Anti-neuroinflammatory Activity of a Novel Cannabinoid Derivative by Inhibiting the NF-κB Signaling Pathway in Lipopolysaccharide-Induced BV-2 Microglial Cells
Microglial-mediated neuroinflammation has recently been implicated as one of the important mechanisms responsible for the progression of neurodegenerative diseases. Activated microglia cells produce various neurotoxic factors that are harmful to neurons. Therefore, suppression of the inflammatory re...
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Elsevier
2013-01-01
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Series: | Journal of Pharmacological Sciences |
Online Access: | http://www.sciencedirect.com/science/article/pii/S1347861319303871 |
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author | Sandeep Vasant More Ju-Young Park Byung-Wook Kim Hemant Kumar Hyung-Woo Lim Seong-Mook Kang Sushruta Koppula Sung-Hwa Yoon Dong-Kug Choi |
author_facet | Sandeep Vasant More Ju-Young Park Byung-Wook Kim Hemant Kumar Hyung-Woo Lim Seong-Mook Kang Sushruta Koppula Sung-Hwa Yoon Dong-Kug Choi |
author_sort | Sandeep Vasant More |
collection | DOAJ |
description | Microglial-mediated neuroinflammation has recently been implicated as one of the important mechanisms responsible for the progression of neurodegenerative diseases. Activated microglia cells produce various neurotoxic factors that are harmful to neurons. Therefore, suppression of the inflammatory response elicited by activated microglia is considered a potential therapeutic target for neurodegenerative diseases. The cannabinoid (CB) system is widespread in the central nervous system and is very crucial for modulating a spectrum of neurophysiological functions such as pain, appetite, and cognition. In the present study, we synthesized and investigated a novel CB derivative (CD-101) for its ability to suppress lipopolysaccharide (LPS)-mediated activation of BV-2 microglial cells and subsequent release of various inflammatory mediators. CD-101 significantly inhibited the production of inflammatory markers such as nitric oxide, cyclooxygenase-2, and pro-inflammatory cytokines such as tumor necrosis factor-α, interleukin-1β, and interleukin-6. The anti-neuroinflammatory effect of this novel cannabinoid derivative occurred by inhibiting p38MAPK phosphorylation and by decreasing nuclear translocation of p65 subunit of nuclear factor kappa-B in LPS-stimulated BV-2 microglial cells. These results suggest that the use of the cannabinoid derivative CD-101 might be a potential therapeutic target against neuroinflammatory disorders. Keywords:: lipopolysaccharide, microglia, neuroinflammation, cannabinoid signaling |
first_indexed | 2024-04-12T10:00:08Z |
format | Article |
id | doaj.art-9703c51b73154e899b042a0c9813829b |
institution | Directory Open Access Journal |
issn | 1347-8613 |
language | English |
last_indexed | 2024-04-12T10:00:08Z |
publishDate | 2013-01-01 |
publisher | Elsevier |
record_format | Article |
series | Journal of Pharmacological Sciences |
spelling | doaj.art-9703c51b73154e899b042a0c9813829b2022-12-22T03:37:35ZengElsevierJournal of Pharmacological Sciences1347-86132013-01-011212119130Anti-neuroinflammatory Activity of a Novel Cannabinoid Derivative by Inhibiting the NF-κB Signaling Pathway in Lipopolysaccharide-Induced BV-2 Microglial CellsSandeep Vasant More0Ju-Young Park1Byung-Wook Kim2Hemant Kumar3Hyung-Woo Lim4Seong-Mook Kang5Sushruta Koppula6Sung-Hwa Yoon7Dong-Kug Choi8Department of Biotechnology, Research Institute for Biomedical and Health Science, Konkuk University, Chungju 380-701, Republic of KoreaDepartment of Molecular Science and Technology, Ajou University, Suwon 443-749, Republic of KoreaDepartment of Biotechnology, Research Institute for Biomedical and Health Science, Konkuk University, Chungju 380-701, Republic of KoreaDepartment of Biotechnology, Research Institute for