Anti-inflammatory Activity of Natural Geranylated Flavonoids: Cyclooxygenase and Lipoxygenase Inhibitory Properties and Proteomic Analysis

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00027162%3A_____%2F17%3AN0000114" target="_blank" >RIV/00027162:_____/17:N0000114 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/61389030:_____/17:00476495 RIV/61388963:_____/17:00476495 RIV/62157124:16370/17:43875523

Výsledek na webu

<a href="http://pubs.acs.org/doi/abs/10.1021/acs.jnatprod.6b01011" target="_blank" >http://pubs.acs.org/doi/abs/10.1021/acs.jnatprod.6b01011</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1021/acs.jnatprod.6b01011" target="_blank" >10.1021/acs.jnatprod.6b01011</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Anti-inflammatory Activity of Natural Geranylated Flavonoids: Cyclooxygenase and Lipoxygenase Inhibitory Properties and Proteomic Analysis

Popis výsledku v původním jazyce

Geranyl flavones have been studied as compounds That potentially can be developed as anti-inflammatory agents. A series of natural geranylated flavanones was isolated from Paulownia, tomentosa fruits; and these compounds were studied for their anti-inflammatory activity and possible mechanism of action. Two new compounds were characterized [paulownione C (17) and tomeritodiplacone O (20)], and all of the isolated derivatives were assayed for their ability to inhibit cyclooxygenases, (COX-1 and COX-2) and 5-lipoxygenase (5-LOX). The compounds tested showed variable degrees of activity, with several of them showing activity comparable to or greater than the standards used in COX-1, COX-2, and 5-LOX assays. However, Only the compound tomeritodiplacone O (20) showed more selectivity against COX-2 versus COX-1 when compared with ibuprofen. The ability of the test compounds to interact with the above-mentioned enzymes-was supported by docking studies, which revealed the possible incorporation of selected test substances into the active sites of these enzymes. Furthermore, one of the COX/LOX dual inhibitors, diplacone (14) (a major geranylated flavanone of P. tomentosa), was studied in vitro to obtain a proteomic overview of its effect on inflammation in LPS-treated THP-1 macrophages, supporting its previously observed anti-inflammatory activity and revealing the mechanism of its anti-inflammatory effect.

Název v anglickém jazyce

Anti-inflammatory Activity of Natural Geranylated Flavonoids: Cyclooxygenase and Lipoxygenase Inhibitory Properties and Proteomic Analysis

Popis výsledku anglicky

Geranyl flavones have been studied as compounds That potentially can be developed as anti-inflammatory agents. A series of natural geranylated flavanones was isolated from Paulownia, tomentosa fruits; and these compounds were studied for their anti-inflammatory activity and possible mechanism of action. Two new compounds were characterized [paulownione C (17) and tomeritodiplacone O (20)], and all of the isolated derivatives were assayed for their ability to inhibit cyclooxygenases, (COX-1 and COX-2) and 5-lipoxygenase (5-LOX). The compounds tested showed variable degrees of activity, with several of them showing activity comparable to or greater than the standards used in COX-1, COX-2, and 5-LOX assays. However, Only the compound tomeritodiplacone O (20) showed more selectivity against COX-2 versus COX-1 when compared with ibuprofen. The ability of the test compounds to interact with the above-mentioned enzymes-was supported by docking studies, which revealed the possible incorporation of selected test substances into the active sites of these enzymes. Furthermore, one of the COX/LOX dual inhibitors, diplacone (14) (a major geranylated flavanone of P. tomentosa), was studied in vitro to obtain a proteomic overview of its effect on inflammation in LPS-treated THP-1 macrophages, supporting its previously observed anti-inflammatory activity and revealing the mechanism of its anti-inflammatory effect.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

40301 - Veterinary science

Projekt

<a href="/cs/project/ED0006%2F01%2F01" target="_blank" >ED0006/01/01: Centrum pro aplikovanou mikrobiologii a imunologii ve veterinární medicíne</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2017

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Journal of Natural Products

ISSN

0163-3864

e-ISSN

—

Svazek periodika

80

Číslo periodika v rámci svazku

4

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

8

Strana od-do

999-1006

Kód UT WoS článku

000400538800026

EID výsledku v databázi Scopus

—