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

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 4, 2005, Pages 873-876

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

^a RUTGERS UNIVERSITY   (United States)

Author keywords

Antiinflammatory; Green tea; Growth inhibition; Lactones; Synthesis

Indexed keywords

ARACHIDONIC ACID; CATECHIN; DRUG METABOLITE; EPICATECHIN; EPIGALLOCATECHIN; GALLIC ACID DERIVATIVE;

ANTIINFLAMMATORY ACTIVITY; ARTICLE; CELL GROWTH; CELL IMMORTALIZATION; CONTROLLED STUDY; DRUG SCREENING; DRUG SYNTHESIS; HUMAN; HUMAN CELL;

EID: 16244391107     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.12.070     Document Type: Article

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12. 13C NMR δ 177.0, 153.4, 131.7, 106.8, 80.7, 60.9, 56.3, 41.7, 28.7, 27.2
13. 3 cells per well) and allowed to attach overnight. The medium was replaced with serum-free medium containing the test compounds (0-50 μM). Cells were incubated for 24 h at 37°C. The compound-containing medium was removed, fresh serum-complete medium was added, and the cells were incubated for an additional 24 h. Growth inhibition was determined using 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide (MTT). Cell growth is correlated with mitochondria-mediated reduction of MTT to a purple formazan precipitate. Growth of treated cells was compared to the growth of the untreated controls to determine percent growth inhibition
14. 3H](N) arachidonic acid (NEN Life Science, Boston, MA, USA). The cells were incubated overnight to allow absorption of the labeled arachidonic acid, washed twice with PBS containing 0.1% BSA, and stimulated for 1 h with 2 μg/mL lipopolysaccharide (LPS). The medium was replaced with new, serum-free medium containing test compounds (20 μM) and the cells were incubated for an additional 18 h at 37°C. After incubation, the medium was collected, centrifuged at 12,000 rpm for 10 min and radioactivity in the extracellular fluid was measured with a scintillation counter
15. 5 cells per well) for 1 h with 2 μg/mL LPS. The medium was then replaced with serum-free medium containing the test compounds (20 μM) and cells were cultured for 18 h. NO production was determined spectrophotometrically using previously-reported methods