Abstract
Neuroinflammation is believed to be involved in the pathogenesis of neurodegenerative diseases. Our novel synthetic compound 2-acetyl-1-ethyl-7- hydroxy-6-methoxy-1, 2, 3, 4-tetrahydroisoquinoline (AETIQ) was tested for its anti-inflammatory properties in activated microglial BV-2 cells. AETIQ attenuated nitric oxide (NO) and reactive oxygen species generation. It also downregulated the production of the proinflammatory enzymes inducible NO synthase, cyclooxygenase-2, and matrix metalloproteinase-3 at both mRNA and protein levels. Furthermore, AETIQ suppressed generation of the proinflammatory cytokines IL-1β and TNF-α as determined by reverse transcriptase-polymerase chain reaction (RT-PCR) and ELISA assays. AETIQ attenuated NFκB signaling by downregulating NFκB nuclear translocation. The compound was stable against the liver enzymes in the microsomal and S9 fractions, indicative of good bioavailability. These results suggested that AETIQ might be utilized towards development of a therapy for neuroinflammation-related diseases.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 766-774 |
| Number of pages | 9 |
| Journal | Inflammation |
| Volume | 37 |
| Issue number | 3 |
| DOIs | |
| State | Published - Jan 1 2014 |
| Externally published | Yes |
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Keywords
- microglia
- neuroinflammation
- nitric oxide
- proinflammatory cytokines
- reactive oxygen species
ASJC Scopus subject areas
- Immunology and Allergy
- Immunology
Cite this
AETIQ : A novel synthetic compound with anti-inflammatory properties in activated microglia. / Son, Hyo Jin; Shin, Nari; Shin, Eun Jung; Chi, Dae Yoon; Seo, Jai; Lee, Cheol Soon; Hwang, Onyou.
In: Inflammation, Vol. 37, No. 3, 01.01.2014, p. 766-774.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - AETIQ
T2 - A novel synthetic compound with anti-inflammatory properties in activated microglia
AU - Son, Hyo Jin
AU - Shin, Nari
AU - Shin, Eun Jung
AU - Chi, Dae Yoon
AU - Seo, Jai
AU - Lee, Cheol Soon
AU - Hwang, Onyou
PY - 2014/1/1
Y1 - 2014/1/1
N2 - Neuroinflammation is believed to be involved in the pathogenesis of neurodegenerative diseases. Our novel synthetic compound 2-acetyl-1-ethyl-7- hydroxy-6-methoxy-1, 2, 3, 4-tetrahydroisoquinoline (AETIQ) was tested for its anti-inflammatory properties in activated microglial BV-2 cells. AETIQ attenuated nitric oxide (NO) and reactive oxygen species generation. It also downregulated the production of the proinflammatory enzymes inducible NO synthase, cyclooxygenase-2, and matrix metalloproteinase-3 at both mRNA and protein levels. Furthermore, AETIQ suppressed generation of the proinflammatory cytokines IL-1β and TNF-α as determined by reverse transcriptase-polymerase chain reaction (RT-PCR) and ELISA assays. AETIQ attenuated NFκB signaling by downregulating NFκB nuclear translocation. The compound was stable against the liver enzymes in the microsomal and S9 fractions, indicative of good bioavailability. These results suggested that AETIQ might be utilized towards development of a therapy for neuroinflammation-related diseases.
AB - Neuroinflammation is believed to be involved in the pathogenesis of neurodegenerative diseases. Our novel synthetic compound 2-acetyl-1-ethyl-7- hydroxy-6-methoxy-1, 2, 3, 4-tetrahydroisoquinoline (AETIQ) was tested for its anti-inflammatory properties in activated microglial BV-2 cells. AETIQ attenuated nitric oxide (NO) and reactive oxygen species generation. It also downregulated the production of the proinflammatory enzymes inducible NO synthase, cyclooxygenase-2, and matrix metalloproteinase-3 at both mRNA and protein levels. Furthermore, AETIQ suppressed generation of the proinflammatory cytokines IL-1β and TNF-α as determined by reverse transcriptase-polymerase chain reaction (RT-PCR) and ELISA assays. AETIQ attenuated NFκB signaling by downregulating NFκB nuclear translocation. The compound was stable against the liver enzymes in the microsomal and S9 fractions, indicative of good bioavailability. These results suggested that AETIQ might be utilized towards development of a therapy for neuroinflammation-related diseases.
KW - microglia
KW - neuroinflammation
KW - nitric oxide
KW - proinflammatory cytokines
KW - reactive oxygen species
UR - http://www.scopus.com/inward/record.url?scp=84902549648&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84902549648&partnerID=8YFLogxK
U2 - 10.1007/s10753-013-9795-8
DO - 10.1007/s10753-013-9795-8
M3 - Article
C2 - 24402420
AN - SCOPUS:84902549648
VL - 37
SP - 766
EP - 774
JO - Inflammation
JF - Inflammation
SN - 0360-3997
IS - 3
ER -