Inhibition of proliferation of human cancer cells and cyclooxygenase enzymes by anthocyanidins and catechins

The widespread consumption of diets rich in anthocyanin and catechin content prompted the evaluation of their in vitro inhibitory effects on cyclooxygenase (COX) enzymes and on the proliferation of human cancer cell lines. Five anthocyanidins consisting of cyanidin (1), delphinidin (2), pelargonidin (3), peonidin (4), and malvidin (5) were tested for COX-1 and -2 enzyme inhibitory activities at 40 muM. Eleven catechins consisting of (+)-catechin (6), (-)-catechin (7), (+/-)-catechin (8), (+)-epicatechin (9), (-)-epicatechin (10), (-)-epigallocatechin (11), (-)-gallocatechin (12), (-)-epicatechin gallate (13), (-)-catechin gallate (14), (-)-epigallocatechin gallate (15), and (-)-gallocatechin gallate (16) were tested for inhibitory effects of COX-1 and -2 enzymes at 80 muM. Of the compounds tested, the galloyl derivatives of the catechins 11-15, cyanidin (1) and malvidin (5), showed the best COX inhibitory activities compared with the commercial anti-inflammatory drugs ibuprofen (at 10 muM), naproxen (at 10 muM), Vioxx(R) (at 1.67 ppm), and Celebrex(TM) (at 1.67 ppm). Inhibition of the proliferation of the human cancer cell lines MCF-7 (breast), SF-268 (central nervous system, CNS), HCT-116 (colon), and NCI-H460 (lung) was evaluated at concentrations between 100 and 6.25 muM compared with the commercial standard, adriamycin (doxorubicin) at 6.25 muM At 100-muM concentrations, anthocyanidins 1-5 and catechins 6-10 did not inhibit proliferation of the four cell lines. At 50-muM concentrations, catechins 12, 15, and 16 showed 95%, 100%, and 97% inhibition of breast cells, respectively. At 50-muM concentrations 12 and 16 were the most effective catechins against colon cells (85% and 93%, respectively) and lung cells (87% and 67%, respectively). CNS cells were the most sensitive of the test cell lines, and total growth inhibition was obtained with catechins 12 and 16 at 100-muM concentrations. Overall, only the galloyl derivatives of catechins 11-16 inhibited the Proliferation of the cancer cell lines.