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Effects of 3-(2-Hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (HMP) upon signalling pathways of lipopolysaccharide-induced iNOS synthesis in RAW 264.7 cells.

NO synthesis in the RAW 264.7 murine macrophage line. The inhibition of NO synthesis was related to inhibition of p38 phosphorylation and kinase activity that led to significant inhibition of phosphorylation of ATF-2. This effect in turn caused inhibition of AP-1-DNA binding which partially explains...

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Main Authors: Choi, Yi Liew, Kok, Wai Lam, Min, Kyu Kim, Harith, Hanis Hazeera, Chau, Ling Tham, Cheah, Yoke Kqueen, Sulaiman, Mohd Roslan, Lajis, Md. Nordin, Israf Ali, Daud Ahmad
Format: Article
Language:English
English
Published: Elsevier 2011
Online Access:http://psasir.upm.edu.my/id/eprint/24565/1/Effects%20of%203.pdf
http://psasir.upm.edu.my/id/eprint/24565/
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spelling my.upm.eprints.245652015-10-05T08:22:41Z http://psasir.upm.edu.my/id/eprint/24565/ Effects of 3-(2-Hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (HMP) upon signalling pathways of lipopolysaccharide-induced iNOS synthesis in RAW 264.7 cells. Choi, Yi Liew Kok, Wai Lam Min, Kyu Kim Harith, Hanis Hazeera Chau, Ling Tham Cheah, Yoke Kqueen Sulaiman, Mohd Roslan Lajis, Md. Nordin Israf Ali, Daud Ahmad NO synthesis in the RAW 264.7 murine macrophage line. The inhibition of NO synthesis was related to inhibition of p38 phosphorylation and kinase activity that led to significant inhibition of phosphorylation of ATF-2. This effect in turn caused inhibition of AP-1-DNA binding which partially explains the inhibitory effect upon the synthesis of iNOS. HMP had no effect upon phosphorylation of JNK, ERK1/2 and STAT-1. Kinase activity of JNK and ERK1/2 was also not affected by HMP as determined by levels of phosphorylated c-jun and phosphorylated elk-1. Furthermore HMP failed to block phosphorylation of IκBα, and subsequent nuclear translocation and DNA-binding activity of p65 NF-κB in IFN-γ/LPS-induced RAW 264.7 cells. Molecular docking experiments confirmed that HMP fits well in the highly conserved hydrophobic pocket of p38 MAP kinase. We conclude that the synthetic HMP is a chalcone analogue that selectively inhibits the p38/ATF-2 and AP-1 signaling pathways in the NO synthesis by the macrophage RAW 264.7. Elsevier 2011-01 Article PeerReviewed application/pdf en http://psasir.upm.edu.my/id/eprint/24565/1/Effects%20of%203.pdf Choi, Yi Liew and Kok, Wai Lam and Min, Kyu Kim and Harith, Hanis Hazeera and Chau, Ling Tham and Cheah, Yoke Kqueen and Sulaiman, Mohd Roslan and Lajis, Md. Nordin and Israf Ali, Daud Ahmad (2011) Effects of 3-(2-Hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (HMP) upon signalling pathways of lipopolysaccharide-induced iNOS synthesis in RAW 264.7 cells. International Immunopharmacology, 11 (1). pp. 85-95. ISSN 1567-5769; ESSN: 1878-1705 10.1016/j.intimp.2010.10.011 English
institution Universiti Putra Malaysia
building UPM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Putra Malaysia
content_source UPM Institutional Repository
url_provider http://psasir.upm.edu.my/
language English
English
description NO synthesis in the RAW 264.7 murine macrophage line. The inhibition of NO synthesis was related to inhibition of p38 phosphorylation and kinase activity that led to significant inhibition of phosphorylation of ATF-2. This effect in turn caused inhibition of AP-1-DNA binding which partially explains the inhibitory effect upon the synthesis of iNOS. HMP had no effect upon phosphorylation of JNK, ERK1/2 and STAT-1. Kinase activity of JNK and ERK1/2 was also not affected by HMP as determined by levels of phosphorylated c-jun and phosphorylated elk-1. Furthermore HMP failed to block phosphorylation of IκBα, and subsequent nuclear translocation and DNA-binding activity of p65 NF-κB in IFN-γ/LPS-induced RAW 264.7 cells. Molecular docking experiments confirmed that HMP fits well in the highly conserved hydrophobic pocket of p38 MAP kinase. We conclude that the synthetic HMP is a chalcone analogue that selectively inhibits the p38/ATF-2 and AP-1 signaling pathways in the NO synthesis by the macrophage RAW 264.7.
format Article
author Choi, Yi Liew
Kok, Wai Lam
Min, Kyu Kim
Harith, Hanis Hazeera
Chau, Ling Tham
Cheah, Yoke Kqueen
Sulaiman, Mohd Roslan
Lajis, Md. Nordin
Israf Ali, Daud Ahmad
spellingShingle Choi, Yi Liew
Kok, Wai Lam
Min, Kyu Kim
Harith, Hanis Hazeera
Chau, Ling Tham
Cheah, Yoke Kqueen
Sulaiman, Mohd Roslan
Lajis, Md. Nordin
Israf Ali, Daud Ahmad
Effects of 3-(2-Hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (HMP) upon signalling pathways of lipopolysaccharide-induced iNOS synthesis in RAW 264.7 cells.
author_facet Choi, Yi Liew
Kok, Wai Lam
Min, Kyu Kim
Harith, Hanis Hazeera
Chau, Ling Tham
Cheah, Yoke Kqueen
Sulaiman, Mohd Roslan
Lajis, Md. Nordin
Israf Ali, Daud Ahmad
author_sort Choi, Yi Liew
title Effects of 3-(2-Hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (HMP) upon signalling pathways of lipopolysaccharide-induced iNOS synthesis in RAW 264.7 cells.
title_short Effects of 3-(2-Hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (HMP) upon signalling pathways of lipopolysaccharide-induced iNOS synthesis in RAW 264.7 cells.
title_full Effects of 3-(2-Hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (HMP) upon signalling pathways of lipopolysaccharide-induced iNOS synthesis in RAW 264.7 cells.
title_fullStr Effects of 3-(2-Hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (HMP) upon signalling pathways of lipopolysaccharide-induced iNOS synthesis in RAW 264.7 cells.
title_full_unstemmed Effects of 3-(2-Hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (HMP) upon signalling pathways of lipopolysaccharide-induced iNOS synthesis in RAW 264.7 cells.
title_sort effects of 3-(2-hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (hmp) upon signalling pathways of lipopolysaccharide-induced inos synthesis in raw 264.7 cells.
publisher Elsevier
publishDate 2011
url http://psasir.upm.edu.my/id/eprint/24565/1/Effects%20of%203.pdf
http://psasir.upm.edu.my/id/eprint/24565/
_version_ 1643828397873299456
score 13.211869

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