PPD 型人参皂苷衍生物的结构修饰、生物活性及构效关系的研究进展。
Insight on structural modification, biological activity, structure-activity relationship of PPD-type ginsenoside derivatives.
机构信息
College of Chemical Engineering, Department of Pharmaceutical Engineering, Northwest University, 229 Taibai North Road, Xi'an 710069, China.
College of Chemical Engineering, Department of Pharmaceutical Engineering, Northwest University, 229 Taibai North Road, Xi'an 710069, China; Shaanxi Key Laboratory of Degradable Biomedical Materials, School of Chemical Engineering, Northwest University, 229 Taibai North Road, Xi'an 710069, China; Biotech. & Biomed. Research Institute, School of Chemical Engineering, Northwest University, 229 Taibai North Road, Xi'an 710069, China.
出版信息
Fitoterapia. 2022 Apr;158:105135. doi: 10.1016/j.fitote.2022.105135. Epub 2022 Jan 31.
Ginsenosides, characterized by triterpenoid, are one of the active components of ginseng. Among them, PPD-type ginsenosides have potent and diverse pharmacological activities, while the effective applications and clinical studies are limited by the poor stability, water solubility and oral bioavailability. In this review, we have attempted to demonstrate the structural-activity relationship of chemical modifications on the dammarane-type skeleton and the C-17 side chain, noting that certain structurally modified derivatives exhibit satisfactory pharmacological activity. This review will provide ideas for the design and synthesis of novel PPD derivatives, and valuable help for the further study of PPD derivatives to make it realize clinical application.
人参皂苷以三萜为特征，是人参的有效成分之一。其中，PPD 型人参皂苷具有强大多样的药理活性，但由于其稳定性差、水溶性和口服生物利用度低，有效应用和临床研究受到限制。本综述试图展示对达玛烷骨架和 C-17 侧链进行化学修饰的结构-活性关系，并指出某些结构修饰的衍生物表现出令人满意的药理活性。本综述将为新型 PPD 衍生物的设计和合成提供思路，为进一步研究 PPD 衍生物实现临床应用提供有价值的帮助。
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