Abstract
Syntheses are reported for metabolites M4 (1) and M6 (2) of the green tea polyphenols epicatechin (EC) and epigallocatechin (EGC) and their gallate derivatives. Several methoxy-derivatives of 1 and 2 were also prepared. Compounds 1 and 2 were evaluated for growth inhibitory activity against a panel of immortalized and malignant human cell lines with 1 being the more active compound. The possible antiinflammatory activity of 1 and its trimethoxy derivative was also evaluated. Neither compound inhibited the release of arachidonic acid, although 1 inhibited NO production by 50% at 20 microM.
Publication types
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Research Support, N.I.H., Extramural
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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 / chemistry*
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Anti-Inflammatory Agents / pharmacology
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology
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Arachidonic Acid / metabolism
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Catechin / analogs & derivatives*
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Catechin / metabolism
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Catechin / pharmacology
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Cell Line
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Humans
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Lipopolysaccharides / pharmacology
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Macrophages / drug effects
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Mice
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Nitric Oxide / biosynthesis
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Structure-Activity Relationship
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Tea / chemistry
Substances
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Anti-Inflammatory Agents
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Antineoplastic Agents
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Lipopolysaccharides
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Tea
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Arachidonic Acid
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Nitric Oxide
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Catechin