School of Pharmacy, University of Reading, Whiteknights, Reading RG6 6UB, UK.
Int J Mol Sci. 2019 Jun 25;20(12):3106. doi: 10.3390/ijms20123106.
Cardiovascular diseases represent a major cause of mortality and morbidity in the world, and specifically, thrombotic conditions such as heart attacks and strokes are caused by unwarranted activation of platelets and subsequent formation of blood clots (thrombi) within the blood vessels during pathological circumstances. Therefore, platelets act as a primary therapeutic target to treat and prevent thrombotic conditions. Current treatments are limited due to intolerance, and they are associated with severe side effects such as bleeding complications. Hence, the development of novel therapeutic strategies for thrombotic diseases is an urgent priority. Flavonoids are naturally occurring plant-derived molecules that exert numerous beneficial effects in humans through modulating the functions of distinct cell types. However, naturally occurring flavonoids suffer from several issues such as poor solubility, lipophilicity, and bioavailability, which hinder their efficacy and potency. Despite these, flavonoids act as versatile templates for the design and synthesis of novel molecules for various therapeutic targets. Indeed, several synthetic flavonoids have recently been developed to improve their stability, bioavailability, and efficacy, including for the modulation of platelet function. Here, we provide insight into the actions of certain natural flavonoids along with the advantages of synthetic flavonoids in the modulation of platelet function, haemostasis, and thrombosis.
心血管疾病是世界范围内主要的死亡和发病原因，特别是在病理情况下，血栓形成情况如心脏病发作和中风是由血小板的不必要激活以及随后在血管内形成血栓（血栓）引起的。因此，血小板是治疗和预防血栓形成情况的主要治疗靶点。目前的治疗方法受到耐受性的限制，并且与出血并发症等严重副作用相关。因此，开发治疗血栓性疾病的新型治疗策略是当务之急。类黄酮是天然存在的植物衍生分子，通过调节不同细胞类型的功能，在人类中发挥多种有益作用。然而，天然类黄酮存在溶解度差、亲脂性和生物利用度低等问题，这阻碍了它们的疗效和效力。尽管如此，类黄酮仍然是设计和合成各种治疗靶点新型分子的多功能模板。事实上，最近已经开发出几种合成类黄酮来提高它们的稳定性、生物利用度和疗效，包括调节血小板功能。在这里，我们提供了某些天然类黄酮以及合成类黄酮在调节血小板功能、止血和血栓形成方面的作用的见解。
