Quercetin and green tea extract supplementation downregulates genes related to tissue inflammatory responses to a 12-week high fat-diet in mice

10.3390/nu9070773Nutrients9777

Modeling the Effect of Phase II Conjugations on Topoisomerase I Poisoning: Pilot Study with Luteolin and Quercetin

Estrogen Receptors (ERs) are ligand-dependent intracellular transcriptional factors involved in many diseases. ERs mediate many of the effects of estrogens, but also exogenous compounds are able to interfere with ER, disrupting endocrine signaling. Among these xenobiotics, compounds present in food and feed make ERs a relevant target in the context of dietary modulation of health. In this sense, urolithins, gut microbiota derived metabolites of plant polyphenolic ellagitannins, may represent good candidates to act as phytoestrogens that are able to modulate the activity of ERs. An in silico method to qualitatively evaluate the potential xenoestrogenic agonistic behavior of ellagitannin-derived metabolites is proposed. The "full-dry" in silico approach involved structure based virtual screening (SBVS), docking simulations and re-scoring procedures. Results provided valuable insights about the phase II conjugations (glucuronidation, sulfation, and methylation, occurring in vivo) affecting the estrogenicity of these compounds on α- and β-ER isoforms. Hydroxylation patterns also revealed a significant role in the agonistic behavior of urolithin derivatives. On the whole, ellagitannin-derived metabolites exerted different predicted xenoestrogenic activity depending on chemical structures, and the applied in silico approach may represent a successful and easy choice to analyze enormous datasets of food-related compounds in order to understand their potential biological features

The Efficacy of Quercetin in Cardiovascular Health

Cardiovascular disease is a major cause of death worldwide despite the majority of its risk factors being preventable and treatable. The results of numerous epidemiological studies suggest that a diet rich in fruits and vegetables affords protection against CVD, and this may be attributed, in part, to the flavonoid quercetin. The aims of this review are to summarise the current knowledge on the bioavailability and metabolism of quercetin as well as discuss the current evidence behind the potential mechanisms by which quercetin exerts its cardioprotective effects. This review summarises key human studies administering quercetin that have been published to date. Although interesting results have been seen in animal and cell culture studies, in general, these have not been replicated in human trials. Several studies have, however, shown that quercetin can reduce blood pressure in hypertensive patients. The exact mechanisms are yet to be elucidated. Further studies are required to investigate the use of quercetin as a cardioprotective treatment, in particular long-term and dose–response studies