雷公藤甲素前药的研究进展

潘祥; 王均伟; 胡立宏

雷公藤甲素前药的研究进展

南京中医药大学药学院，江苏省中药功效物质重点实验室，江苏南京 210023

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出版历程
- 刊出日期: 2020-09-10

Research Progress of Triptolide Prodrugs

摘要

摘要: 雷公藤制剂是中药中治疗自身免疫疾病的首选药物，在治疗类风湿性关节炎、肾小球肾炎和多种癌症中显示卓越疗效。雷公藤甲素被认为是雷公藤制剂中最主要的活性成分，具有免疫抑制、抗炎、抗肿瘤等多种药理活性。但雷公藤甲素自身存在毒性较大、水溶性差、治疗窗口窄等成药性缺陷，极大地限制了其临床应用。雷公藤甲素的毒性源自其产生药效的作用机制，常规的结构修饰很难改善其成药性，因此，如何实现雷公藤甲素的减毒增效是目前迫切需要解决的问题。通过前药设计策略，改善水溶性、提高药物靶向性，有望解决雷公藤甲素成药性差的问题。
- 雷公藤甲素 /
- 成药性 /
- 结构修饰 /
- 前药
Abstract: The preparations of Tripterygium wilfordii Hook F. have been widely used for the treatment of autoimmune and inflammatory diseases， and they show excellent curative effects in attenuating rheumatoid arthritis， glomerulonephritis and cancers. Triptolide (TPL) was determined as the primary biologically active ingredient of Tripterygium wilfordii. However， it shows high toxicity， poor water solubility， and narrow therapeutic window， which greatly limits its clinical applications. It was reported that the toxicity of triptolide originated from the mechanism of its medicinal effect， thus conventional structural modification was difficult to improve its druggability. Therefore， how to reduce the toxicity and increase the efficacy of triptolide is a problem needs to be solved urgently. It is expected to solve the problem of poor druggability of triptolide by improving water solubility and targeted delivery through the strategy of prodrug design.
- triptolide /
- druggability /
- structural modification /
- prodrug

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参考文献(25)

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