Middle Molecular Weight Heparinyl Amino Acid Derivatives (MHADs) Function as Indirect Radical Scavengers in Vitro

We conducted the novel synthesis of middle molecular weight heparinyl amino acid derivatives (MHADs) to reduce the adverse effect of heparin (HE) based on its anticoagulant activity. Subsequently, we investigated the radical scavenging effects of 12 kinds of MHAD on cultured human umbilical vein endothelial cells (HUV-ECs) damaged by oxygen free radicals using xanthine and xanthine oxidase in vitro. As a result, middle molecular weight heparinyl phenylalanine, middle molecular weight heparinyl leucine, and middle molecular weight heparinyl tyrosine showed significant protective effects on HUV-ECs. In conclusion, these three HE derivatives might be candidates for therapeutic agents to treat diseases attributed to peroxidation.