松果菊苷药动/药效研究进展与思考

Progress and thoughts on pharmacodynamics and pharmacokinetics of echinacoside

本文综述了近年来松果菊苷(ECH)在抗衰老、提高记忆力与神经保护、抗肿瘤、保护肝脏及免疫调节等方面的药理作用研究进展,探讨了其可能的作用机制。此外,还对ECH的吸收和代谢等药代动力学最新研究进展进行总结,并将其药效学特征与药代动力学行为进行联系与比较,指出了ECH药效学和药代动力学之间存在的表面矛盾,并就如何解释这些矛盾进行了探讨。在此基础上,提出天然来源的创新药物通常具有系统前广泛代谢的特点,发挥整体药效作用的可能是其活性代谢产物;应针对中药I类新药的这些特点,加强系统前代谢转化研究;并制订科学合理的临床前药物代谢动力学技术指导原则,用以指导具有类似特点的中药I类新药的研究。

This review makes a summary on the pharmacological effects and involved mecha nisms of echinacoside（ECH）, including anti-aging, memory improvement, neuro-protective, anti-tumor, liver protective, and immunoloregulation. Besides, the advances in pharmacokinetics of ECH such as absorption and metabolism are also summarized. Based on such summaries, this paper furthers the discussions on the apparent contradiction between the observed pharmacological effects and pharmacokinetic behaviors of ECH. Based on the above, this paper points out the natural sourced innovative drugs were usually characterized on its extensively pre-system metabolism. The overall affection may be contributed by their active metabolites. To aim directly at such characteristics of Type I the tradi tional Chinese medicine （TCM） new drugs, we should strengthen the research on pre-system metabolic transformation, as well as establishing scientific and reasonable preclinical pharmacoki netic guiding principle, to direct the research of Type I TCM new drugs with similar characteristics.