Kunming Medical University School of Public Health, Kunming, Yunnan, China.
Health Effects Laboratory Division, National Institute for Occupational Safety and Health, Centers for Disease Control and Prevention, Morgantown, WV, USA.
Pharmacol Ther. 2018 Oct;190:105-127. doi: 10.1016/j.pharmthera.2018.05.006. Epub 2018 May 6.
Stroke and myocardial infarction are among the most common causes of mortality and disability in the world. The ischemic injury underlying these illnesses is complex, involving intricate interplays among many biological functions including energy metabolism, vascular regulation, hemodynamics, oxidative stress, inflammation, platelet activation, and tissue repair that take place in a context- and time-dependent manner. The current drug therapy of choice is to timely resupply the blood to the ischemic tissue; but reperfusion may introduce additional harm to the tissue through a process known as ischemia/reperfusion injury. As such, new drugs that would complement reperfusion by providing neural and cardiovascular protection and by targeting multiple abnormalities in ischemia are receiving increased attention. Scutellarin is an herbal flavonoid glucuronide with multiple pharmacological activities. Owing to its multiple beneficial effects, such as anti-oxidant, anti-inflammation, vascular relaxation, anti-platelet, anti-coagulation, and myocardial protection, scutellarin has been used clinically to treat stroke, myocardial infarction, and diabetic complications. Over the past three decades, clinical and pharmacological studies have accumulated a body of evidence that not only demonstrated these therapeutic effects, but also provided significant insights into the pharmacokinetic behavior, therapeutic profile, and mode of action of scutellarin in humans and animal models. Medicinal modification and new drug delivery methods have led to the development of new derivatives and formulations of scutellarin with improved bioavailability, efficacy, and safety. Here we review the current literature on scutellarin to provide a comprehensive understanding of the pharmacological activity, mechanism of action, toxicity, and therapeutic potential of scutellarin for the treatment of ischemia, diabetic complications, and other chronic diseases.
中风和心肌梗死是世界上最常见的死亡和残疾原因之一。这些疾病的缺血性损伤很复杂，涉及许多生物学功能的复杂相互作用，包括能量代谢、血管调节、血液动力学、氧化应激、炎症、血小板激活和组织修复，这些过程发生在依赖上下文和时间的方式中。目前的药物治疗选择是及时向缺血组织供应血液；但再灌注可能会通过一种称为缺血/再灌注损伤的过程给组织带来额外的伤害。因此，新的药物通过提供神经和心血管保护以及针对缺血的多种异常来补充再灌注，越来越受到关注。野黄芩苷是一种具有多种药理活性的草药类黄酮葡萄糖醛酸苷。由于其多种有益作用，如抗氧化、抗炎、血管舒张、抗血小板、抗凝和心肌保护作用，野黄芩苷已在临床上用于治疗中风、心肌梗死和糖尿病并发症。在过去的三十年中，临床和药理学研究积累了大量证据，不仅证明了这些治疗作用，而且还为野黄芩苷在人类和动物模型中的药代动力学行为、治疗特征和作用机制提供了重要的见解。药物修饰和新的药物递送方法导致了野黄芩苷新衍生物和制剂的开发，这些新衍生物和制剂具有改善的生物利用度、疗效和安全性。在这里，我们综述了野黄芩苷的现有文献，以全面了解野黄芩苷治疗缺血、糖尿病并发症和其他慢性疾病的药理活性、作用机制、毒性和治疗潜力。
