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

Abstract

Herbal-fl avonoids (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-fl avonoids 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 fl avonoids isoorientin (HF5) and genkwanin (HF6) were investigated. Antiproliferative 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) fl uorescence spectroscopy. HeLa and PC3 cell lines were treated with fl avonoids at 10, 50 and 100 μg/mL concentrations over a 48 hour period. Stable anti-proliferative effi cacy plots were obtained for tested fl avonoids. From the fl avonoids, 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 fl avonoids form the basis of in vivo preclinical studies as important nutraceuticals of the daily diet, as well as modelled in medical and pharmacological applications.

Allergens and their associated small molecule ligands—their dual role in sensitization

“…For example, SAs bind steroid hormones, saturated and unsaturated fatty acids, thyroxine, vitamin D, and flavonoid metabolites, as well as many exogenous compounds like drugs (Table 1). [37][38][39]43,[49][50][51] It was also shown that small-molecule compounds like carbohydrates may bind SAs through the amino groups of lysine residues that are located on the surface of these proteins. 49,52 It was shown that derivatives of carbohydrates, such as the food additive D-mannitol, can form stable covalent derivatives with SAs, leading to the haptenization of these proteins.…”

Flavonoids-Macromolecules Interactions in Human Diseases with Focus on Alzheimer, Atherosclerosis and Cancer

“…Several studies have been performed to characterize the interactions between dietary flavonoids and proteins, mainly serum and food-related proteins, for example, serum albumins and β-casein [ 26 , 27 , 28 , 29 , 30 ]. Flavonoid–protein interactions mainly occur by noncovalent bonding that is derived from hydrophobic, van der Waals, hydrogen bridge-binding, and ionic interactions, which can change protein conformations and enzyme activities [ 31 ].…”

EVALUATION OF THE PHYTOCHEMICAL PROPERTIES AND DNA PROTECTIVE ACTIVITY OF BOLANTHUS ORTEGIOIDES (FISCH. and C.A. MEY.) MADHANI and RABELER

“…The present study provides the first data obtained from a HPLC analysis of phenolics in B. ortegioides methanolic extract. Some previous studies have described flavonoids (Geçibesler and Aydın, 2020), lipophilic fractions (Geçibesler et al, 2016), triterpene saponins (Horo et al, 2015) and essential oil compositions (Kiliç et al, 2013) of B. ortegioides. It is emphasized that HPLC data of phenolics of the genus Bolanthus is not available in the current literature (Özbek Yazici and Özmen, 2017).…”