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

Hyejin Kang; Sae Kwang Ku; Hyukjae Choi; Jong Sup Bae

doi:10.1016/j.bmcl.2016.03.030

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

Hyejin Kang, Sae Kwang Ku, Hyukjae Choi, Jong Sup Bae

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	1873-1876
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	26
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2016.03.030
State	Published - 15 Apr 2016

Keywords

Diketopiperazine
HUVEC
LPS
Vascular permeability

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2016.03.030

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title = "Three diketopiperazines from marine-derived bacteria inhibit LPS-induced endothelial inflammatory responses",

abstract = "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.",

keywords = "Diketopiperazine, HUVEC, LPS, Vascular permeability",

author = "Hyejin Kang and Ku, {Sae Kwang} and Hyukjae Choi and Bae, {Jong Sup}",

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doi = "10.1016/j.bmcl.2016.03.030",

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T1 - Three diketopiperazines from marine-derived bacteria inhibit LPS-induced endothelial inflammatory responses

AU - Kang, Hyejin

AU - Ku, Sae Kwang

AU - Choi, Hyukjae

AU - Bae, Jong Sup

PY - 2016/4/15

Y1 - 2016/4/15

N2 - 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.

AB - 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.

KW - Diketopiperazine

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KW - LPS

KW - Vascular permeability

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ER -

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

Abstract

Keywords

UN SDGs

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