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

来源：

LIFE SCIENCES | 2013年 / 92卷 / 8-9期

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

页码：506 / 511

页数：6

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