Department of Organic Chemistry, School of Chemical Sciences, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.
Department of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.
Life Sci. 2020 May 15;249:117512. doi: 10.1016/j.lfs.2020.117512. Epub 2020 Mar 5.
Hypertension is one of the leading causes of mortality in relation to the cardiovascular conditions and easily the most overlooked and poorly managed disease in mankind. With well over 200 drugs available in the market globally, there is still an urgency to search for antihypertensive alternatives due to the subpar efficacy and unwarranted side effects of the current choices. Present studies reported over 250 types of plant-derived compounds were being investigated for potential pharmacological effects on the vasculature in the last 3 decades. There were numerous literatures that claimed various compounds exhibiting vasorelaxant properties to a certain extent with low numbers of these compounds being successfully adapted into the current medicinal practice for treatment of hypertension. The issue is the scarcity of reviews that summarizes the discovery of this field and the lack of thorough comparison of these compounds to identify which of these vasodilators should be the next face of hypertension management. Thus, this review is aiming towards identifying the relationship between a major class of plant-derived compounds, flavonoid's activity as a vasodilator with their signalling pathways and their structural characteristics according to their vasorelaxant properties. Interestingly, we found that both nitric oxide and voltage-operated calcium channels pathways, and two of the flavonoid's structural characteristics play crucial roles in eliciting strong vasorelaxant effects. We have faith that the insights of this review will serve as a reference for those researching similar topics in the future and potentially lead to the development of more promising antihypertensive alternative.
高血压是心血管疾病相关死亡的主要原因之一，也是人类最容易被忽视和管理不善的疾病。目前全球市场上有超过 200 种药物，但由于现有选择的疗效不佳和不必要的副作用，仍然迫切需要寻找抗高血压的替代品。过去 30 年的研究报告称，有 250 多种植物衍生化合物正在被研究用于治疗血管的潜在药理学作用。有许多文献声称各种化合物在一定程度上具有血管舒张特性，但只有少数化合物成功地被应用于目前治疗高血压的医学实践中。问题是，缺乏对这一领域发现的综述，也缺乏对这些化合物的全面比较，以确定哪些血管扩张剂应该成为高血压管理的下一个焦点。因此，本综述旨在根据血管舒张特性，确定植物衍生化合物的一大类——类黄酮作为血管扩张剂的活性与其信号通路和结构特征之间的关系。有趣的是，我们发现一氧化氮和电压门控钙通道途径，以及类黄酮的两个结构特征，在引起强烈的血管舒张作用方面起着关键作用。我们相信，本综述的观点将为未来研究类似课题的人员提供参考，并有可能为开发更有前途的抗高血压替代品提供帮助。
