Synthesis of Lipoamino Acids and Their Activity against Cerebral Ischemic Injury

Molecules

Li-Yun Yao¹  Qi Lin¹  Yin-Yao Niu¹  Ke-Min Deng¹  Jian-Hua Zhang¹ 

[1] Institute of Pharmaceutical Research, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China

关键词: lipoamino acids;    neuroprotection;    brain ischemia;    oxygen-glucose deprivation;   

DOI  :  10.3390/molecules14104051

来源: mdpi

【 摘 要 】

A series of lipoamino acids were synthesized and their neuroprotective effect against brain ischemia induced by oxygen-glucose deprivation (OGD) on rat cerebral slices was evaluated. Among these compounds, N-stearoyl-L-tyrosine (4), N-stearoyl-L-serine (5) and N-stearoyl-L-threonine (6) exhibited good neuroprotective activity. We found that the neuroprotective activity of lipoamino acids depended on the acyl group, the presence of a free carboxylic function and a free hydroxyl group at the branched chain of the amino acids. The results also showed that 5 was the most active compound, protecting rat brain slices against OGD as well as hydrogen peroxide (H₂O₂) insult at the range of 1–10 M.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.