Anti-Inflammatory and Proliferative Properties of Luteolin-7-O-Glucoside.

Alessandro De Stefano,Massimo Pieri,Manfredi Tesauro,Alessandro Terrinoni,Carmine Cardillo,Sabrina Caporali,Marilena Minieri,Valentina Rovella,Sergio Bernardini,Francesca Schinzari,Eleonora Candi,Nicola Di Daniele

doi:10.3390/ijms22031321

Abstract

Flavonoids display a broad range of structures and are responsible for the major organoleptic characteristics of plant-derived foods and beverages. Recent data showed their activity, and in particular of luteolin-7-O-glucoside (LUT-7G), in reduction of oxidative stress and inflammatory mechanisms in different physiological systems. In this paper, we tried to elucidate how LUT-7G could exert both antioxidant and anti-inflammatory effects in endothelial cells cultured in vitro. Here, we showed that LUT-7G is able to inhibit the STAT3 pathway, to have an antiproliferative action, and an important antioxidant property in HUVEC cells. These properties are exerted by the flavone in endothelial through the transcriptional repression of a number of inflammatory cytokines and their receptors, and by the inhibition of ROS generation. ROS and STAT3 activation has been correlated with the production of oxysterols and other hydroxylated fatty acids, and they have been recognized important as players of atherogenesis and cardiocirculatory system diseases. The analysis of the general production pathway of these hydroxylated species, showed a strong decrease of cholesterol hydroxylated species such as 7-alpha-hydroxicholesterol, 7-beta-hydroxicholesterol by the treatment with LUT-7G. This confirms the anti-inflammatory properties of LUT-7G also in the endothelial district, showing for the first time the molecular pathway that verify previous postulated cardiovascular benefits of this flavone.

Highlights

The antioxidant activity of luteolin olin inhibits inflammatory responses induced by lipopolysaccharide (LPS) [10], tumour and its glycosidesnecrosis have been evaluated
IL-6 in a dose-dependent luteolin inhibits inflammatory responses induced by lipopolysaccharide (LPS)and
[10],induced tumourepithelialParticularly, STAT3 has been correlated to MMP secretion necrosis factor-α (TNF-α), andtransition

Summary

Introduction

An increasing number of plant-derived molecules, such as flavonoids, which are a class of plant secondary metabolites have shown positive effects on several conditions such as cardiovascular and immunological diseases and in cancer [1,2]. They display a large range of structures and, they are responsible for the major organoleptic characteristics of plant-derived foods and beverages, color and taste properties and they contribute to the nutritional qualities of fruits and vegetables [3]. Recent developments in the understanding of oxidative stress and inflammatory mechanisms of the cardiovascular system tried to elucidate how flavonoids exert beneficial cardiovascular effects because the understanding of oxidative stress and inflammatory mechanisms the cardiovascular of their anti-oxidant and anti-inflammatory properties, coupledof with their capacity to system tried to cellular elucidate how flavonoids exert beneficial cardiovascular effects because modulate key function [4,5]

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