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 μg/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 Kb values of 3.81 x 104 M-1 and 6.00 x 104 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.

Highlights

  • Flavonoids are bioactive secondary metabolites occurring in higherplants

  • The xCELLigence real-time graphs obtained in the treatment of HeLa and PC3 cells with the flavonoids cells are shown in the Figure 2a

  • The loss of cell index (LCI) of the compounds on concentration-dependent cell lines at 36 hours were statistically significant at p

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Summary

Introduction

Flavonoids are bioactive secondary metabolites occurring in higherplants They have broadspectrum pharmacological effects including anticancer, antioxidant, antimicrobial, anti-inflammatory, anti-allergic and immunosuppressive, as well as low systemic toxicity. Human serum albumin (HSA) is the most abundant carrier protein (about 46 mg/mL) in blood plasma (Basken & Green 2009, Callmann et al 2019). It is responsible for the transport of endogenous and exogenous substances such as fatty acids, amino acids, hormones, ions and medicines (Cui et al 2010, Naik et al 2010, Yaseen et al 2018, Pang et al 2019). Each domain is divided into two sub-domains of A and B, respectively (IA, IB, IIA, IIB, IIIA and IIIB)

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