Plasma Protein Binding of Herbal-Flavonoids to Human Serum Albumin and Their Anti-proliferative Activities

Abstract

Herbal-flavonoids (HF) as polyphenolic secondary metabolites are taken in the daily diet to join in many metabolic processes in the human organism. Anti-proliferative activities and human serum albumin (HSA) binding capacities of herbal-flavonoids namely 7,5'-dimethoxyisoetin (HF1), homoorientin-6 `'-4-O-methyl-myo-inositol (HF2), (2R, 3R)-(+)-dihydrokaempferol-7,4'-dimethylether (HF3), eriodictyol-7,4'-dimethylether (HF4) and flavonoids isoorientin (HF5) and genkwanin (HF6) were investigated. Anti-proliferative activities were determined by the xCELLigence system by treatment with human prostate (PC3) and cervical cancer (HeLa) cells. The binding capacities were studied by two-dimensional (2D-FL) and three-dimensional (3D-FL) fluorescence spectroscopy. HeLa and PC3 cell lines were treated with flavonoids at 10, 50 and 100 mu g/mL concentrations over a 48 hour period. Stable anti-proliferative efficacy plots were obtained for tested flavonoids. From the flavonoids, HF3 and HF4 showed the strongest anti-proliferative effect against PC3 and HeLa cell line. HF1 and HF2 exhibited the strongest binding capacity to the HSA corresponding to K-b values of 3.81 x 10(4) M-1 and 6.00 x 10(4) M-1, respectively. The studies revealed that the flavonoids form the basis of in vivo preclinical studies as important nutraceuticals of the daily diet, as well as modelled in medical and pharmacological applications.