These data suggest that isorhamnetin and quercetin 3-O-glucoside may be the active forms of quercetin in prevention of bladder cancer.

– GreenMedInfo Summary

Abstract Title:

Metabolism and growth inhibitory activity of cranberry derived flavonoids in bladder cancer cells.

Abstract Source:

Food Funct. 2016 Sep 14 ;7(9):4012-4019. PMID: 27711848

Abstract Author(s):

Jeevan K Prasain, Rajani Rajbhandari, Adam B Keeton, Gary A Piazza, Stephen Barnes

Article Affiliation:

Jeevan K Prasain

Abstract:

In the present study, anti-proliferative activities of cranberry derived flavonoids and some of their in vivo metabolites were evaluated using a panel of human bladder tumor cell lines (RT4, SCABER, and SW-780) and non-tumorigenic immortalized human uroepithelial cells (SV-HUC). Among the compounds tested, quercetin 3-O-glucoside, isorhamnetin (3′-O-methylquercetin), myricetin and quercetin showed strong concentration-dependent cell growth inhibitory activities in bladder cancer cells with IC50 values in a range of 8-92μM. Furthermore, isorhamnetin and myricetin had very low inhibitory activity against SV-HUC even at very high concentrations (>200μM) compared to bladder cancer cells, indicating that their cytotoxicity is selective for cancer cells. To determine whether the differential cell growth inhibitory effects of isomeric flavonoids quercetin 3-O-glucoside (active) and hyperoside (quercetin 3-O-galactoside) (inactive) are related to their metabolism by the cancer cells, SW-780 cells were incubated with these compounds and their metabolism was examined by LC-MS/MS. Compared to quercetin 3-O-glucoside, hyperoside undergoes relatively less metabolic biotransformation (methylation, glucuronidation and quinone formation). These datasuggest that isorhamnetin and quercetin 3-O-glucoside may be the active forms of quercetin in prevention of bladder cancer in vivo and emphasize the importance of metabolism for the prevention of bladder cancer by diets rich in cranberries.

Academic Cite:

Jeevan K Prasain, Rajani Rajbhandari, Adam B Keeton, Gary A Piazza, Stephen Barnes. Metabolism and growth inhibitory activity of cranberry derived flavonoids in bladder cancer cells. Food Funct. 2016 Sep 14 ;7(9):4012-4019.

Pubmed-Cite:

Jeevan K Prasain, Rajani Rajbhandari, Adam B Keeton, Gary A Piazza, Stephen Barnes. Metabolism and growth inhibitory activity of cranberry derived flavonoids in bladder cancer cells. Food Funct. 2016 Sep 14 ;7(9):4012-4019. PMID: 27711848

GMI-Cite:

Jeevan K Prasain, Rajani Rajbhandari, Adam B Keeton, Gary A Piazza, Stephen Barnes. Metabolism and growth inhibitory activity of cranberry derived flavonoids in bladder cancer cells. Food Funct. 2016 Sep 14 ;7(9):4012-4019. PMID: 27711848

Article Published Date : Sep 13, 2016

Study Type : In Vitro Study

Additional Links

Substances : Cranberry : CK(349) : AC(69)

Diseases : Bladder Cancer : CK(349) : AC(100)

Pharmacological Actions : Chemopreventive : CK(2835) : AC(787), Cytotoxic : CK(76) : AC(60)

Additional Keywords : Selective Cytotoxicity : CK(158) : AC(112)