Abstract
Various natural and synthetic compounds including alkaloids, terpenoids and phenolics were tested for inhibition of the cell surface expression of intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1), both of which are crucial in the regulation of immune response and inflammation. Of 40 compounds tested, two compounds significantly downregulated the expression of VCAM-1 on murine endothelial cells (F-2) and ten compounds that of ICAM-1 on mouse myeloid leukemia cells (M1). Sanguinarine chloride (5) and isoliquiritigenin (13) were capable of lowering the levels of both ICAM-1 and VCAM-1. The structure-activity relationships study on chalcone and flavone derivatives related to 13 suggested that the inhibitory activity of the chalcone derivatives is attributable to the 4-hydroxy group as well as the possible coplanarity between the phenyl ring and the adjacent conjugated ketone.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkaloids / isolation & purification
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Alkaloids / pharmacology*
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / isolation & purification
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Benzophenanthridines
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Chalcone / analogs & derivatives*
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Chalcone / isolation & purification
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Chalcone / pharmacology*
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Chalcones
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Intercellular Adhesion Molecule-1 / drug effects*
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Isoquinolines
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Mice
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Mice, Inbred Strains
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Molecular Structure
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Phenols / isolation & purification
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Phenols / pharmacology
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Plants, Medicinal / chemistry*
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Structure-Activity Relationship
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Terpenes / isolation & purification
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Terpenes / pharmacology
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Tumor Cells, Cultured / drug effects
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Vascular Cell Adhesion Molecule-1 / drug effects*
Substances
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Alkaloids
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Anti-Inflammatory Agents, Non-Steroidal
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Benzophenanthridines
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Chalcones
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Isoquinolines
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Phenols
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Terpenes
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Vascular Cell Adhesion Molecule-1
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Intercellular Adhesion Molecule-1
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Chalcone
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sanguinarine
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isoliquiritigenin