Asymmetric synthesis of novel N-(1-phenyl-2,3-dihydroxypropyl)arachidonylamides and evaluation of their anti-inflammatory activity

被引:1
|
作者
Kattamuri, Padmanabha V. [1 ]
Salmonsen, Rebecca [2 ]
McQuain, Catherine [2 ]
Burstein, Sumner [2 ]
Sun, Hao [3 ]
Li, Guigen [1 ,3 ]
机构
[1] Texas Tech Univ, Dept Chem & Biochem, Lubbock, TX 79409 USA
[2] Univ Massachusetts, Sch Med, Dept Biochem & Mol Pharmacol, Worcester, MA 01605 USA
[3] Nanjing Univ, Inst Chem & Biomed Sci, Nanjing 210093, Jiangsu, Peoples R China
基金
美国国家卫生研究院;
关键词
Cannabinoid receptor; Anandamide; Arachidonyl amide; 15-Deoxy-Delta(13,14)-PGJ(2) (PGJ) stimulation; Apoptosis; CB2 CANNABINOID RECEPTORS; INFLAMMATORY RESOLUTION; ANANDAMIDE; ANALOGS; ARACHIDONYLETHANOLAMIDE; ACID;
D O I
10.1016/j.lfs.2012.06.040
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
Aims: To design and synthesize novel N-(1-phenyl-2,3-dihydroxypropyl)arachidonylamides and evaluate their analgesic and anti-inflammatory potential. Main methods: The murine macrophage cell line RAW 264.7 has been widely used as a model for inflammatory responses in vitro. Our model consists of cultured monolayers of RAW 264.7 cells in which media concentrations of 15-deoxy-Delta(13,14)-PGJ(2) (PGJ) are measured by ELISA following LPS (10 ng/ml) stimulation and treatment with 0.1. 0.3, 1.0.3.0 and 10 mu M concentrations of the compounds. Key findings: Our data indicate that several of our compounds have the capacity to increase production of PGJ and may also increase the occurrence of programmed cell death (apoptosis). Significance: Thus these agents are potential candidates for the therapy of conditions characterized by ongoing (chronic) inflammation and its associated pain. (C) 2012 Elsevier Inc. All rights reserved.
引用
收藏
页码:506 / 511
页数:6
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