Li Xiao-Jiaoyang, Jiang Zhen-Zhou, Zhang Lu-yong
Jiangsu Center of Drug Screening, China Pharmaceutical University, Nanjing 210009, China.
Jiangsu Center of Drug Screening, China Pharmaceutical University, Nanjing 210009, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, China Pharmaceutical University, Nanjing 210009, China.
J Ethnopharmacol. 2014 Aug 8;155(1):67-79. doi: 10.1016/j.jep.2014.06.006. Epub 2014 Jun 13.
Tripterygium wilfordii Hook. f. (Tripterygium wilfordii), also known as Huangteng and gelsemium elegan, is a traditional Chinese medicine that has been marketed in China as Tripterygium wilfordii glycoside tablets. Triptolide (TP), an active component in Tripterygium wilfordii extracts, has been used to treat various diseases, including lupus, cancer, rheumatoid arthritis and nephritic syndrome. This review summarizes recent developments in the research on the pharmacodynamics, pharmacokinetics, pharmacy and toxicology of TP, with a focus on its novel mechanism of reducing toxicity. This review provides insight for future studies on traditional Chinese medicine, a field that is both historically and currently important.
We included studies published primarily within the last five years that were available in online academic databases (e.g., PubMed, Google Scholar, CNKI, SciFinder and Web of Science).
TP has a long history of use in China because it displays multiple pharmacological activities, including anti-rheumatism, anti-inflammatory, anti-tumor and neuroprotective properties. It has been widely used for the treatment of various diseases, such as rheumatoid arthritis, nephritic syndrome, lupus, Behcet׳s disease and central nervous system diseases. Recently, numerous breakthroughs have been made in our understanding of the pharmacological efficacy of TP. Although TP has been marketed as a traditional Chinese medicine, its multi-organ toxicity prevents it from being widely used in clinical practice.
Triptolide, a biologically active natural product extracted from the root of Tripterygium wilfordii, has shown promising pharmacological effects, particularly as an anti-tumor agent. Currently, in anti-cancer research, more effort should be devoted to investigating effective anti-tumor targets and confirming the anti-tumor spectrum and clinical indications of novel anti-tumor pro-drugs. To apply TP appropriately, with high efficacy and low toxicity, the safety and non-toxic dose range for specific target organs and diseases should be determined, the altered pathways and mechanisms of exposure need to be clarified, and an early warning system for toxicity needs to be established. With further in-depth study of the efficacy and toxicity of TP, we believe that TP will become a promising multi-use drug with improved clinical efficacy and safety in the future.
雷公藤（Tripterygium wilfordii Hook. f.），又称黄藤和断肠草，是一种传统中药，在中国已作为雷公藤多苷片上市。雷公藤甲素（TP）是雷公藤提取物中的一种活性成分，已被用于治疗多种疾病，包括狼疮、癌症、类风湿性关节炎和肾病综合征。本综述总结了TP在药效学、药代动力学、药剂学和毒理学研究方面的最新进展，重点关注其降低毒性的新机制。本综述为传统中药这一历史悠久且当下仍很重要的领域的未来研究提供了见解。
我们纳入了主要在过去五年内发表于在线学术数据库（如PubMed、谷歌学术、中国知网、SciFinder和科学引文索引）的研究。
TP在中国有悠久的使用历史，因为它具有多种药理活性，包括抗风湿、抗炎、抗肿瘤和神经保护特性。它已被广泛用于治疗各种疾病，如类风湿性关节炎、肾病综合征、狼疮、白塞病和中枢神经系统疾病。最近，我们对TP药理作用的认识有了许多突破。尽管TP已作为传统中药上市，但其多器官毒性使其无法在临床实践中广泛应用。
雷公藤甲素是从雷公藤根中提取的一种具有生物活性的天然产物，已显示出有前景的药理作用，尤其是作为一种抗肿瘤药物。目前，在抗癌研究中，应更加努力地研究有效的抗肿瘤靶点，并确认新型抗肿瘤前药的抗肿瘤谱和临床适应症。为了合理应用TP，实现高效低毒，应确定特定靶器官和疾病的安全和无毒剂量范围，阐明暴露途径和机制的改变，并建立毒性预警系统。随着对TP疗效和毒性的进一步深入研究，我们相信TP未来将成为一种有前景的多用途药物，临床疗效和安全性将得到改善。
