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槲皮素在心血管疾病中的潜在药物应用。

Potential Pharmaceutical Applications of Quercetin in Cardiovascular Diseases.

作者信息

Papakyriakopoulou Paraskevi, Velidakis Nikolaos, Khattab Elina, Valsami Georgia, Korakianitis Ioannis, Kadoglou Nikolaos Pe

机构信息

Laboratory of Biopharmaceutics-Pharmacokinetics, Department of Pharmacy, School of Health Sciences, National & Kapodistrian University of Athens, 15784 Athens, Greece.

Medical School, University of Cyprus, Nicosia 2029, Cyprus.

出版信息

Pharmaceuticals (Basel). 2022 Aug 18;15(8):1019. doi: 10.3390/ph15081019.

Abstract

Quercetin, as a member of flavonoids, has emerged as a potential therapeutic agent in cardiovascular diseases (CVDs) in recent decades. In this comprehensive literature review, our goal was a critical appraisal of the pathophysiological mechanisms of quercetin in relation to the classical cardiovascular risk factors (e.g., hyperlipidemia), atherosclerosis, etc. We also assessed experimental and clinical data about its potential application in CVDs. Experimental studies including both in vitro methods and in vivo animal models mainly outline the following effects of quercetin: (1) antihypertensive, (2) hypolipidemic, (3) hypoglycemic, (4) anti-atherosclerotic, and (5) cardioprotective (suppressed cardiotoxicity). From the clinical point of view, there are human studies and meta-analyses implicating its beneficial effects on glycemic and lipid parameters. In contrast, other human studies failed to demonstrate consistent favorable effects of quercetin on other cardiometabolic risk factors such as MS, obesity, and hypertension, underlying the need for further investigation. Analyzing the reason of this inconsistency, we identified significant drawbacks in the clinical trials' design, while the absence of pharmacokinetic/pharmacodynamic tests prior to the studies attenuated the power of clinical results. Therefore, additional well-designed preclinical and clinical studies are required to examine the therapeutic mechanisms and clinical efficacy of quercetin in CVDs.

摘要

槲皮素作为黄酮类化合物的一员,在近几十年已成为心血管疾病(CVD)的一种潜在治疗药物。在这篇全面的文献综述中,我们的目标是对槲皮素与经典心血管危险因素(如高脂血症)、动脉粥样硬化等相关的病理生理机制进行批判性评估。我们还评估了其在心血管疾病中潜在应用的实验和临床数据。包括体外方法和体内动物模型的实验研究主要概述了槲皮素的以下作用:(1)降压,(2)降血脂,(3)降血糖,(4)抗动脉粥样硬化,以及(5)心脏保护(抑制心脏毒性)。从临床角度来看,有人类研究和荟萃分析表明其对血糖和血脂参数有有益作用。相比之下,其他人类研究未能证明槲皮素对其他心脏代谢危险因素如代谢综合征、肥胖和高血压有一致的有利作用,这表明需要进一步研究。分析这种不一致的原因,我们发现临床试验设计存在重大缺陷,而研究前缺乏药代动力学/药效学测试削弱了临床结果的说服力。因此,需要更多设计良好的临床前和临床研究来检验槲皮素在心血管疾病中的治疗机制和临床疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/43ba/9412669/bb50930bd35f/pharmaceuticals-15-01019-g001.jpg

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