原创力文档synthesis of lipoamino acids and their activity against cerebral ischemic injury合成lipoamino酸和他们的活动对脑缺血性损伤.pdfVIP
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synthesis of lipoamino acids and their activity against cerebral ischemic injury合成lipoamino酸和他们的活动对脑缺血性损伤
Molecules 2009, 14, 4051-4064; doi:10.3390/molecule
OPEN ACCESS
molecules
ISSN 1420-3049
/journal/molecules
Article
Synthesis of Lipoamino Acids and Their Activity against
Cerebral Ischemic Injury
Li-Yun Yao, Qi Lin, Yin-Yao Niu, Ke-Min Deng, Jian-Hua Zhang and Yang Lu *
Institute of Pharmaceutical Research, Shanghai Jiao Tong University School of Medicine, Shanghai
200025, China
* Author to whom correspondence should be addressed; E-Mail: huaxue@.
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 (H O ) insult at the range of 1–10 M.
2 2
Keywords: lipoamino acids; neuroprotection; brain ischemia; oxygen-glucose deprivation
1. Introduction
Cerebral ischemia would lead
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