and showed a significant RLAR inhibitory activity with IC50 value of 22.5 mu M (3.3-tetramethyleneglutaric acid: 28.7 mu M). Compound 4 exhibited potent inhibitory activity against RLAR (IC50 = 14.9 mu M). In the further experiment ex vivo, cataractogenesis of rat lenses induced with xylose was significantly inhibited by compound 1 treatment.