Lab of Cardiovascular Pathophysiology, Dept of Cell Biology, University of Calabria, 87030 Arcavacata di Rende (CS), Italy.
Nutr Metab Cardiovasc Dis. 2011 May;21(5):362-71. doi: 10.1016/j.numecd.2009.10.011. Epub 2010 Jan 21.
Moderate red wine consumption associates with lower incidence of cardiovascular diseases. Attention to the source of this cardioprotection was focused on flavonoids, the non-alcoholic component of the red wine, whose intake inversely correlates with adverse cardiovascular events. We analysed whether two red wine flavonoids, quercetin and myricetin, affect mammalian basal myocardial and coronary function.
Quercetin and myricetin effects were evaluated on isolated and Langendorff perfused rat hearts under both basal conditions and α- and β-adrenergic stimulation. The intracellular signalling involved in the effects of these flavonoids was analysed on perfused hearts and by western blotting on cardiac and HUVEC extracts. Quercetin induced biphasic inotropic and lusitropic effects, positive at lower concentrations and negative at higher concentrations. Contrarily, Myricetin elicits coronary dilation, without affecting contractility and relaxation. Simultaneous administration of the two flavonoids only induced vasodilation. Quercetin-elicited positive inotropism and lusitropism depend on β1/β2-adrenergic receptors and associate with increased intracellular cAMP, while the negative inotropism and lusitropism observed at higher concentrations were α-adrenergic-dependent. NOS inhibition abolished Myricetin-elicited vasodilation, also inducing Akt, ERK1/2 and eNOS phosphorylation in both ventricles and HUVEC. Myricetin-dependent vasodilation increases intracellular cGMP and is abolished by triton X-100.
The cardiomodulation elicited on basal mechanical performance by quercetin and the selective vasodilation induced by myricetin point to these flavonoids as potent cardioactive principles, able to protect the heart in the presence of cardiovascular diseases.
适量饮用红酒与较低的心血管疾病发病率有关。人们关注这种心脏保护作用的来源主要集中在类黄酮上，类黄酮是红酒的非酒精成分，其摄入量与不良心血管事件呈负相关。我们分析了两种红酒类黄酮，槲皮素和杨梅素，是否会影响哺乳动物基础心肌和冠状动脉功能。
在基础条件以及α-和β-肾上腺素刺激下，我们评估了槲皮素和杨梅素对分离和 Langendorff 灌注大鼠心脏的影响。在灌注心脏和心脏和 HUVEC 提取物的 Western blot 分析中，研究了这些类黄酮作用涉及的细胞内信号。槲皮素诱导双相正性变力和变时作用，在较低浓度时为阳性，在较高浓度时为阴性。相反，杨梅素引起冠状血管扩张，不影响收缩力和舒张。同时给予两种类黄酮仅引起血管扩张。槲皮素诱导的正性变力和变时作用依赖于β1/β2-肾上腺素能受体，并与细胞内 cAMP 增加相关，而在较高浓度下观察到的负性变力和变时作用则依赖于α-肾上腺素能。NOS 抑制消除了杨梅素引起的血管扩张，同时还诱导了心室和 HUVEC 中的 Akt、ERK1/2 和 eNOS 磷酸化。杨梅素依赖性血管扩张增加细胞内 cGMP，并用 Triton X-100 消除。
槲皮素对基础机械性能产生的心脏调节作用以及杨梅素引起的选择性血管扩张表明这些类黄酮是有效的心脏活性物质，能够在存在心血管疾病的情况下保护心脏。
