Fu Yuqi, Yang Le, Liu Lei, Kong Ling, Sun Hui, Sun Ye, Yin Fengting, Yan Guangli, Wang Xijun
State Key Laboratory of Integration and Innovation of Classic Formula and Modern Chinese Medicine, National Chinmedomics Research Center, National TCM Key Laboratory of Serum Pharmacochemistry, Metabolomics Laboratory, Department of Pharmaceutical Analysis, Heilongjiang University of Chinese Medicine, Heping Road 24, Harbin 150040, China.
State Key Laboratory of Dampness Syndrome, The Second Affiliated Hospital Guangzhou University of Chinese Medicine, Dade Road 111, Guangzhou 510006, China.
Pharmaceuticals (Basel). 2024 Dec 10;17(12):1665. doi: 10.3390/ph17121665.
Rhein is a natural active ingredient in traditional Chinese medicine that has attracted much attention due to its wide range of pharmacological activities. However, its clinical application is limited by low water solubility, poor oral absorption, and potential toxicity to the liver and kidneys. Recently, advanced extraction and synthesis techniques have made it possible to develop derivatives of rhein, which have better pharmacological properties and lower toxicity. This article comprehensively summarizes the biological activity and action mechanism of rhein. Notably, we found that TGF-1 is the target of rhein improving tissue fibrosis, while NF-B is the main target of its anti-inflammatory effect. Additionally, we reviewed the current research status of the pharmacokinetics, toxicology, structural optimization, and potential drug applications of rhein and found that the coupling and combination therapy of rhein and other active ingredients exhibit a synergistic effect, significantly enhancing therapeutic efficacy. Finally, we emphasize the necessity of further studying rhein's pharmacological mechanisms, toxicology, and development of analogs, aiming to lay the foundation for its widespread clinical application as a natural product and elucidate its prospects in modern medicine.
大黄素是中药中的一种天然活性成分，因其广泛的药理活性而备受关注。然而，其临床应用受到低水溶性、口服吸收差以及对肝脏和肾脏潜在毒性的限制。近年来，先进的提取和合成技术使得开发大黄素衍生物成为可能，这些衍生物具有更好的药理特性和更低的毒性。本文全面总结了大黄素的生物活性及作用机制。值得注意的是，我们发现转化生长因子-1是大黄素改善组织纤维化的靶点，而核因子-κB是其抗炎作用的主要靶点。此外，我们综述了大黄素的药代动力学、毒理学、结构优化及潜在药物应用的研究现状，发现大黄素与其他活性成分的联合及联合疗法具有协同效应，显著提高了治疗效果。最后，我们强调进一步研究大黄素的药理机制、毒理学及类似物开发的必要性，旨在为其作为天然产物广泛应用于临床奠定基础，并阐明其在现代医学中的前景。
