Andrographolide, the main bioactive component separated from Andrographis paniculata in 1951, has been scrutinized with a modern drug discovery approach for anti-inflammatory properties since 1984. Identification of new uses of existing drugs can be facilitated by searching for evidence linking them to known or yet undiscovered drug targets and human disease states to develop new therapeutic indications.Furthermore, a wide spectrum of biological properties of andrographolide such as anticancer, antibacterial, antiviral, hepatoprotective, antioxidant, anti-malarial, anti-atherosclerosis are also reported. However, poor water solubility and instability limit its clinical application. It becomes crucial to enhance its pharmacological function and find a new treatment option for more diseases. Therefore, this article reviews the major recent developments in andrographolide, including repurposing applications in different diseases and underlying mechanisms, particularly focusing on pharmacological enhancement of andrographolide such as derivatives, chemical modifications with potent biological activity and drug delivery. The repurposing and pharmacological enhancement of andrographolide would not only have exciting therapeutic potential to different diseases to facilitate drug marketing, but also decrease the economic burden on healthcare worldwide.

穿心莲内酯是1951年从穿心莲中分离出的主要生物活性成分，自1984年以来就已经通过现代药物发现方法进行了研究，以研究其抗炎特性。尚未发现的药物靶标和人类疾病状态将开发新的治疗指征。此外，还报道了穿心莲内酯的广泛生物学特性，例如抗癌，抗菌，抗病毒，保肝，抗氧化，抗疟疾，抗动脉粥样硬化。但是，水溶性差和不稳定性限制了其临床应用。增强其药理功能并为更多疾病找到新的治疗选择至关重要。所以，本文回顾了穿心莲内酯最近的主要发展，包括重新定位在不同疾病和潜在机制中的应用，特别着重于穿心莲内酯的药理增强作用，例如衍生物，具有强大生物活性的化学修饰和药物传递。穿心莲内酯的再利用和药理增强作用不仅对各种疾病具有令人兴奋的治疗潜力，以促进药物销售，而且还减轻了全世界医疗保健的经济负担。