Abstract
Derivatives based on a benzotropolone skeleton (9-26) have been prepared by the enzymatic coupling (horseradish peroxidase/H2O2) of selected pairs of compounds (1-8), one with a vic-trihydroxyphenyl moiety, and the other with an ortho-dihydroxyphenyl structure. Some of these compounds have been found to inhibit TPA-induced mice ear edema, nitric oxide (NO) synthesis, and arachidonic acid release by LPS-stimulated RAW 264.7 cells. Their cytotoxic activities against KYSE 150 and 510 human esophageal squamous cell carcinoma and HT 29 human colon cancer cells were also evaluated.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
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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Arachidonic Acid / metabolism
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Biflavonoids / chemistry*
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Biochemistry / methods
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Carcinoma, Squamous Cell / drug therapy
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Catechin / chemistry*
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Cell Division / drug effects
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Cells, Cultured
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Colonic Neoplasms / drug therapy
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Drug Evaluation, Preclinical / methods
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Ear Diseases / chemically induced
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Ear Diseases / drug therapy
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Edema / chemically induced
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Edema / drug therapy
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Esophageal Neoplasms / drug therapy
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Female
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Horseradish Peroxidase / chemistry
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Horseradish Peroxidase / metabolism
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Humans
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Macrophages / drug effects
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Macrophages / metabolism
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Mice
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Mice, Inbred Strains
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Structure-Activity Relationship
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Tea / chemistry
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Tetradecanoylphorbol Acetate / toxicity
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Toxicity Tests
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Tumor Cells, Cultured
Substances
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Anti-Inflammatory Agents
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Biflavonoids
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Tea
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theaflavin
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Arachidonic Acid
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Catechin
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Horseradish Peroxidase
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Tetradecanoylphorbol Acetate