Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China.
Molecules. 2019 Jun 24;24(12):2323. doi: 10.3390/molecules24122323.
Pinocembrin is one of the most abundant flavonoids in propolis, and it may also be widely found in a variety of plants. In addition to natural extraction, pinocembrin can be obtained by biosynthesis. Biosynthesis efficiency can be improved by a metabolic engineering strategy and a two-phase pH fermentation strategy. Pinocembrin poses an interest for its remarkable pharmacological activities, such as neuroprotection, anti-oxidation, and anti-inflammation. Studies have shown that pinocembrin works excellently in treating ischemic stroke. Pinocembrin can reduce nerve damage in the ischemic area and reduce mitochondrial dysfunction and the degree of oxidative stress. Given its significant efficacy in cerebral ischemia, pinocembrin has been approved by China Food and Drug Administration (CFDA) as a new treatment drug for ischemic stroke and is currently in progress in phase II clinical trials. Research has shown that pinocembrin can be absorbed rapidly in the body and easily cross the blood-brain barrier. In addition, the absorption/elimination process of pinocembrin occurs rapidly and shows no serious accumulation in the body. Pinocembrin has also been found to play a role in Parkinson's disease, Alzheimer's disease, and specific solid tumors, but its mechanisms of action require in-depth studies. In this review, we summarized the latest 10 years of studies on the biosynthesis, pharmacological activities, and pharmacokinetics of pinocembrin, focusing on its effects on certain diseases, aiming to explore its targets, explaining possible mechanisms of action, and finding potential therapeutic applications.
乔松素是蜂胶中含量最丰富的类黄酮之一，也可能广泛存在于多种植物中。除了天然提取，乔松素也可以通过生物合成获得。通过代谢工程策略和两相 pH 发酵策略可以提高生物合成效率。乔松素因其显著的药理活性而备受关注，如神经保护、抗氧化和抗炎作用。研究表明，乔松素在治疗缺血性中风方面效果显著。乔松素可以减少缺血区域的神经损伤，减少线粒体功能障碍和氧化应激程度。鉴于其在脑缺血方面的显著疗效，乔松素已被中国食品药品监督管理局（CFDA）批准为缺血性中风的新药，目前正在进行 II 期临床试验。研究表明，乔松素在体内能迅速吸收，容易穿过血脑屏障。此外，乔松素的吸收/消除过程迅速，体内不会出现严重的蓄积。乔松素还被发现对帕金森病、阿尔茨海默病和某些实体肿瘤有作用，但作用机制仍需深入研究。本综述总结了近 10 年来关于乔松素的生物合成、药理活性和药代动力学的研究，重点关注其对某些疾病的影响，旨在探索其靶点，解释可能的作用机制，并寻找潜在的治疗应用。
