Asymmetric synthesis of novel N-(1-phenyl-2,3-dihydroxypropyl)arachidonylamides and evaluation of their anti-inflammatory activity.
Asymmetric synthesis of novel N-(1-phenyl-2,3-dihydroxypropyl)arachidonylamides and evaluation of their anti-inflammatory activity.
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新型N-(1-苯基-2,3-二羟丙基)花生四烯酰胺的不对称合成及其抗炎活性评价。
DOI：
10.1016/j.lfs.2012.06.040
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发表时间：
2013
期刊：
影响因子：
6.1
通讯作者：
Li,Guigen
中科院分区：
文献类型：
--
作者：
Kattamuri,PadmanabhaV;Salmonsen,Rebecca;McQuain,Catherine;Burstein,Sumner;Sun,Hao;Li,Guigen
目的设计合成N-（1-苯基-2，3-二羟丙基）花生四烯酰胺类化合物，并对其镇痛抗炎活性进行评价。我们的模型由RAW 264.7细胞的培养单层组成，其中在LPS（10 ng/ml）刺激和用0.1、0.3、1.0、1.5、1关键发现我们的数据表明，我们的几种化合物具有增加PGJ产量的能力，也可能增加程序性细胞死亡（凋亡）的发生。意义因此，这些药物是治疗以持续（慢性）炎症及其相关疼痛为特征的疾病的潜在候选药物。
AIMSTo design and synthesize novel N-(1-phenyl-2,3-dihydroxypropyl)arachidonylamides and evaluate their analgesic and anti-inflammatory potential.MAIN METHODSThe 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-Δ13,14-PGJ2(PGJ) are measured by ELISA following LPS (10ng/ml) stimulation and treatment with 0.1, 0.3, 1.0, 3.0 and 10μM concentrations of the compounds.KEY FINDINGSOur 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).SIGNIFICANCEThus these agents are potential candidates for the therapy of conditions characterized by ongoing (chronic) inflammation and its associated pain.