Cardiovascular Ion Channels as a Molecular Target of Flavonoids

Abstract

SUMMARYFlavonoids are a class of naturally occurring polyphenols abundant in edibles and beverages of plant origin. Epidemiological studies consistently associate high flavonoid intake with a reduced risk for the development of cardiovascular diseases. So far these beneficial effects have been mainly attributed to nonspecific antioxidant and antiinflammatory properties. However, there is an increasing body of evidence that flavonoids specifically target molecular structures including cardiovascular ion channels. Playing a pivotal role in the regulation of vascular tone and cardiac electric activity, ion channels represent a major target for the induction of antihypertensive and cardioprotective effects. Thus, pharmacological properties of flavonoids on cardiovascular ion channels, ion currents and tissue preparations are being increasingly addressed in experimental studies. Whereas it has become clear that cardiovascular ion channels represent an important molecular target of flavonoids, the published data have not yet been systematically reviewed.

Polyphenol compounds and PKC signaling

“…In most of these instances, the antioxidant property of polyphenols is suggested as being responsible for their observed beneficial effects. Despite the predominant focus on the antioxidant activities, polyphenols have also been implicated in other roles independent of their antioxidant property like antibacterial [26, 27], anti-inflammatory [28] and modulation of ion transport [29]. …”

Effects of coadministration of natural polyphenols with doxycycline or calcium modulators on acute Chlamydia pneumoniae infection in vitro

“…17,18 Phenolic compounds have been associated with a wide range of biological activities; among others, they have been shown to affect Ca 2+ channel regulation in mammalian cells at physiological concentrations. As reviewed by Scholz et al, 19 the type and strength of the effect depends highly on the compound concentration and on the cell and channel type. In our earlier work with rat pituitary GH 4 C 1 cells expressing L-type Ca 2+ channels, luteolin and octyl gallate inhibited the uptake of Ca 2+ from extracellular media, whereas quercetin increased the uptake, and rhamnetin showed no effect on the Ca 2+ ion uptake at a concentration of 20 mg ml À1 (63-71 mM).…”

CZE/PAD and HPLC-UV/PAD Profile of Flavonoids from Maytenus aquifolium and Maytenus ilicifolia “espinheira santa” Leaves Extracts

“…Many flavonoids found in plants have biological and pharmacological activities, such as antimicrobial, antiinflammatory, and antiallergic action [4][5][6][7]. The antioxidant property of these substances has also been established and correlated to their protective effects on cardiovascular disease and some forms of cancer [8][9][10].…”