Islam Md Nurul, Ishita Ishrat Jahan, Jung Hyun Ah, Choi Jae Sue
Department of Food Science and Nutrition, Pukyong National University, Busan 608-737, Republic of Korea.
Department of Food Science and Human Nutrition, Chonbuk National University, Jeonju 561-756, Republic of Korea.
Food Chem Toxicol. 2014 Jul;69:55-62. doi: 10.1016/j.fct.2014.03.042. Epub 2014 Apr 5.
Vicenin 2, isolated from a traditionally used medicinal plant Artemisia capillaris, is a 6,8-di-C-glucoside of apigenin which has been previously reported to possess a wide variety of pharmacological activities including antioxidant, anti-inflammatory, anti-cancer, and hepatoprotective. However, there have not been any reports concerning its anti-diabetic potential until now. Therefore, in the present study, we evaluated the anti-diabetic potential of vicenin 2 via α-glucosidase, protein tyrosine phosphatase 1B (PTP1B), rat lens aldose reductase (RLAR), and advanced glycation end products (AGE) formation inhibitory assays. Vicenin 2 strongly inhibited α-glucosidase, PTP1B, and RLAR in the corresponding assays. In addition, vicenin 2 inhibited the formation of both fluorescent AGE and nonfluorescent AGE, e.g., CML, as well as the level of fructosamine in glucose-fructose-induced bovine serum albumin (BSA) glycation. In the test system, vicenin 2 suppressed glycation-induced protein oxidation by attenuating the formation of protein carbonyl groups as well as by inhibiting the modification of protein thiol groups. Moreover, vicenin 2 was found to be a potent inhibitor of glycation-induced formation of amyloid cross-β structures in BSA. Taken together, vicenin 2 might be a useful lead for the development of multiple target-oriented therapeutic modalities for the treatment of diabetes and diabetes-associated complications.
从传统药用植物茵陈蒿中分离得到的异荭草苷2是芹菜素的6,8 - 二 - C - 葡萄糖苷，此前有报道称其具有多种药理活性，包括抗氧化、抗炎、抗癌和保肝作用。然而，迄今为止尚未有关于其抗糖尿病潜力的报道。因此，在本研究中，我们通过α - 葡萄糖苷酶、蛋白酪氨酸磷酸酶1B（PTP1B）、大鼠晶状体醛糖还原酶（RLAR）以及晚期糖基化终产物（AGE）形成抑制试验评估了异荭草苷2的抗糖尿病潜力。在相应试验中，异荭草苷2强烈抑制α - 葡萄糖苷酶、PTP1B和RLAR。此外，异荭草苷2抑制荧光AGE和非荧光AGE（如羧甲基赖氨酸）的形成，以及葡萄糖 - 果糖诱导的牛血清白蛋白（BSA）糖基化中的果糖胺水平。在测试系统中，异荭草苷2通过减弱蛋白质羰基的形成以及抑制蛋白质巯基的修饰来抑制糖基化诱导的蛋白质氧化。此外，发现异荭草苷2是BSA中糖基化诱导的淀粉样β - 交叉结构形成的有效抑制剂。综上所述，异荭草苷2可能是开发用于治疗糖尿病及糖尿病相关并发症的多靶点治疗方法的有用先导化合物。
