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Identification of N-benzyltetrahydroisoquinolines as novel anti-neuroinflammatory agents
Authors:Brian Gabet  Ping-Chang Kuo  Steven Fuentes  Yamini Patel  Ahmed Adow  Mary Alsakka  Paula Avila  Teri Beam  Jui-Hung Yen  Dennis A Brown
Institution:1. Manchester University College of Pharmacy and Health Sciences, 10627 Diebold Rd, Fort Wayne, IN 46845, United States;2. Department of Microbiology and Immunology, Indiana University School of Medicine, 2101 E. Coliseum Blvd, Fort Wayne, IN 46805, United States
Abstract:A series of simplified berberine analogs was designed, synthesized, and evaluated for anti-inflammatory activity. SAR studies identified N-benzyltetrahydroisoquinoline 7d as a potent berberine analog. 7d suppressed LPS-induced inflammatory cytokine levels in both BV2 cells and primary microglia. Taken together, our results suggest that simplified BB analogs have therapeutic potential as a novel class of anti-neuroinflammatory agents.
Keywords:BB  berberine  CNS  central nervous system  EAE  experimental autoimmune encephalomyelitis  LPS  lipopolysaccharide  MS  multiple sclerosis  Berberine  Neuroinflammation  Multiple sclerosis
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