Natural Products Laboratory, Indian Institute of Chemical Technology, Uppal Road, Hyderabad 500607, India.
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4928-31. doi: 10.1016/j.bmcl.2011.04.131. Epub 2011 May 5.
Bergenin (1), major bioactive compound isolated from methanolic extract of Mallotus philippinensis, displayed moderate AGE inhibition activity (IC(50)=186.73 μM). A series of derivatives of bergenin (3a-k) containing variety of aromatic acids were synthesized under mild conditions by modification of sugar part. Selective esterification of hydroxyl groups on the sugar part enhanced antiglycation potential of bergenin. Compounds 3j and 3k exhibited potent antiglycation activity with the IC(50) values of 60.75 and 12.28 μM, respectively.
Bergenin（1）是从马缨丹的甲醇提取物中分离得到的主要生物活性化合物，显示出中等的 AGE 抑制活性（IC（50）=186.73 μM）。通过修饰糖部分，合成了一系列含有各种芳香酸的 Bergenin 衍生物（3a-k）。糖部分上羟基的选择性酯化增强了 Bergenin 的抗糖化潜力。化合物 3j 和 3k 表现出较强的抗糖化活性，IC（50）值分别为 60.75 和 12.28 μM。
