Synthesis and biological activity of the tea catechin metabolites, M4 and M6 and their methoxy-derivatives

Joshua D. Lambert, Joseph E. Rice, Jungil Hong, Zhe Hou, Chung S. Yang

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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 μM.

Original languageEnglish (US)
Pages (from-to)873-876
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number4
DOIs
StatePublished - Feb 15 2005

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All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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