Glycation inhibitory activity and the identification of an active compound in Plantago asiatica extract

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 μg/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. Copyright © 2007 John Wiley & Sons, Ltd.