School of Medicine, South China University of Technology, Guangzhou, China; Division of Clinical Pharmacology, Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Rochester, MN, USA.
School of Medicine, South China University of Technology, Guangzhou, China.
Pharmacol Res. 2020 Oct;160:105079. doi: 10.1016/j.phrs.2020.105079. Epub 2020 Jul 15.
Pulsatilla Decoction (Bai-Tou-Weng-Tang) has been used medically in China for thousands of years for the treatment of diseases caused by bacteria. In recent decades, Pulsatilla Decoction is becoming a well-known formula prescription used for the treatment of ulcerative colitis in traditional Chinese medicine. Pulsatilla chinensis is the chief herbal source of Pulsatilla Decoction, and it is rich in triterpenoid saponins, such as anemoside B4, anemoside A3, and 23-hydroxybetulinic acid. Anemoside B4 is the most abundant of that group and has been used as a quality control marker for Pulsatilla chinensis. As the major active component of Pulsatilla chinensis, anemoside B4 has also received attention as a pure compound for its therapeutic potential. In this review, we systematically analyze the findings on triterpenoid saponins, especially anemoside B4, anemoside A3 and 23-hydroxybetulinic acid, included in Pulsatilla chinensis and Pulsatilla Decoction. We discuss the pharmacokinetics and tissue distribution of these triterpenoid saponins as well as their biological activities. We also summarize the pharmacological effects of anemoside B4 and its two possible metabolites, anemoside A3 and 23-hydroxybetulinic acid, as pure compounds. In summary, this review sketches a profile of the state of existing knowledge with regard to the pharmacological effects of anemoside B4, especially its anti-inflammatory and immunomodulatory effects. These findings point to the possibility that anemoside B4 has potential to be studied further as a natural compound-originated immunomodulatory agent for the treatment of inflammatory diseases such as ulcerative colitis and thus, may represent one of the most important active components of Pulsatilla Decoction responsible for its anti-ulcerative colitis efficacy.
白头翁汤在中国被用于医学治疗已有数千年历史，可治疗由细菌引起的疾病。近几十年来，白头翁汤已成为一种著名的中药方剂，用于治疗溃疡性结肠炎。白头翁是白头翁汤的主要草药来源，富含三萜皂苷，如白头翁皂苷 B4、白头翁皂苷 A3 和 23-羟基白桦酸。白头翁皂苷 B4 是该组中最丰富的一种，已被用作白头翁质量控制的标志物。作为白头翁的主要活性成分，白头翁皂苷 B4 因其治疗潜力也受到关注。在本综述中，我们系统地分析了白头翁和白头翁汤中包含的三萜皂苷，特别是白头翁皂苷 B4、白头翁皂苷 A3 和 23-羟基白桦酸的研究结果。我们讨论了这些三萜皂苷的药代动力学和组织分布及其生物学活性。我们还总结了白头翁皂苷 B4 及其两种可能代谢物白头翁皂苷 A3 和 23-羟基白桦酸作为纯化合物的药理作用。总之，本综述概述了关于白头翁皂苷 B4 的药理作用的现有知识状态，特别是其抗炎和免疫调节作用。这些发现表明，白头翁皂苷 B4 有可能作为一种天然化合物衍生的免疫调节剂进一步研究，用于治疗溃疡性结肠炎等炎症性疾病，因此，可能是白头翁汤治疗溃疡性结肠炎疗效的最重要活性成分之一。
