College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, PR China.
College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, PR China.
Biomed Pharmacother. 2020 May;125:110002. doi: 10.1016/j.biopha.2020.110002. Epub 2020 Feb 25.
As a universal Chinese medicine, Rhei Radix et Rhizoma was used for centuries in different fields including pharmaceutical, health care and cosmetics. Chrysophanol (Chr) is one of the most important anthraquinone components isolated from plants of the Rheum genus. Current reports show that in Rheum officinale, Chr is the most abundant free anthraquinone compound [1] and exerts a number of beneficial effects, such as anti-inflammation, anti-cancer, and anti-depressive effects and offers neuroprotection. We collected information about Chr from the Internet databases PubMed, Web of Science, Europe PMC and CNKI with a combination of keywords including "Chr", "Pharmacology", and "Pharmacokinetics". All data about this ingredient in this review were extracted from articles published before September 2019. Based on the literature found, we concluded that (1) Chr exhibited potential anti-inflammation, anti-cardiovascular disease (CVD)and anti-cancer activities by regulating signaling pathway transduction (NF-κB, MAPK, PI3K/Akt, etc.); (2) compared with free Chr, pharmacokinetic studies revealed that other forms of Chr, such as nanoparticle-based and liposome-based Chr, showed high bioavailability. Nevertheless, we also found that the understanding of the exact differences in the regulation of multiple molecular signaling pathways is in a preliminary stage and needs to be clarified. Moreover, further studies are required to determine the apoptotic mechanism of Chr in cancer cells. Finally, we found that (3) structure modification studies demonstrated potential relationships between structure and drug activity. The purpose of this review is to summarize the pharmacological activities, intracorporal processes and structure-activity relationships of Chr and to provide an up-to-date reference for further research and clinical applications.
作为一种通用的中药,大黄已经在医药、保健和化妆品等不同领域使用了几个世纪。大黄酸(Chr)是从大黄属植物中分离得到的最重要的蒽醌类成分之一。目前的研究报告表明,在大黄中,Chr 是最丰富的游离蒽醌化合物[1],具有多种有益作用,如抗炎、抗癌、抗抑郁作用和神经保护作用。我们从互联网数据库 PubMed、Web of Science、Europe PMC 和中国知网(CNKI)中收集了有关 Chr 的信息,关键词组合包括“Chr”、“药理学”和“药代动力学”。本综述中关于该成分的所有数据均从 2019 年 9 月之前发表的文章中提取。基于文献研究,我们得出结论:(1)Chr 通过调节信号通路转导(NF-κB、MAPK、PI3K/Akt 等),显示出潜在的抗炎、抗心血管疾病(CVD)和抗癌活性;(2)与游离 Chr 相比,药代动力学研究表明,其他形式的 Chr,如基于纳米粒子和基于脂质体的 Chr,表现出较高的生物利用度。然而,我们也发现,对多种分子信号通路调节的确切差异的理解还处于初步阶段,需要进一步澄清。此外,还需要进一步研究以确定 Chr 在癌细胞中的凋亡机制。最后,我们发现:(3)结构修饰研究表明结构与药物活性之间存在潜在关系。本综述的目的是总结 Chr 的药理学活性、体内过程和构效关系,为进一步的研究和临床应用提供最新参考。