Flavonoids isolated from medicinal herbs have been utilized as valuable health-care agents due to their virous biological applications. Alpinetin is a natural flavonoid that emerges in many widely used medicinal plants, and has been frequently applied in Chinese patent drugs. Accumulated evidence has demonstrated that alpinetin possesses a broad range of pharmacological activities such as antitumor, antiinflammation, hepatoprotective, cardiovascular protective, lung protective, antibacterial, antiviral, neuroprotective, and other properties through regulating multiple signaling pathways with low systemic toxicity. However, pharmacokinetic studies have documented that alpinetin may have poor oral bioavailability correlated to its extensive glucuronidation. Currently, the reported pharmacological properties and pharmacokinetics profiles of alpinetin are rare to be scientifically reviewed. In this article, we aimed to highlight the mechanisms of action of alpinetin in various diseases to strongly support its curative potentials for prospective clinical applications. We also summarized the pharmacokinetics properties and proposed some viable strategies to convey an appreciable reference for future advances of alpinetin in drug development.

从药材中分离出来的黄酮类化合物由于其具有毒性的生物学应用而被用作有价值的保健剂。山楂素是一种天然黄酮类化合物，存在于许多广泛使用的药用植物中，并在中成药中得到频繁应用。积累的证据表明，alpinetin通过调节多种信号通路具有低全身毒性，具有广泛的药理活性，如抗肿瘤、抗炎、保肝、保护心血管、保护肺、抗菌、抗病毒、保护神经等。然而，药代动力学研究表明，alpinetin 的口服生物利用度可能较差，这与其广泛的葡萄糖醛酸化有关。现在，报道的高山青素药理特性和药代动力学特征很少得到科学审查。在本文中，我们旨在强调高山青素在各种疾病中的作用机制，以强烈支持其在前瞻性临床应用中的治疗潜力。我们还总结了药代动力学特性，并提出了一些可行的策略，为山药在药物开发中的未来进展提供可观的参考。