Three diketopiperazines from marine-derived bacteria inhibit LPS-induced endothelial inflammatory responses

被引：14

作者：

Kang, Hyejin ^{[1
]}

Ku, Sae-Kwang ^{[2
]}

Choi, Hyukjae ^{[3
]}

Bae, Jong-Sup ^{[1
]}

机构：

[1] Kyungpook Natl Univ, Pharmaceut Sci Res Inst, Coll Pharm, CMRI,Plus KNU Multiom Based Creat Drug Res Team B, 80 Dahak Ro, Daegu 41566, South Korea

[2] Daegu Haany Univ, Dept Anat & Histol, Coll Korean Med, Gyongsan 38610, South Korea

[3] Yeungnam Univ, Coll Pharm, Gyongsan 38541, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 08期

基金：

新加坡国家研究基金会;

关键词：

Diketopiperazine; LPS; Vascular permeability; HUVEC; HOST-SPECIFIC PHYTOTOXIN; SPOTTED KNAPWEED; MECHANISMS; DYSFUNCTION; MACULOSIN; PROTEIN; INJURY; SEPSIS; SPONGE;

D O I：

10.1016/j.bmcl.2016.03.030

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Diketopiperazine is a natural products found from bacteria, fungi, marine sponges, gorgonian and red algae. They are cyclic dipeptides possessing relatively simple and rigid structures with chiral nature and various side chains. Endothelial dysfunction is a key pathological feature of many inflammatory diseases, including sepsis. In the present study, three (1-3) of diketopiperazines were isolated from two strains of marine-derived bacteria. The compounds were investigated for their effects against lipopolysaccharide (LPS)-mediated endothelial inflammatory responses in vitro and in vivo. From 1 mu M, 1-3 inhibited LPS-induced hyperpermeability, adhesion, and migration of leukocytes across a human endothelial cell monolayer and in mice in a dose-dependent manner suggesting that 1-3 may serve as potential scaffolds for the development of therapeutic agents to treat vascular inflammatory disorders. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：1873 / 1876

页数：4

共 30 条

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