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Synthesis of Lipoamino Acids and Their Activity against Cerebral Ischemic Injury
Institute of Pharmaceutical Research, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China
* Author to whom correspondence should be addressed.
Received: 14 August 2009; in revised form: 22 September 2009 / Accepted: 29 September 2009 / Published: 12 October 2009
Abstract: 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.
Keywords: lipoamino acids; neuroprotection; brain ischemia; oxygen-glucose deprivation
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MDPI and ACS Style
Yao, L.-Y.; Lin, Q.; Niu, Y.-Y.; Deng, K.-M.; Zhang, J.-H.; Lu, Y. Synthesis of Lipoamino Acids and Their Activity against Cerebral Ischemic Injury. Molecules 2009, 14, 4051-4064.
Yao L-Y, Lin Q, Niu Y-Y, Deng K-M, Zhang J-H, Lu Y. Synthesis of Lipoamino Acids and Their Activity against Cerebral Ischemic Injury. Molecules. 2009; 14(10):4051-4064.
Yao, Li-Yun; Lin, Qi; Niu, Yin-Yao; Deng, Ke-Min; Zhang, Jian-Hua; Lu, Yang. 2009. "Synthesis of Lipoamino Acids and Their Activity against Cerebral Ischemic Injury." Molecules 14, no. 10: 4051-4064.