Total Phenolic and Flavonoid Content and Biological Activities of Extracts and Isolated Compounds of Cytisus villosus Pourr.

Francisco León,Farida Larit,Samira Benyahia,Stephen Cutler

doi:10.3390/biom9110732

Abstract

The aim of this study was to evaluate the total phenolic and flavonoid content, and the in vitro antioxidant, anti-inflammatory, antibacterial, antifungal, antimalarial, cytotoxicity, and antiprotozoal activities of the Algerian plant Cytisus villosus Pourr. (Syn. Cytisus triflorus L’Hérit.). Additionally, the radioligand displacement affinity on opioid and cannabinoid receptors was assessed for the extracts and isolated pure compounds. The hydro alcoholic extract of the aerial part of C. villosus was partitioned with chloroform (CHCl3), ethyl acetate (EtOAc), and n-butanol (n-BuOH). The phenolic content of the C. villosus extracts was evaluated using a modified Folin–Ciocalteau method. The total flavonoid content was measured spectrometrically using the aluminum chloride colorimetric assay. The known flavonoids genistein (1), chrysin (2), chrysin-7-O-β-d-glucopyranoside (3), and 2″-O-α-l-rhamnosylorientin (4) were isolated. The antioxidant activities of the extracts and isolated compounds were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DDPH) and cellular antioxidant activity (CAA) assays. The plant extracts showed moderate antioxidant activity. EtOAc and n-BuOH extracts showed moderate anti-inflammatory activity through the inhibition of induced nitric oxide synthase (iNOS) with IC50 values of 48 and 90 µg/mL, respectively. The isolated pure compounds 1 and 3 showed good inhibition of Inducible nitric oxide synthase (iNOS) with IC50 values of 9 and 20 µg/mL, respectively. Compounds 1 and 2 exhibited lower inhibition of Nuclear Factor kappa-light-chain-enhancer of activated B cells (NF-κB) with IC50 values of 28 and 38 µg/mL, respectively. Furthermore, the extracts and isolated pure compounds have been shown to exhibit low affinity for cannabinoid and opioid receptors. Finally, n-BuOH extract was a potent inhibitor of Trypanosoma brucei with IC50 value of 7.99 µg/mL and IC90 value of 12.61 µg/mL. The extracts and isolated compounds showed no antimicrobial, antimalarial nor antileishmanial activities. No cytotoxic effect was observed on cancer cell lines. The results highlight this species as a promising source of anti-inflammatory and antitrypanosomal agents.

Highlights

Natural compounds derived from plants have played an important role from ancient to recent times in the management and treatment of many maladies with wide effects, such as antioxidants associated with reduced risks of cancer, cardiovascular disease, diabetes, infectious diseases, and other disorders associated with age [1]
Phytochemical study of the hydro ethanolic extract of the aerial part of C. villosus led to the Phytochemical study of the hydro ethanolic extract of the aerial part of C. villosus led to the isolation of four known flavonoids (1) genistein, (2) chrysin, (3) chrysin-7-O-β-D-glucopyranoside, isolation of four known flavonoids (1) genistein, (2) chrysin, (3) chrysin-7-O-β-d-glucopyranoside, and (4) 2"-O-α-L-rhamnosylorientin (Figure 1)
The structures of the known compounds were identified by comparison of their spectroscopic data with those reported in the literature [33]

Summary

Introduction

Natural compounds derived from plants have played an important role from ancient to recent times in the management and treatment of many maladies with wide effects, such as antioxidants associated with reduced risks of cancer, cardiovascular disease, diabetes, infectious diseases, and other disorders associated with age [1]. The high antioxidant activity of polyphenols is mainly due to their redox properties, which allow them to act as reducing agents, hydrogen donors, and singlet oxygen quenchers. In this context, oxidative stress plays an important role in the progression of neurodegenerative conditions, including rheumatic and cardiovascular disorders, metabolic syndrome, and other diseases [4]. Inflammation is considered to be a risk factor for hypertension, diabetes, and several types of cancer, and can be involved in Alzheimer’s disease pathogenesis

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