AETIQ: A novel synthetic compound with anti-inflammatory properties in activated microglia

Hyo Jin Son, Nari Shin, Eun Jung Shin, Dae Yoon Chi, Jai Seo, Cheol Soon Lee, Onyou Hwang

Research output: Contribution to journalArticle

1 Citation (Scopus)

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 languageEnglish (US)
Pages (from-to)766-774
Number of pages9
JournalInflammation
Volume37
Issue number3
DOIs
StatePublished - Jan 1 2014
Externally publishedYes

Fingerprint

Microglia
Anti-Inflammatory Agents
Down-Regulation
Matrix Metalloproteinase 3
Nitric Oxide Synthase Type II
Enzymes
Cyclooxygenase 2
Reverse Transcriptase Polymerase Chain Reaction
Interleukin-1
Neurodegenerative Diseases
Biological Availability
Reactive Oxygen Species
Nitric Oxide
Enzyme-Linked Immunosorbent Assay
Cytokines
Messenger RNA
Liver
Proteins
Therapeutics
2-acetyl-1-ethyl-7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinoline

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 journalArticle

Son, Hyo Jin ; Shin, Nari ; Shin, Eun Jung ; Chi, Dae Yoon ; Seo, Jai ; Lee, Cheol Soon ; Hwang, Onyou. / AETIQ : A novel synthetic compound with anti-inflammatory properties in activated microglia. In: Inflammation. 2014 ; Vol. 37, No. 3. pp. 766-774.
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