Choi Soo-Youn, Jung Sung-Hoon, Lee Hyun-Sun, Park Kwen-Woo, Yun Bong-Sik, Lee Kwang-Won
Department of Food Science, College of Life Sciences and Biotechnology, Korea University, 1,5-ga, Anam-dong, Sungbuk-ku, Seoul 136-701, South Korea.
Phytother Res. 2008 Mar;22(3):323-9. doi: 10.1002/ptr.2316.
The glycation reaction involves a series of non-enzymatic reactions between the carbonyl group on reducing sugars and the amino group on proteins leading to the formation of advanced glycation end-products (AGEs), which are acknowledged to be involved in the pathogenesis of diabetic and aging-related complications. Consequently, the development of AGE inhibitors is considered to have therapeutic potential in patients with diabetes or age-related diseases. The preliminary results showed that a methanol extract (PAE) of Plantago asiatica, which is traditionally used as a folk medicine in Asian countries to treat fever, cough, wound etc., had strong glycation inhibitory activity. The effects of the extract on AGE fluorescence were dose-dependent, reaching 41% inhibition at 0.1 microg/mL of extract. The purified principle from PAE was identified as plantamajoside. As well as antioxidant activities, in vitro glycation inhibitory activities with 10 and 25 mm plantamajoside were higher than those with 10 and 25 mm aminoguanidine. The results demonstrate that PAE and plantamajoside had significant effects on in vitro AGE formation, and the glycation inhibitory activity and antioxidant activity of plantamajoside were comparable to those obtained using millimolar concentrations of the standard antiglycation agent aminoguanidine, and the antioxidant ascorbate, respectively.
糖基化反应涉及还原糖上的羰基与蛋白质上的氨基之间的一系列非酶促反应,导致晚期糖基化终产物(AGEs)的形成,AGEs被认为与糖尿病及衰老相关并发症的发病机制有关。因此,AGE抑制剂的开发被认为对糖尿病患者或与年龄相关疾病的患者具有治疗潜力。初步结果表明,车前草的甲醇提取物(PAE)具有很强的糖基化抑制活性,在亚洲国家,车前草传统上被用作民间药物来治疗发热、咳嗽、伤口等。该提取物对AGE荧光的影响呈剂量依赖性,提取物浓度为0.1μg/mL时抑制率达41%。从PAE中纯化得到的主要成分被鉴定为大车前苷。除了抗氧化活性外,10和25 mM大车前苷的体外糖基化抑制活性高于10和25 mM氨基胍。结果表明,PAE和大车前苷对体外AGE的形成有显著影响,大车前苷的糖基化抑制活性和抗氧化活性分别与使用毫摩尔浓度的标准抗糖基化剂氨基胍和抗氧化剂抗坏血酸所获得的活性相当。