Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE2 Productions and Nitric Oxide in Murine RAW 264.7 Macrophages

A series of thirteen triarylpyrazole analogs were investigated as inhibitors of lipopolysaccharide (LPS)-induced prostaglandin E2 (PGE2) and nitric oxide (NO) production in RAW 264.7 macrophages. The target compounds 1a–m</...

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Autores principales:	Mahmoud M. Gamal El-Din, Mohammed I. El-Gamal, Young-Do Kwon, Su-Yeon Kim, Hee-Soo Han, Sang-Eun Park, Chang-Hyun Oh, Kyung-Tae Lee, Hee-Kwon Kim
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	amide anti-inflammatory COX-2 iNOS NO PGE<sub>2</sub> Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/f9d0f03beb1344b18df4f2d77a158151
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spelling	oai:doaj.org-article:f9d0f03beb1344b18df4f2d77a1581512021-11-11T18:29:24ZEvaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE<sub>2</sub> Productions and Nitric Oxide in Murine RAW 264.7 Macrophages10.3390/molecules262164891420-3049https://doaj.org/article/f9d0f03beb1344b18df4f2d77a1581512021-10-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6489https://doaj.org/toc/1420-3049A series of thirteen triarylpyrazole analogs were investigated as inhibitors of lipopolysaccharide (LPS)-induced prostaglandin E<sub>2</sub> (PGE<sub>2</sub>) and nitric oxide (NO) production in RAW 264.7 macrophages. The target compounds <b>1a</b>–<b>m</b> have first been assessed for cytotoxicity against RAW 264.7 macrophages to determine their non-cytotoxic concentration(s) for anti-inflammatory testing to make sure that the inhibition of PGE<sub>2</sub> and NO production would not be caused by cytotoxicity. It was found that compounds <b>1f</b> and <b>1m</b> were the most potent PGE<sub>2</sub> inhibitors with IC<sub>50</sub> values of 7.1 and 1.1 μM, respectively. In addition, these compounds also showed inhibitory effects of 11.6% and 37.19% on LPS-induced NO production, respectively. The western blots analysis of COX-2 and iNOS showed that the PGE<sub>2</sub> and NO inhibitory effect of compound <b>1m</b> are attributed to inhibition of COX-2 and iNOS protein expression through inactivation of p38.Mahmoud M. Gamal El-DinMohammed I. El-GamalYoung-Do KwonSu-Yeon KimHee-Soo HanSang-Eun ParkChang-Hyun OhKyung-Tae LeeHee-Kwon KimMDPI AGarticleamideanti-inflammatoryCOX-2iNOSNOPGE<sub>2</sub>Organic chemistryQD241-441ENMolecules, Vol 26, Iss 6489, p 6489 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	amide anti-inflammatory COX-2 iNOS NO PGE<sub>2</sub> Organic chemistry QD241-441
spellingShingle	amide anti-inflammatory COX-2 iNOS NO PGE<sub>2</sub> Organic chemistry QD241-441 Mahmoud M. Gamal El-Din Mohammed I. El-Gamal Young-Do Kwon Su-Yeon Kim Hee-Soo Han Sang-Eun Park Chang-Hyun Oh Kyung-Tae Lee Hee-Kwon Kim Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE<sub>2</sub> Productions and Nitric Oxide in Murine RAW 264.7 Macrophages
description	A series of thirteen triarylpyrazole analogs were investigated as inhibitors of lipopolysaccharide (LPS)-induced prostaglandin E<sub>2</sub> (PGE<sub>2</sub>) and nitric oxide (NO) production in RAW 264.7 macrophages. The target compounds <b>1a</b>–<b>m</b> have first been assessed for cytotoxicity against RAW 264.7 macrophages to determine their non-cytotoxic concentration(s) for anti-inflammatory testing to make sure that the inhibition of PGE<sub>2</sub> and NO production would not be caused by cytotoxicity. It was found that compounds <b>1f</b> and <b>1m</b> were the most potent PGE<sub>2</sub> inhibitors with IC<sub>50</sub> values of 7.1 and 1.1 μM, respectively. In addition, these compounds also showed inhibitory effects of 11.6% and 37.19% on LPS-induced NO production, respectively. The western blots analysis of COX-2 and iNOS showed that the PGE<sub>2</sub> and NO inhibitory effect of compound <b>1m</b> are attributed to inhibition of COX-2 and iNOS protein expression through inactivation of p38.
format	article
author	Mahmoud M. Gamal El-Din Mohammed I. El-Gamal Young-Do Kwon Su-Yeon Kim Hee-Soo Han Sang-Eun Park Chang-Hyun Oh Kyung-Tae Lee Hee-Kwon Kim
author_facet	Mahmoud M. Gamal El-Din Mohammed I. El-Gamal Young-Do Kwon Su-Yeon Kim Hee-Soo Han Sang-Eun Park Chang-Hyun Oh Kyung-Tae Lee Hee-Kwon Kim
author_sort	Mahmoud M. Gamal El-Din
title	Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE<sub>2</sub> Productions and Nitric Oxide in Murine RAW 264.7 Macrophages
title_short	Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE<sub>2</sub> Productions and Nitric Oxide in Murine RAW 264.7 Macrophages
title_full	Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE<sub>2</sub> Productions and Nitric Oxide in Murine RAW 264.7 Macrophages
title_fullStr	Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE<sub>2</sub> Productions and Nitric Oxide in Murine RAW 264.7 Macrophages
title_full_unstemmed	Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE<sub>2</sub> Productions and Nitric Oxide in Murine RAW 264.7 Macrophages
title_sort	evaluation of the inhibitory effects of pyridylpyrazole derivatives on lps-induced pge<sub>2</sub> productions and nitric oxide in murine raw 264.7 macrophages
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/f9d0f03beb1344b18df4f2d77a158151
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Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE<sub>2</sub> Productions and Nitric Oxide in Murine RAW 264.7 Macrophages

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