Potential Implications of Quercetin and its Derivatives in Cardioprotection

Abstract

Quercetin (QCT) is a natural polyphenolic compound enriched in human food, mainly in vegetables, fruits and berries. QCT and its main derivatives, such as rhamnetin, rutin, hyperoside, etc., have been documented to possess many beneficial effects in the human body including their positive effects in the cardiovascular system. However, clinical implications of QCT and its derivatives are still rare. In the current paper we provide a complex picture of the most recent knowledge on the effects of QCT and its derivatives in different types of cardiac injury, mainly in ischemia-reperfusion (I/R) injury of the heart, but also in other pathologies such as anthracycline-induced cardiotoxicity or oxidative stress-induced cardiac injury, documented in in vitro and ex vivo, as well as in in vivo experimental models of cardiac injury. Moreover, we focus on cardiac effects of QCT in presence of metabolic comorbidities in addition to cardiovascular disease (CVD). Finally, we provide a short summary of clinical studies focused on cardiac effects of QCT. In general, it seems that QCT and its metabolites exert strong cardioprotective effects in a wide range of experimental models of cardiac injury, likely via their antioxidant, anti-inflammatory and molecular pathways-modulating properties; however, ageing and presence of lifestyle-related comorbidities may confound their beneficial effects in heart disease. On the other hand, due to very limited number of clinical trials focused on cardiac effects of QCT and its derivatives, clinical data are inconclusive. Thus, additional well-designed human studies including a high enough number of patients testing different concentrations of QCT are needed to reveal real therapeutic potential of QCT in CVD. Finally, several negative or controversial effects of QCT in the heart have been reported, and this should be also taken into consideration in QCT-based approaches aimed to treat CVD in humans.

Synergistic Protection by Isoquercitrin and Quercetin against Glutamate-Induced Oxidative Cell Death in HT22 Cells via Activating Nrf2 and HO-1 Signaling Pathway: Neuroprotective Principles and Mechanisms of Dendropanax morbifera Leaves

“…Both Caco-2 cells treated with isoquercitrin alone accumulated both quercetin and isoquercitrin within an hour, suggesting that isoquercitrin is readily metabolized to quercetin by cellular glucosidases [ 57 ]. Dietary flavonoids undergo diverse metabolism in the intestinal tract by enzymes such as lactase-phlorizin hydrolase and cytosolic glucosidases as well as microbiota [ 52 , 53 , 59 ]. This metabolic transformation may influence the absorption and bioavailability of individual quercetin derivatives in a more intensive and complicated manner, in plant extracts composed of diverse flavonoids [ 52 , 57 ].…”

Composition and Antioxidant Activity of Phenolic Compounds in Fruit of the Genus Rosa L.

“…These compounds are important for human health because of their strong antioxidant and anticancer activities [ 54 , 55 , 56 ]. The consumption of products rich in quercetin and its glycosides reduces the risk of cardiovascular [ 57 , 58 ] and neurodegenerative diseases [ 59 , 60 ].…”

A Study on the Mechanism of Milkvetch Root in the Treatment of Diabetic Nephropathy Based on Network Pharmacology

“…Quercetin, a flavonoid, is a potent antioxidant found in common medicinal herbs and possesses a wide spectrum of biologic activities [ 36 ]. It also has antioxidant, hypoglycemic, hypolipidemic, tumor suppression, and anti-inflammatory effects [ 37 , 38 ]. One study showed that quercetin liposome or free quercetin could prevent weight loss, decrease kidney hypertrophy index, decrease blood glucose level, and decrease 24-hour urine protein levels in diabetic nephropathy model rats [ 39 ].…”