Kampa Rafał P, Sęk Aleksandra, Bednarczyk Piotr, Szewczyk Adam, Calderone Vincenzo, Testai Lara
Laboratory of Intracellular Ion Channels, Nencki Institute of Experimental Biology PAS, Warsaw, Poland.
Department of Pharmacy, University of Pisa, Italy.
J Pharm Pharmacol. 2023 Apr 7;75(4):466-481. doi: 10.1093/jpp/rgac093.
Acute myocardial ischemia is one of the major causes of illness in western society. Reduced coronary blood supply leads to cell death and loss of cardiomyocyte population, resulting in serious and often irreversible consequences on myocardial function. Mitochondrial potassium (mitoK) channels have been identified as fine regulators of mitochondrial function and, consequently, in the metabolism of the whole cell, and in the mechanisms underlying the cardioprotection. Interestingly, mitoK channels represent a novel putative target for treating cardiovascular diseases, particularly myocardial infarction, and their modulators represent an interesting tool for pharmacological intervention. In this review, we took up the challenge of selecting flavonoids that show cardioprotective properties through the activation of mitoK channels.
A brief overview of the main information on mitoK channels and their participation in the induction of cytoprotective processes was provided. Then, naringenin, quercetin, morin, theaflavin, baicalein, epigallocatechin gallate, genistein, puerarin, luteolin and proanthocyanidins demonstrated to be effective modulators of mitoK channels activity, mediating many beneficial effects.
The pathophysiological role of mitoK channels has been investigated as well as the impact of flavonoids on this target with particular attention to their potential role in the prevention of cardiovascular disorders.
急性心肌缺血是西方社会主要的致病原因之一。冠状动脉供血减少会导致细胞死亡和心肌细胞数量丧失，从而对心肌功能产生严重且往往不可逆的后果。线粒体钾（mitoK）通道已被确定为线粒体功能的精细调节因子，因此也参与整个细胞的代谢以及心脏保护的潜在机制。有趣的是，mitoK通道是治疗心血管疾病，尤其是心肌梗死的一种新的假定靶点，其调节剂是药物干预的一个有趣工具。在本综述中，我们接受了一项挑战，即筛选出通过激活mitoK通道而具有心脏保护特性的黄酮类化合物。
简要概述了mitoK通道的主要信息及其在诱导细胞保护过程中的作用。然后，柚皮素、槲皮素、桑色素、茶黄素、黄芩素、表没食子儿茶素没食子酸酯、染料木黄酮、葛根素、木犀草素和原花青素被证明是mitoK通道活性的有效调节剂，介导了许多有益作用。
研究了mitoK通道的病理生理作用以及黄酮类化合物对该靶点的影响，特别关注它们在预防心血管疾病中的潜在作用。