Biomedical and Health Science, Konkuk University, Chungju 380-701, Republic of KoreaDepartment of Biotechnology, Research Institute for Biomedical and Health Science, Konkuk University, Chungju 380-701, Republic of KoreaDepartment of Biotechnology, Research Institute for Biomedical and Health Science, Konkuk University, Chungju 380-701, Republic of KoreaDepartment of Biotechnology, Research Institute for Biomedical and Health Science, Konkuk University, Chungju 380-701, Republic of KoreaDepartment of Molecular Science and Technology, Ajou University, Suwon 443-749, Republic of KoreaDepartment of Biotechnology, Research Institute for Biomedical and Health Science, Konkuk University, Chungju 380-701, Republic of Korea; Corresponding author. choidk@kku.ac.krMicroglial-mediated neuroinflammation has recently been implicated as one of the important mechanisms responsible for the progression of neurodegenerative diseases. Activated microglia cells produce various neurotoxic factors that are harmful to neurons. Therefore, suppression of the inflammatory response elicited by activated microglia is considered a potential therapeutic target for neurodegenerative diseases. The cannabinoid (CB) system is widespread in the central nervous system and is very crucial for modulating a spectrum of neurophysiological functions such as pain, appetite, and cognition. In the present study, we synthesized and investigated a novel CB derivative (CD-101) for its ability to suppress lipopolysaccharide (LPS)-mediated activation of BV-2 microglial cells and subsequent release of various inflammatory mediators. CD-101 significantly inhibited the production of inflammatory markers such as nitric oxide, cyclooxygenase-2, and pro-inflammatory cytokines such as tumor necrosis factor-α, interleukin-1β, and interleukin-6. The anti-neuroinflammatory effect of this novel cannabinoid derivative occurred by inhibiting p38MAPK phosphorylation and by decreasing nuclear translocation of p65 subunit of nuclear factor kappa-B in LPS-stimulated BV-2 microglial cells. These results suggest that the use of the cannabinoid derivative CD-101 might be a potential therapeutic target against neuroinflammatory disorders. Keywords:: lipopolysaccharide, microglia, neuroinflammation, cannabinoid signalinghttp://www.sciencedirect.com/science/article/pii/S1347861319303871 |
spellingShingle | Sandeep Vasant More Ju-Young Park Byung-Wook Kim Hemant Kumar Hyung-Woo Lim Seong-Mook Kang Sushruta Koppula Sung-Hwa Yoon Dong-Kug Choi Anti-neuroinflammatory Activity of a Novel Cannabinoid Derivative by Inhibiting the NF-κB Signaling Pathway in Lipopolysaccharide-Induced BV-2 Microglial Cells Journal of Pharmacological Sciences |
title | Anti-neuroinflammatory Activity of a Novel Cannabinoid Derivative by Inhibiting the NF-κB Signaling Pathway in Lipopolysaccharide-Induced BV-2 Microglial Cells |
title_full | Anti-neuroinflammatory Activity of a Novel Cannabinoid Derivative by Inhibiting the NF-κB Signaling Pathway in Lipopolysaccharide-Induced BV-2 Microglial Cells |
title_fullStr | Anti-neuroinflammatory Activity of a Novel Cannabinoid Derivative by Inhibiting the NF-κB Signaling Pathway in Lipopolysaccharide-Induced BV-2 Microglial Cells |
title_full_unstemmed | Anti-neuroinflammatory Activity of a Novel Cannabinoid Derivative by Inhibiting the NF-κB Signaling Pathway in Lipopolysaccharide-Induced BV-2 Microglial Cells |
title_short | Anti-neuroinflammatory Activity of a Novel Cannabinoid Derivative by Inhibiting the NF-κB Signaling Pathway in Lipopolysaccharide-Induced BV-2 Microglial Cells |
title_sort | anti neuroinflammatory activity of a novel cannabinoid derivative by inhibiting the nf κb signaling pathway in lipopolysaccharide induced bv 2 microglial cells |
url | http://www.sciencedirect.com/science/article/pii/S1347861319303871 |
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