Aldose Reductase Inhibitory Compounds from Xanthium strumarium

• Published in: Archives of pharmacal research 2013, 36(9), , pp.1090-1095
• Main Authors: Yoon, Ha Na, Lee, Min Young, Kim, Jin-Kyu, Suh, Hong-Won, Lim, Soon Sung
• Format: Article
• Language: English
• Subjects: Aldehyde Reductase - antagonists & inhibitors; Aldehyde Reductase - genetics; Aldehyde Reductase - metabolism; Animals; Caffeic Acids - chemistry; Caffeic Acids - isolation & purification; Caffeic Acids - pharmacology; Diabetes Complications - prevention & control; Drug Discovery; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - isolation & purification; Enzyme Inhibitors - pharmacology; Erythrocytes - drug effects; Erythrocytes - enzymology; Erythrocytes - metabolism; Ethnopharmacology; Eye Proteins - antagonists & inhibitors; Eye Proteins - metabolism; Fruit - chemistry; Galactitol - metabolism; Humans; In Vitro Techniques; Lens, Crystalline - drug effects; Lens, Crystalline - enzymology; Lens, Crystalline - metabolism; Male; Medicine; Molecular Structure; Pharmacology/Toxicology; Pharmacy; Quinic Acid - analogs & derivatives; Quinic Acid - chemistry; Quinic Acid - isolation & purification; Quinic Acid - pharmacology; Rats; Rats, Sprague-Dawley; Recombinant Proteins - chemistry; Recombinant Proteins - metabolism; Republic of Korea; Research Article; Xanthium - chemistry; 약학
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/s12272-013-0123-5

As part of our ongoing search for natural sources of therapeutic and preventive agents for diabetic complications, we evaluated the inhibitory effects of components of the fruit of Xanthium strumarium ( X. strumarium ) on aldose reductase (AR) and galactitol formation in rat lenses with high levels of glucose. To identify the bioactive components of X. strumarium , 7 caffeoylquinic acids and 3 phenolic compounds were isolated and their chemical structures were elucidated on the basis of spectroscopic evidence and comparison with published data. The abilities of 10 X. strumarium -derived components to counteract diabetic complications were investigated by means of inhibitory assays with rat lens AR (rAR) and recombinant human AR (rhAR). From the 10 isolated compounds, methyl-3,5-di- O -caffeoylquinate showed the most potent inhibition, with IC 50 values of 0.30 and 0.67 μM for rAR and rhAR, respectively. In the kinetic analyses using Lineweaver–Burk plots of 1/velocity and 1/substrate, methyl-3,5-di- O -caffeoylquinate showed competitive inhibition of rhAR. Furthermore, methyl-3,5-di- O -caffeoylquinate inhibited galactitol formation in the rat lens and in erythrocytes incubated with a high concentration of glucose, indicating that this compound may be effective in preventing diabetic complications.