Abstract：
Diabetes complications are associated with aldose reductase (AR) and advanced glycation end products (AGEs). Using bioassay-guided isolation by column chromatography, 10 flavonoids and one coumarin were isolated from Poncirus trifoliata Rafin and tested in vitro for an inhibitory effect against human recombinant AR (HRAR) and rat lens AR (RLAR). Prunin, narirutin, and naringin inhibited RLAR (IC50 0.48-2.84 μM) and HRAR (IC50 0.68-4.88 μM). Docking simulations predicted negative binding energies and interactions with the RLAR and HRAR binding pocket residues. Prunin (0.1 and 12.5 μM) prevented the formation of fluorescent AGEs and nonfluorescent Nε-(carboxymethyl) lysine (CML), as well as the fructose-glucose-mediated protein glycation and oxidation of human serum albumin (HSA). Prunin suppressed the formation of the β-cross-amyloid structure of HSA. These results indicate that prunin inhibits oxidation-dependent protein damage, AGE formation, and AR, which may help prevent diabetes complications.
摘要：
糖尿病并发症与醛糖还原酶（AR）和晚期糖基化终产物（AGEs）有关。使用生物测定指导的柱层析分离，从三叶草中分离出10种类黄酮和1种香豆素，并在体外测试了其对人重组AR（HRAR）和大鼠晶状体AR（RLAR）的抑制作用。普宁,那利鲁丁,和柚皮苷抑制RLAR(IC500.48-2.84μM)和HRAR(IC500.68-4.88μM)。对接模拟预测了负结合能以及与RLAR和HRAR结合袋残基的相互作用。普宁（0.1和12.5μM）防止荧光AGEs和非荧光Nε-（羧甲基）赖氨酸（CML）的形成，以及果糖-葡萄糖介导的人血清白蛋白（HSA）的蛋白质糖基化和氧化。Prunin抑制了HSA的β-交叉淀粉样蛋白结构的形成。这些结果表明，prunin抑制氧化依赖性蛋白质损伤，年龄形成，AR,这可能有助于预防糖尿病并发症。
