AETIQ: A Novel Synthetic Compound with Anti-inflammatory Properties in Activated Microglia

作者：Son Hyo Jin; Shin Nari; Shin Eun Jung; Chi Dae Yoon; Seo Jai Woong; Lee Cheol Soon; Hwang Onyou^*

来源：Inflammation, 2014, 37(3): 766-774.

DOI：10.1007/s10753-013-9795-8

• microglia
• neuroinflammation
• nitric oxide
• proinflammatory cytokines
• reactive oxygen species

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-1 beta and TNF-alpha as determined by reverse transcriptase-polymerase chain reaction (RT-PCR) and ELISA assays. AETIQ attenuated NF kappa B signaling by downregulating NF kappa B 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.

• 出版日期2014-6