• Tohoku J. Exp. Med. · Jul 2024

    New Dihydropyridine Derivative Attenuates NF-κB Activation via Suppression of Calcium Influx in a Mouse BV-2 Microglial Cell Line.

    • Kota Sato, Yuto Sasaki, Michiko Ohno-Oishi, Kuniyuki Kano, Junken Aoki, Kosuke Ohsawa, Takayuki Doi, Hiroyuki Yamakoshi, Yoshiharu Iwabuchi, Chihiro Kawano, Yoshiyuki Hirata, and Toru Nakazawa.
    • Department of Ophthalmology, Tohoku University Graduate School of Medicine.
    • Tohoku J. Exp. Med. 2024 Jul 18; 263 (2): 151160151-160.

    AbstractActivated microglia contribute to many neuroinflammatory diseases in the central nervous system. In this study, we attempted to identify an anti-inflammatory compound that could suppress microglial activation. We performed high-throughput screening with a chemical library developed at our institute. We performed a luciferase assay of nuclear factor-kappa B (NF-κB) reporter stable HT22 cells and identified a compound that was confirmed to inhibit the anti-inflammatory response in BV2 microglial cells. The selected dihydropyridine derivative can suppress the expression response of interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor (TNF), as well as NF-κB phosphorylation and nuclear translocation, and reduce the intracellular calcium level. Thus, our identified compound has a potential role in suppressing microglial activation and may contribute to the development of a new therapeutic molecule against neuroinflammatory diseases.

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