Paraliane and pepluane diterpenes as anti-inflammatory agents: First insights in structure-activity relationships

被引：23
作者：
Barile, Elisa
Fattorusso, Ernesto
Ialenti, Armando
Ianaro, Angela
Lanzotti, Virginia
机构：
[1] Univ Molise, DISTAAM, I-86100 Campobasso, Italy
[2] Univ Naples Federico II, Dipartimento Chim Sostanze Nat, I-80131 Naples, Italy
[3] Univ Naples Federico II, Dipartimento Farmacol Sperimentale, I-80131 Naples, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 15期
关键词：
euphorbiae; natural products; diterpenes; paraliane; pepluane; anti-inflammatory activity; nitric oxide; SAR studies;
D O I：
10.1016/j.bmcl.2007.05.072
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two new diterpenes, named paralianone (2) and pepluene (3), based, respectively, on rare paraliane and pepluane skeletons, have been isolated from Euphorbia paralias, together with two known analogues (4 and 5), and their stereostructure determined by spectroscopic methods. The isolated compounds were tested as anti-inflammatory agents in vitro for evaluating their ability to inhibit the nitric oxide production in LPS-stimulated J774 murine macrophages. Compound 4 showed the highest anti-inflammatory activity comparable to those recently discovered for pepluanone (1). The data obtained provided first insights towards the structure-activity relationship of this class of compounds highlighting the key role of D-ring structure. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4196 / 4200
页数：5
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