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:
Berberine; Multiple sclerosis; Neuroinflammation.
Copyright © 2018 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents / chemical synthesis
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology*
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Cell Line, Transformed
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Cytokines / metabolism
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Inflammation / chemically induced
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Lipopolysaccharides
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Mice
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Microglia / drug effects
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Molecular Conformation
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Neuroprotective Agents / chemical synthesis
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Neuroprotective Agents / chemistry
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Neuroprotective Agents / pharmacology*
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Structure-Activity Relationship
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Tetrahydroisoquinolines / chemical synthesis
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Tetrahydroisoquinolines / chemistry
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Tetrahydroisoquinolines / pharmacology*
Substances
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Anti-Inflammatory Agents
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Cytokines
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Lipopolysaccharides
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Neuroprotective Agents
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Tetrahydroisoquinolines