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

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• 作者：Hyejin Kang^a ; ^&dagger ; ; Sae-Kwang Ku^b ; ^&dagger ; ; Hyukjae Choi^c ; Jong-Sup Bae^a ; ^{baejs@knu.ac.kr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Diketopiperazine ; LPS ; Vascular permeability ; HUVEC
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 April 2016
• 年：2016
• 卷：26
• 期：8
• 页码：1873-1876
• 全文大小：1085 K

文摘

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 μM, 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.