Therapeutic effect of a novel curcumin derivative GT863 on a mouse model of amyotrophic lateral sclerosis

Hajime Kato, Hiroyasu Sato, Michiaki Okuda, Jun Wu, Shingo Koyama, Yasuhiko Izumi, Tomonori Waku, Mitsuyoshi Iino, Masashi Aoki, Shigeki Arawaka, Yasuyuki Ohta, Kenichi Ishizawa, Kanan Kawasaki, Yasuomi Urano, Tomohiro Miyasaka, Noriko Noguchi, Toshiaki Kume, Akinori Akaike, Hachiro Sugimoto & Takeo Kato
The present study investigated the therapeutic effects of the curcumin derivative 3-[(1E)-2-(1H-indol-6-yl)ethenyl]-5-[(1E)-2-[2-methoxy-4-(2-pyridylmethoxy)phenyl]ethenyl]-1H-pyrazole (GT863) in amyotrophic lateral sclerosis (ALS). The inhibitory effect of GT863 on superoxide dismutase 1 (SOD1) aggregation was evaluated in cell-free assays. GT863 interfered with the conformational changes of the SOD1 protein and later, oligomeric aggregation. Furthermore, its antioxidant, anti-inflammatory, and neuroprotective effects were evaluated in cell-free and cultured cell assays. GT863 inhibited H2O2− and glutamate-induced cytotoxicity and activated an antioxidant responsive element...
1 citation reported since publication in 2021.
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